40 results on '"J. J. D'Angelo"'
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2. GENITO-URINARY
- Author
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B. Milligan, J. W. Best, and J. J. Angelo
- Subjects
Surgery - Published
- 1962
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3. Photo-oxidation of NO using an exterior paint--screening of various commercial titania in powder pressed and paint films.
- Author
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Aguia C, Angelo J, Madeira LM, and Mendes A
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- Catalysis, Kinetics, Ultraviolet Rays, Air Pollution prevention & control, Nitric Oxide chemistry, Paint analysis, Photochemical Processes, Titanium chemistry
- Abstract
The present work aims to evaluate the photocatalytic activity of photo-TiO(2) from various producers (Evonik, Kemira, Kronos, Millennium, Sachtleben and Tayca), in the form of powder pressed films and upon incorporation in a water-based paint, for outdoor NO abatement. The photocatalytic activity of the different samples was evaluated in terms of NO conversion and selectivity towards nitrite and nitrate ions following approximately the ISO 22197-1:2007(E) standard. The highest yields obtained for powder pressed films were achieved with VLP7000 (0.70), followed by VLP7101 (0.55) and UVLP7500 (0.55), all from Kronos. On the other hand, when incorporated in paint films, the highest yields were obtained with PC500 and PC105 from Millennium and UV100 from Sachtleben (ca. 0.15). The paint matrix plays an important role on the photocatalytic activity. In particular, the time for steady state is one or two orders of magnitude higher when the photocatalysts are incorporated in paint films in relation to the powder pressed films. The paint films were activated following the procedure recommended by the above-mentioned standard. However, the photocatalytic activity of films incorporating P25 (Evonik) was displayed only when higher power radiation and higher humidity conditions were used. This allowed for similar levels of photocatalytic activity as the other paint films., (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Published
- 2011
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4. Crystal and electronic structures of magnesium(II), copper(II), and mixed magnesium(II)-copper(II) complexes of the quinoline half of styrylquinoline-type HIV-1 integrase inhibitors.
- Author
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Courcot B, Firley D, Fraisse B, Becker P, Gillet JM, Pattison P, Chernyshov D, Sghaier M, Zouhiri F, Desmaële D, d'Angelo J, Bonhomme F, Geiger S, and Ghermani NE
- Subjects
- Computer Simulation, Crystallization, Crystallography, X-Ray, Electrons, HIV Integrase Inhibitors chemical synthesis, Hydrogen Bonding, Models, Chemical, Models, Molecular, Molecular Structure, Organometallic Compounds chemical synthesis, Quantum Theory, Static Electricity, Copper chemistry, HIV Integrase Inhibitors chemistry, Magnesium chemistry, Organometallic Compounds chemistry, Quinolines chemistry
- Abstract
A new target in AIDS therapy development is HIV-1 integrase (IN). It was proven that HIV-1 IN required divalent metal cations to achieve phosphodiester bond cleavage of DNA. Accordingly, all newly investigated potent IN inhibitors contain chemical fragments possessing a high ability to chelate metal cations. One of the promising leads in the polyhydroxylated styrylquinolines (SQLs) series is (E)-8-hydroxy-2-[2-(4,5-dihydroxy-3-methoxyphenyl)-ethenyl]-7-quinoline carboxylic acid (1). The present study focuses on the quinoline-based progenitor (2), which is actually the most probable chelating part of SQLs. Conventional and synchrotron low-temperature X-ray crystallographic studies were used to investigate the chelating power of progenitor 2. Mg2+ and Cu2+ cations were selected for this purpose, and three types of metal complexes of 2 were obtained: Mg(II) complex (4), Cu(II) complex (5) and mixed Mg(II)-Cu(II) complexes (6 and 7). The analysis of the crystal structure of complex 4 indicates that two tridentate ligands coordinate two Mg2+ cations, both in octahedral geometry. The Mg-Mg distance was found equal to 3.221(1) A, in agreement with the metal-metal distance of 3.9 A encountered in the crystal structure of Escherichia coli DNA polymerase I. In 5, the complex is formed by two bidentate ligands coordinating one copper ion in tetrahedral geometry. Both mixed Mg(II)-Cu(II) complexes, 6 and 7 exhibit an original arrangement of four ligands linked to a central heterometallic cluster consisting of three octahedrally coordinated magnesium ions and one tetrahedrally coordinated copper ion. Quantum mechanics calculations were also carried out in order to display the electrostatic potential generated by the dianionic ligand 2 and complex 4 and to quantify the binding energy (BE) during the formation of the magnesium complex of progenitor 2. A comparison of the binding energies of two hypothetical monometallic Mg(II) complexes with that found in the bimetallic magnesium complex 4 was made.
- Published
- 2007
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5. Long-circulating PEGylated polycyanoacrylate nanoparticles as new drug carrier for brain delivery.
- Author
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Calvo P, Gouritin B, Chacun H, Desmaële D, D'Angelo J, Noel JP, Georgin D, Fattal E, Andreux JP, and Couvreur P
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- Animals, Blood-Brain Barrier, Chemical Phenomena, Chemistry, Physical, Diffusion, Drug Carriers, Drug Delivery Systems, Fluorescent Dyes, Isotope Labeling, Male, Mice, Microspheres, Particle Size, Permeability drug effects, Rats, Sucrose administration & dosage, Sucrose pharmacokinetics, Surface-Active Agents pharmacology, Suspensions, Tissue Distribution, Acrylic Resins pharmacokinetics, Brain metabolism, Polyethylene Glycols pharmacokinetics
- Abstract
Purpose: The aim of this study was to evaluate the ability of long-circulating PEGylated cyanoacrylate nanoparticles to diffuse into the brain tissue., Methods: Biodistribution profiles and brain concentrations of [14C]-radiolabeled PEG-PHDCA, polysorbate 80 or poloxamine 908-coated PHDCA nanoparticles, and uncoated PHDCA nanoparticles were determined by radioactivity counting after intravenous administration in mice and rats. In addition, the integrity of the blood-brain barrier (BBB) after nanoparticles administration was evaluated by in vivo quantification of the diffusion of [14C]-sucrose into the brain. The location of fluorescent nanoparticles in the brain was also investigated by epi-fluorescent microscopy., Results: Based on their long-circulating characteristics, PEGylated PHDCA nanoparticles penetrated into the brain to a larger extent than all the other tested formulations. Particles were localized in the ependymal cells of the choroid plexuses, in the epithelial cells of pia mater and ventricles, and to a lower extent in the capillary endothelial cells of BBB. These phenomena occurred without any modification of BBB permeability whereas polysorbate 80-coated nanoparticles owed, in part, their efficacy to BBB permeabilization induced by the surfactant. Poloxamine 908-coated nanoparticles failed to increase brain concentration probably because of their inability to interact with cells., Conclusions: This study proposes PEGylated poly (cyanoacrylate) nanoparticles as a new brain delivery system and highlights two requirements to design adequate delivery systems for such a purpose: a) long-circulating properties of the carrier, and b) appropriate surface characteristics to allow interactions with BBB endothelial cells.
- Published
- 2001
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6. HIV-1 integrase: the next target for AIDS therapy?
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d'Angelo J, Mouscadet JF, Desmaële D, Zouhiri F, and Leh H
- Subjects
- Animals, Anti-HIV Agents chemistry, Binding Sites drug effects, Cell Line, Crystallography, X-Ray, Drug Design, Enzyme Inhibitors chemistry, HIV Integrase chemistry, HIV-1 enzymology, HIV-1 physiology, Humans, Macromolecular Substances, Molecular Structure, Protein Conformation, Protein Structure, Tertiary, Quinolines chemistry, Rats, Recombinant Proteins antagonists & inhibitors, Virus Integration drug effects, Acquired Immunodeficiency Syndrome drug therapy, Anti-HIV Agents pharmacology, Enzyme Inhibitors pharmacology, HIV Integrase drug effects, HIV-1 drug effects, Quinolines pharmacology
- Abstract
HIV-1 is the aetiological agent of AIDS. Present treatment of AIDS uses a combination therapy with reverse transcriptase and protease inhibitors. Recently, the integrase (IN), the third enzyme of HIV-1 which is necessary for the integration process of proviral DNA into the host genome, has reached as a legitimate new drug target. Several families of inhibitors of the catalytic core domain of HIV-1 IN exhibiting submicromolar activities have now been identified. Our contribution in this field was related to the development of new polyhydroxylated styrylquinolines. The latter compounds have proved to be potent HIV-1 IN inhibitors, that block the replication of HIV-1 in cell culture, and are devoid of cytotoxicity. The crystal structure of the catalytically active core domain of a HIV-1 IN mutant has been determined. The active site region is identified by the position of two of the conserved carboxylate residues essential for catalysis, Asp64 and Asp116, which coordinate a Mg2+ ion, whereas the third catalytic residue, Glu152 does not participate in metal binding. However, a recent molecular dynamics simulation of the HIV-1 IN catalytic domain provides support to the hypothesis that a second metal ion is likely to be carried into the HIV-1 IN active site by the DNA substrate. The structure of a complex of the HIV-1 IN core domain with the inhibitor 5-CITEP has been recently reported. The inhibitor binds centrally in the active site of the IN and makes a number of close contacts with the protein, particularly with Lys156, Lys159 and Gln148, amino acids which were identified to be near the active site of the enzyme, through site-directed mutagenis and photo-crosslinking experiments. The exact mechanism by which HIV-1 IN inhibitors block the catalytic activity of the protein remains unknown. However, several putative pharmacophore components have been characterized. All these groups lie in a possible coordination to a divalent ion, supporting thus the hypothesis that the interaction causing the inhibition is mediated by one or two cations. Finally, among the HIV-1 IN inhibitors, three classes have proved to exhibit significant antiviral activities. Thus, it seems likely that the efficient use of HIV-1 IN as a target for rational design will become possible in the next future, possibly through the use of combination regimens including IN inhibitors.
- Published
- 2001
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7. The asymmetric Michael reaction involving chiral imines: recent progress at the Université Paris-Sud.
- Author
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Desmaële D, Cavé C, Dumas F, and d'Angelo J
- Published
- 2001
8. Design of folic acid-conjugated nanoparticles for drug targeting.
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Stella B, Arpicco S, Peracchia MT, Desmaële D, Hoebeke J, Renoir M, D'Angelo J, Cattel L, and Couvreur P
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- Capsules, Carrier Proteins metabolism, Excipients pharmacokinetics, Folate Receptors, GPI-Anchored, Folic Acid pharmacokinetics, Polyethylene Glycols pharmacokinetics, Drug Delivery Systems methods, Excipients chemistry, Folic Acid chemistry, Polyethylene Glycols chemistry, Receptors, Cell Surface, Surface Plasmon Resonance methods
- Abstract
The new concept developed in this study is the design of poly(ethylene glycol) (PEG)-coated biodegradable nanoparticles coupled to folic acid to target the folate-binding protein; this molecule is the soluble form of the folate receptor that is overexpressed on the surface of many tumoral cells. For this purpose, a novel copolymer, the poly[aminopoly(ethylene glycol)cyanoacrylate-co-hexadecyl cyanoacrylate] [poly(H(2)NPEGCA-co-HDCA)] was synthesized and characterized. Then nanoparticles were prepared by nanoprecipitation of the obtained copolymer, and their size, zeta potential, and surface hydrophobicity were investigated. Nanoparticles were then conjugated to the activated folic acid via PEG terminal amino groups and purified from unreacted products. Finally, the specific interaction between the conjugate folate-nanoparticles and the folate-binding protein was evaluated by surface plasmon resonance. This analysis confirmed a specific binding of the folate-nanoparticles to the folate-binding protein. This interaction did not occur with nonconjugated nanoparticles used as control. Thus, folate-linked nanoparticles represent a potential new drug carrier for tumor cell-selective targeting., (Copyright 2000 Wiley-Liss, Inc.)
- Published
- 2000
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9. Factors affecting the use of a single switch with assistive technology devices.
- Author
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Angelo J
- Subjects
- Equipment Design, Humans, Task Performance and Analysis, Disabled Persons, Motor Skills, Self-Help Devices
- Abstract
Identifying consumers' motor ability for consistent and reliable control can be a difficult yet essential part of a single switch assessment. Current literature does not identify the essential components of a single switch evaluation. Therefore, the following focus group study was conducted. Six occupational therapists with experience in assistive technology service delivery participated in a focus group meeting. The purpose of the meeting was to identify essential components of a single switch evaluation in the single switch assistive technology assessment. Eleven items were identified as essential to the single switch assessment. They are: reliability of motor movements, volitional nature of movement, safety, movements that are easily performed, endurance, activities and positions the client assumes throughout the day and evening, efficiency of movement, previous successful movements, ability to perform timed response, ability to activate the access device within a given time frame, and time between switch closures. The significance of this study is that essential components of a single switch evaluation were identified. Using this detailed information should lead to optimal switch placement and switch use.
- Published
- 2000
10. Near infrared with principal component analysis as a novel analytical approach for nanoparticle technology.
- Author
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Brigger I, Chaminade P, Desmaële D, Peracchia MT, d'Angelo J, Gurny R, Renoir M, and Couvreur P
- Subjects
- Magnetic Resonance Spectroscopy methods, Spectroscopy, Near-Infrared methods, Colloids chemistry, Polymers chemistry
- Abstract
Purpose: To progress in the characterization of a poly(MePEGcyanoacrylate-co-hexadecylcyanoacrylate) (poly(PEGCA-co-HDCA) copolymer and the nanoparticles formed from this copolymer., Methods: Poly(PEGCA-co-HDCA) at a MePEG/hexadecyl ratio of 1:4 was investigated by 1H-NMR and near infrared spectroscopy. The nanoparticle suspensions, obtained by the methods of nanoprecipitation or emulsion--solvent evaporation, as well as the crude nanoparticles and their dispersion medium--were analyzed by MePEG measurement, 1H-NMR, and near infrared spectroscopy., Results: The 1H-NMR results showed that the (poly(PEGCA-co-HDCA) copolymer obtained bore lateral hydrophilic MePEG chains and lateral hydrophobic hexadecyl chains in a final ratio of 1:4. However, this ratio, although reproducible from batch to batch, represented only a mean value for different molecular species. Indeed, our results demonstrated the formation of more hydrophobic poly(alkyl-cyanoacrylate) oligomers (with a higher content of hexadecyl chains) and other more hydrophilic oligomers (with a higher MePEG content). Only the more hydrophobic oligomers were able to form solid pegylated nanoparticles. As far as these nanoparticles were concerned, determination of their MePEG content allowed the calculation of a distance of 1.2 nm and 1.05 nm between 2 grafted MePEG chains at the nanoparticle surface, when obtained by nanoprecipitation and emulsion-solvent evaporation, respectively. Moreover, when the same copolymer batch was used, different nanoparticles were obtained according to the preparation method, as seen by near infrared spectroscopy., Conclusions: The nanoparticles obtained by nanoprecipitation or emulsion-solvent evaporation of poly(PEGCA-co-HDCA) 1:4 copolymer displayed a different supramolecular organization, as evidenced by the near infrared spectroscopy results. Moreover, these nanoparticles showed surface characteristics compatible with a long circulating carrier.
- Published
- 2000
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11. Modeling of the inhibition of retroviral integrases by styrylquinoline derivatives.
- Author
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Ouali M, Laboulais C, Leh H, Gill D, Desmaële D, Mekouar K, Zouhiri F, d'Angelo J, Auclair C, Mouscadet JF, and Le Bret M
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- Algorithms, Avian Sarcoma Viruses enzymology, Binding Sites, DNA metabolism, Enzyme Inhibitors metabolism, HIV Integrase chemistry, HIV Integrase Inhibitors metabolism, Integrases metabolism, Magnesium metabolism, Molecular Conformation, Molecular Structure, Quinolines metabolism, Recombinant Proteins metabolism, Static Electricity, Structure-Activity Relationship, Thermodynamics, Enzyme Inhibitors chemistry, HIV Integrase metabolism, HIV Integrase Inhibitors chemistry, HIV-1 enzymology, Models, Molecular, Quinolines chemistry
- Abstract
Styrylquinoline derivatives, known to be potent inhibitors of HIV-1 integrase, have been experimentally tested for their inhibitory effect on the disintegration reaction catalyzed by catalytic cores of HIV-1 and Rous sarcoma virus (RSV) integrases. A modified docking protocol, consisting of coupling a grid search method with full energy minimization, has been specially designed to study the interaction between the inhibitors and the integrases. The inhibitors consist of two moieties that have hydroxyl and/or carboxyl substituents: the first moiety is either benzene, phenol, catechol, resorcinol, or salicycilic acid; the hydroxyl substituents on the second (quinoline) moiety may be in the keto or in the enol forms. Several tautomeric forms of the drugs have been docked to the crystallographic structure of the RSV catalytic core. The computed binding energy of the keto forms correlates best with the measured inhibitory effect. The docking procedure shows that the inhibitors bind closely to the crystallographic catalytic Mg(2+) dication. Additional quantum chemistry computations show that there is no direct correlation between the binding energy of the drugs with the Mg(2+) dication and their in vitro inhibitory effect. The designed method is a leading way for identification of potent integrase inhibitors using in silico experiments.
- Published
- 2000
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12. Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture.
- Author
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Zouhiri F, Mouscadet JF, Mekouar K, Desmaële D, Savouré D, Leh H, Subra F, Le Bret M, Auclair C, and d'Angelo J
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- Anti-HIV Agents chemistry, Anti-HIV Agents pharmacology, Catalytic Domain, Cell Line, HIV Integrase chemistry, HIV Integrase Inhibitors chemistry, HIV Integrase Inhibitors pharmacology, Humans, Protein Binding, Quinolines chemistry, Quinolines pharmacology, Structure-Activity Relationship, Styrenes chemistry, Styrenes pharmacology, Virus Replication, Anti-HIV Agents chemical synthesis, HIV Integrase metabolism, HIV Integrase Inhibitors chemical synthesis, HIV-1 drug effects, Quinolines chemical synthesis, Styrenes chemical synthesis
- Abstract
Our prior studies showed that polyhydroxylated styrylquinolines are potent HIV-1 integrase (IN) inhibitors that block the replication of HIV-1 in cell culture at nontoxic concentrations. To explore the mechanism of action of these inhibitors, various novel styrylquinoline derivatives were synthesized and tested against HIV-1 IN and in cell-based assays. Regarding the in vitro experiments, the structural requirements for biological activity are a carboxyl group at C-7, a hydroxyl group at C-8 in the quinoline subunit, and an ancillary phenyl ring. However the in vitro inhibitory profile tolerates deep alterations of this ring, e.g. by the introduction of various substituents or its replacement by heteroatomic nuclei. Regarding the ex vivo assays, the structural requirements for activity are more stringent than for in vitro inhibition. Thus, in addition to an o-hydroxy acid group in the quinoline, the presence of one ortho pair of substituents at C-3' and C-4', particularly two hydroxyl groups, in the ancillary phenyl ring is imperatively required for inhibitory potency. Starting from literature data and the SARs developed in this work, a putative binding mode of styrylquinoline inhibitors to HIV-1 IN was derived.
- Published
- 2000
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13. Tautomers of styrylquinoline derivatives containing a methoxy substituent: computation of their population in aqueous solution and their interaction with RSV integrase catalytic core.
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Ouali M, Laboulais C, Leh H, Gill D, Xhuvani E, Zouhiri F, Desmaele D, d'Angelo J, Auclair C, Mouscadet JF, and Le Bret M
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- Catalytic Domain, Integrases chemistry, Quinones chemistry, Solutions, Spectrometry, Fluorescence, Stereoisomerism, Water chemistry, Avian Sarcoma Viruses enzymology, Integrases metabolism, Quinones metabolism
- Abstract
8-Hydroxy-2-[2-(3-hydroxy-4-methoxyphenyl)ethenyl]-7-quinoline carboxylic acid and 8-hydroxy-2-[2-(3-methoxy-4-hydroxyphenyl)ethenyl]-7-quinoline carboxylic acid inhibit the processing and strand transfer reactions catalyzed by HIV-1 integrase with an IC50 of 2 microM. Some of their spectral properties are briefly reported. Their fluorescence is so weak that it is of no use in an experimental determination of the binding to the protein and we resorted to computer simulation. Both styrylquinoline derivatives, in their monoanionic form, have several dozens of tautomers and each of these forms has four planar rotamers. In this work computer simulations have been performed to determine which tautomer is the most abundant in aqueous solution and which binds to the Rous sarcoma virus (RSV) integrase catalytic core. As the substituents on the quinoline moiety are the same as on salicylic acid, the energies of hydroxy benzoic acid tautomers were also computed both in vacuo and embedded in a continuous medium which had the dielectric constant of bulk water, using the recent CPCM technique. The CPCM method was then applied to the two integrase inhibitors to estimate the tautomer population in water. The binding site of the compounds on the RSV integrase catalytic core was determined through a docking protocol, consisting of coupling a grid search method with full energy minimization. The designed method is a way leading to identification of potent integrase inhibitors using in silico experiments.
- Published
- 2000
14. Visualization of in vitro protein-rejecting properties of PEGylated stealth polycyanoacrylate nanoparticles.
- Author
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Peracchia MT, Harnisch S, Pinto-Alphandary H, Gulik A, Dedieu JC, Desmaële D, d'Angelo J, Müller RH, and Couvreur P
- Subjects
- Adsorption, Animals, Blood Proteins isolation & purification, Drug Carriers, Electrophoresis, Gel, Two-Dimensional, Female, Freeze Fracturing, Humans, Injections, Intravenous, Mice, Mice, Inbred Strains, Biocompatible Materials chemistry, Blood Proteins chemistry, Cyanoacrylates chemistry, Fibrinogen chemistry, Polyethylene Glycols chemistry
- Abstract
The in vitro protein-rejecting properties of PEG-coated polyalkylcyanoacrylate (PACA) nanoparticles were for the first time visualized after freeze-fracture of the nanoparticles pre-incubated with fibrinogen as a model blood protein. The reduced protein association to the nanoparticles was evidenced also by two-dimensional PAGE after incubation of the nanoparticles with human plasma. In vivo experiments showed the 'stealth' long-circulating properties of the PEGylated nanoparticles after intravenous administration to mice. Thus, the images obtained after nanoparticle-protein incubation were predictive of the behavior observed in vivo. In conclusion, freeze-fracture analysis represents a novel and original qualitative approach to investigate the interactions between proteins and particulate systems.
- Published
- 1999
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15. Stealth PEGylated polycyanoacrylate nanoparticles for intravenous administration and splenic targeting.
- Author
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Peracchia MT, Fattal E, Desmaële D, Besnard M, Noël JP, Gomis JM, Appel M, d'Angelo J, and Couvreur P
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- Animals, Cell Line, Female, Injections, Intravenous, Mice, Tissue Distribution, Cyanoacrylates pharmacokinetics, Drug Carriers, Polyethylene Glycols pharmacokinetics, Polymers pharmacokinetics, Spleen metabolism
- Abstract
The aim of the present work was to investigate the biodistribution characteristics of PEG-coated polycyanoacrylate nanoparticles prepared by the nanoprecipitation/solvent diffusion method using the previously synthesized poly(MePEGcyanoacrylate-hexadecylcyanoacrylate) copolymer. It was observed that [14C]-radiolabeled PEGylated nanoparticles remained for a longer time in the blood circulation after intravenous administration to mice, compared to the non-PEGylated poly(hexadecylcyanoacrylate) (PHDCA) nanoparticles. Furthermore, hepatic accumulation was dramatically reduced, whereas a highly increased spleen uptake was shown. The PEGylation degree of the polymer seemed not to affect the in vivo behavior of the nanoparticles, whereas previously obtained in vitro data have shown a modification of plasma protein adsorption depending on the density of PEG at the surface of the particles. Moreover, the study of the in vitro cytotoxicity of the nanoparticles revealed that the PEGylation of the cyanoacrylate polymer reduced its toxicity. These results open up interesting perspectives for the targeting of drugs to other tissues than the liver.
- Published
- 1999
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16. Styrylquinoline derivatives: a new class of potent HIV-1 integrase inhibitors that block HIV-1 replication in CEM cells.
- Author
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Mekouar K, Mouscadet JF, Desmaële D, Subra F, Leh H, Savouré D, Auclair C, and d'Angelo J
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- Cell Line, Transformed, HIV Integrase genetics, HIV Integrase metabolism, HIV-1 enzymology, HIV-1 physiology, Humans, Mutation, Sequence Deletion, Tumor Cells, Cultured, Anti-HIV Agents chemical synthesis, Anti-HIV Agents pharmacology, Anti-HIV Agents toxicity, HIV Integrase Inhibitors chemical synthesis, HIV Integrase Inhibitors pharmacology, HIV Integrase Inhibitors toxicity, HIV-1 drug effects, Quinolines chemical synthesis, Quinolines pharmacology, Quinolines toxicity, Styrenes chemical synthesis, Styrenes pharmacology, Styrenes toxicity, Virus Replication drug effects
- Abstract
On the basis of the fact that several polynucleotidyl transferases, related to HIV integrase, contain in their active site two divalent metal cations, separated by ca. 4 A, new potential HIV integrase inhibitors were designed, in which a quinoline substructure is linked to an aryl nucleus possessing various hydroxy substitution patterns, by means of an ethylenic spacer. Although the most active compounds contain the catechol structure, this group is not essential for the activity, since compound 21 that lacks such a moiety is a potent drug, implicating the presence of a different pharmacophore. The most promising styrylquinolines thus synthesized inhibit HIV-1 integrase in vitro at micromolar or submicromolar concentrations and block HIV replication in CEM cells, with no significant cellular toxicity in a 5-day period assay. These inhibitors are active against integrase core domain-mediated disintegration, suggesting that fragment 50-212 is their actual target. These new styrylquinolines may provide lead compounds for the development of novel antiretroviral agents for AIDS therapeutics, based upon inhibition of HIV integrase. They might also be used in the elucidation of the mechanism of inhibition of this enzyme; e.g., they could serve as candidates for cocrystallization studies with HIV integrase.
- Published
- 1998
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17. Pegylated nanoparticles from a novel methoxypolyethylene glycol cyanoacrylate-hexadecyl cyanoacrylate amphiphilic copolymer.
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Peracchia MT, Vauthier C, Desmaële D, Gulik A, Dedieu JC, Demoy M, d'Angelo J, and Couvreur P
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- Animals, Cell Line, Drug Carriers, Mice, Microscopy, Electron, Particle Size, Spectrometry, X-Ray Emission, Surface Properties, Cyanoacrylates, Macrophages, Peritoneal drug effects, Polyethylene Glycols
- Abstract
Purpose: The aim of this work was to develop PEGylated poly(alkylcyanoacrylate) nanoparticles from a novel methoxypolyethyleneglycol cyanoacrylate-co-hexadecyl cyanoacrylate copolymer., Methods: PEGylated and non-PEGylated nanoparticles were formed by nanoprecipitation or by emulsion/solvent evaporation. Nanoparticles size, zeta potential and surface hydrophobicity were investigated. Surface chemical composition was determined by X-ray photoelectron spectroscopy. Nanoparticle morphology was investigated by transmission electron microscopy after freeze-fracture. Nanoparticles cytotoxicity was assayed in vitro, onto mouse peritoneal macrophages. Cell viability was determined through cell mitochondrial activity, by a tetrazolium-based colorimetric method (MTT test). Finally, the degradation of PEGylated and non-PEGylated poly(hexadecyl cyanoacrylate) nanoparticles was followed spectrophotometrically during incubation of nanoparticles in fetal calf serum., Results: Monodisperse nanoparticles with a mean diameter ranging between 100 and 200 nm were obtained using nanoprecipitation or emulsion/solvent evaporation as preparation procedures. A complete physico-chemical characterization, including surface chemical analysis, allowed to confirm the formation of PEG-coated nanoparticles. The PEGylation of the cyanoacrylate polymer showed reduced cytotoxicity towards mouse peritoneal macrophages. Furthermore, the presence of the PEG segment increased the degradability of the poly(hexadecyl cyanoacrylate) polymer in presence of calf serum., Conclusions: We succeeded to prepare PEGylated nanoparticles from a novel poly(methoxypolyethyleneglycol cyanoacrylate-co-hexadecyl cyanoacrylate) by two different techniques. Physico-chemical characterization showed the formation of a PEG coating layer. Low cytotoxicity and enhanced degradation were also shown.
- Published
- 1998
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18. A survey of persons who use integrated control devices.
- Author
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Angelo J and Trefler E
- Subjects
- Adolescent, Adult, Data Collection, Female, Humans, Male, Middle Aged, Disabled Persons, Patient Satisfaction, Self-Help Devices
- Abstract
Integrated devices allow users to operate multiple pieces of assistive technology items from a single input device. Through this single input device, users with severe physical limitations are able to operate several other devices such as a wheelchair, telephone, computer, and communication aid. Twenty-four integrated control users completed a telephone survey to ascertain consumer satisfaction with integrated controls. Eighteen were either satisfied or very satisfied with the evaluation for an integrated control, one was neither satisfied nor dissatisfied, two were very dissatisfied, and three did not respond to the question. Twenty were very satisfied or satisfied and four were either dissatisfied or very dissatisfied with the training they received. Twenty-two respondents indicated they were either very satisfied or satisfied with their integrated control device, one was neither satisfied nor dissatisfied, and one was very dissatisfied. In general, respondents were satisfied with their integrated control devices. Specifically, respondents were satisfied with the increase in independence and the ability to control other equipment such as television sets and computers. Simplicity, touch sensitivity, and visual/auditory feedback appeared to play important roles in satisfaction.
- Published
- 1998
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19. Identifying best practice in the occupational therapy assistive technology evaluation: an analysis of three focus groups.
- Author
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Angelo J, Buning ME, Schmeler M, and Doster S
- Subjects
- Humans, Outcome and Process Assessment, Health Care, Quality Assurance, Health Care, Benchmarking, Focus Groups, Occupational Therapy, Self-Help Devices
- Published
- 1997
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20. Comparison of anterior trunk supports for children with cerebral palsy.
- Author
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Trefler E and Angelo J
- Subjects
- Adolescent, Child, Child, Preschool, Humans, Cerebral Palsy rehabilitation, Orthotic Devices, Posture
- Abstract
The purpose of this study was to demonstrate outcome measures of one seating component--anterior trunk supports--when used by children with cerebral palsy during a functional activity. The functional activity was pressing a single switch to activate a computer software program. Seventeen children with a mean age of 9 years were included in the study. Subjects had mild to moderate spastic or athetoid cerebral palsy. Seven had a primary diagnosis of athetoid and 10 had a primary diagnosis of spastic cerebral palsy. All subjects needed supplemental seating to maintain an upright posture. The four trunk supports tested were an anterior chest panel, a 1-inch-wide single horizontal chest strap, an anterior shoulder support, and a tray with molded chest support. Data included prehits, response time, and the length of time the subject pressed the switch. A repeated analysis of variance test was used to analyze the data. Data for athetoid and spastic cerebral palsy subject groups were analyzed separately. No statistically significant differences were found between the four trunk supports. Therefore, the choice of trunk supports for this population should be based on client preferences, ease of removal for the caregiver, cost, and aesthetics.
- Published
- 1997
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21. A force feedback joystick and control algorithm for wheelchair obstacle avoidance.
- Author
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Brienza DM and Angelo J
- Subjects
- Equipment Design, Ergonomics, Feedback, Humans, Algorithms, Wheelchairs
- Abstract
Many powered wheelchair users have difficulty manoeuvring in confined spaces. Common tasks such as traversing through doorways, turning around in halls or travelling on a straight path are complicated by an inability to accurately and reliably control the wheelchair with a joystick or other common input device, or by a sensory impairment that prevents the user from receiving feedback from the environment. An active joystick with force feedback to indicate obstacles in the environment has been developed. Two force feedback schemes designed to assist a powered wheelchair user have been developed and implemented using the active joystick. The development of the joystick and associated control algorithms are described.
- Published
- 1996
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22. Technology competencies for occupational therapy practitioners.
- Author
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Hammel J and Angelo J
- Subjects
- Certification, Humans, Licensure, Outcome Assessment, Health Care, Quality Assurance, Health Care, Clinical Competence standards, Occupational Therapy education, Practice Guidelines as Topic, Self-Help Devices
- Abstract
A task force has created a recommended set of technology competencies for occupational therapy practitioners at three levels of practice: entry/basic, intermediate, and advanced. The competencies relate to assistive technology (AT) evaluation, intervention, and resource coordination and reflect minimum knowledge and skills for registered occupational therapists (O.T.R.'s) and certified occupational therapy assistants (C.O.T.A.'s). The competencies were reviewed by members of the American Occupational Therapy Association (AOTA), the COTA network and RESNA, and were coordinated with RESNA's ongoing AT quality assurance and certification efforts. They represent a base for the component of outcome management related to ensuring the quality and competency of AT service deliverers.
- Published
- 1996
- Full Text
- View/download PDF
23. Consumer participation in identifying research and development priorities for power wheelchair input devices and controllers.
- Author
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Brienza D, Angelo J, and Henry K
- Subjects
- Equipment Design, Focus Groups, Humans, Research, Community Participation, Robotics, Technology Transfer, Wheelchairs
- Abstract
A focus group comprised of persons who use power wheelchairs and professionals working in the field were asked to participate in a brainstorming session to determine priorities for the development and application of power mobility input devices and control concepts. The group consensus was that durability and reliability are the most important criteria. Essentially, the expectation is that a power wheelchair must work everyday in the way a person needs it and wants it. At the same time, there is a desire to enhance and advance the features of input devices and control systems. Many would say these changes constitute designing "smarter" power wheelchairs, such as systems that can independently detect obstacles and can provide users with more feedback. This paper presents the rationale behind forming this focus group and details of the results of a brainstorming session where ideas were generated and prioritized. The five most important issues as determined by the group are discussed in depth.
- Published
- 1995
- Full Text
- View/download PDF
24. [Autism and children with Fragile X syndrome].
- Author
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Blanc DS, D'Angelo J, and Lecavelier des Etangs N
- Subjects
- Autistic Disorder genetics, Autistic Disorder psychology, Child, Communication, Epidemiologic Methods, Fragile X Syndrome genetics, Fragile X Syndrome psychology, Humans, Interpersonal Relations, Phenotype, Research Design, Risk Factors, Autistic Disorder complications, Autistic Disorder epidemiology, Fragile X Syndrome complications, Fragile X Syndrome epidemiology
- Abstract
Many epidemiological studies have demonstrated the exceptionally high incidence of autism in children with the fragile X syndrome, and autism is often considered a "behavioral phenotype" of this syndrome. However, the discrepancies between the results of these studies disclosed strong effects of methodological flaws and demonstrated the need for gathering clinical data. Atypical "autistic-like" behaviors were then found to be common, early symptoms of the syndrome occurring against the background of early manifestations of mental retardation. These behaviors reflect these children's exquisite reactivity to change and contact with others. Avoidance of eye contact is the most significant feature. The appropriate diagnosis is not autism but phobia of social relationships. This highly specific vulnerability, which may be inherited, probably leads some of these patients to experience the fate of autistic children. It highlights the influence of environment on the clinical course and indirectly supports the role of early specialized care.
- Published
- 1993
25. An analysis of computer-related articles in occupational therapy periodicals.
- Author
-
Angelo J and Smith RO
- Subjects
- Humans, Database Management Systems, Disabled Persons, Microcomputers, Occupational Therapy instrumentation, Periodicals as Topic
- Abstract
The introduction of personal computers in the late 1970s and early 1980s has affected occupational therapy. Nine journals, three trade newspapers, and one series book published over an 11-year period by four English-speaking countries were catalogued for articles pertaining to computer use in occupational therapy. This investigation yielded 174 articles that were categorized by information type, application of computers covered, sophistication of technology, computer brand, and country of publication. Most articles provided general information, described clinical training applications, used an Apple computer, and were from an American publication. Few articles were reports of research. The percentage of computer-related articles has substantially increased in the observed 11-year period. These findings indicate increased computer use in occupational therapy.
- Published
- 1993
- Full Text
- View/download PDF
26. Returning To Work After Spinal Cord InjuryA Case Study.
- Author
-
Angelo J and Steinfeld E
- Published
- 1993
- Full Text
- View/download PDF
27. Technology.
- Author
-
Angelo J
- Published
- 1993
- Full Text
- View/download PDF
28. Using single-subject design in clinical decision making: the effects of tilt-in-space on head control for a child with cerebral palsy.
- Author
-
Angelo J
- Subjects
- Child, Decision Making, Female, Head, Humans, Research Design, Cerebral Palsy rehabilitation, Posture, Wheelchairs
- Abstract
Single-subject design methodology is a research technique useful in demonstrating the effects of treatment. The technique is described here using the effects of tilt-in-space on the ability to maintain head control. The subject is a 9-year-old child with cerebral palsy. The tilt-in-space angles used are 0 degrees , 15 degrees , and 30 degrees . Data are collected for the three different tilt angles in 10 sessions using an alternating rapid treatment design. Visual analysis of the results indicate that the subject displays greater head control when the wheelchair is placed at 15 degrees or 30 degrees tilt rather than at 0 degrees . This study shows how clinicians can complete single-subject studies to support recommendations for their clients and document the effects of their treatments.
- Published
- 1993
- Full Text
- View/download PDF
29. Comparison of three computer scanning modes as an interface method for persons with cerebral palsy.
- Author
-
Angelo J
- Subjects
- Adolescent, Adult, Athetosis rehabilitation, Humans, Muscle Spasticity rehabilitation, Cerebral Palsy rehabilitation, Communication Aids for Disabled, Microcomputers, Occupational Therapy instrumentation, Software, User-Computer Interface
- Abstract
Occupational therapists are becoming increasingly involved with interface assessments. This involvement is improving the ability of persons with physical disabilities to interact with computers, augmentative communication aids, and other devices. The ability to use these devices facilitates participation in activities that would otherwise be much more difficult to pursue, such as communication, education, work, and recreation. The purpose of the present study was to systematically compare three basic modes of scanning--automatic, inverse, and step--with the use of a single-subject experimental design. Six subjects--3 with spastic and 3 with athetoid cerebral palsy--from a local school volunteered for the study. Results indicated that the 3 subjects with spastic cerebral palsy had the greatest difficulty using the automatic scanning mode. The 3 subjects with athetoid cerebral palsy had the most difficulty using the step scanning mode. The results of this study suggest that clients should attempt each scanning mode and that their performance with each mode be compared to ensure the most appropriate recommendations.
- Published
- 1992
- Full Text
- View/download PDF
30. Peripheral neuropathy in cold agglutinin disease.
- Author
-
Thomas TD, Donofrio PD, and Angelo J
- Subjects
- Biopsy, Demyelinating Diseases diagnosis, Demyelinating Diseases etiology, Demyelinating Diseases pathology, Humans, Male, Microscopy, Electron, Middle Aged, Neural Conduction physiology, Peripheral Nervous System Diseases diagnosis, Peripheral Nervous System Diseases pathology, Sural Nerve pathology, Anemia, Hemolytic, Autoimmune complications, Peripheral Nervous System Diseases etiology
- Abstract
Cold agglutinin disease (CAD) characteristically presents as anemia and cold-induced rash. We report a man with purpura, anemia, cold agglutinins, and a sensory-autonomic polyneuropathy. Treatment with corticosteroids and plasma exchange resulted in resolution of the anemia and polyneuropathy. We propose that CAD may be associated with a reversible sensory-autonomic neuropathy in the absence of cryoglobulinemia. Although unsupported by pathologic findings, pathogenetic hypotheses for the neuropathy in CAD are similar to those proposed for cryoglobulinemic neuropathy.
- Published
- 1991
- Full Text
- View/download PDF
31. Comparing three head-pointing systems using a single subject design.
- Author
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Angelo J, Deterding C, and Weisman J
- Subjects
- Adult, Computer Peripherals, Equipment Design, Female, Humans, Male, Middle Aged, Software, Communication Aids for Disabled
- Abstract
The keyboard is the most commonly used input method for interfacing with computers. When using a keyboard is not possible, alternative computer input methods are needed. Three methods using head control are: Head Master by Prentke Romich, Free Wheel by Pointer Systems, and LROP by Words+. The purpose of this study was to compare these three methods for speed and accuracy using a single subject design for nine individuals with disabilities. Visual inspection of the data revealed that subjects obtained higher scores when using Head Master and LROP than Free Wheel. As a follow-up test, an analysis of variance test for repeated measures showed no difference between using Head Master and LROP but did show a significant difference between Head Master and Free Wheel, and LROP and Free Wheel.
- Published
- 1991
- Full Text
- View/download PDF
32. Selecting computer systems in augmentative communication.
- Author
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Angelo J and Smith RO
- Subjects
- Humans, Software, Communication Aids for Disabled, Computers, Self-Help Devices, Speech Disorders rehabilitation
- Published
- 1990
- Full Text
- View/download PDF
33. Isolation of citroylformic acid-gamma-lactone from a commerical batch of oxaloacetic acid: inhibition of apotyrosine aminotransferase conversion to holoenzyme by this substance.
- Author
-
Johnson RW, Grossman A, Boctor A, Kesner L, D'Angelo J, Frihart CR, and Nakanishi K
- Subjects
- 4-Butyrolactone analogs & derivatives, Animals, Citrates pharmacology, Enzyme Activation drug effects, Lactones isolation & purification, Lactones pharmacology, Liver enzymology, Oxaloacetates analysis, Oxaloacetates standards, Rats, Structure-Activity Relationship, Apoenzymes antagonists & inhibitors, Apoproteins antagonists & inhibitors, Citrates isolation & purification, Tyrosine Transaminase antagonists & inhibitors
- Published
- 1978
- Full Text
- View/download PDF
34. Treadmill exercise testing and silent myocardial ischemia.
- Author
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Froelicher VF, Callaham PR, Angelo J, and Lehmann KG
- Subjects
- Aged, Angina Pectoris epidemiology, Angioplasty, Balloon, Coronary, Coronary Artery Bypass, Coronary Disease mortality, Coronary Disease therapy, Diabetic Angiopathies epidemiology, Diagnosis, Computer-Assisted, Electrocardiography, Ambulatory, Exercise Test, Female, Humans, Male, Middle Aged, Myocardial Infarction epidemiology, Prognosis, Coronary Disease physiopathology
- Published
- 1989
35. Multiple meningiomas of the cervical spinal cord associated with Klippel-Feil malformation and atlantooccipital assimilation.
- Author
-
Holliday PO 3rd, Davis C Jr, and Angelo J
- Subjects
- Adult, Humans, Male, Neurofibromatosis 1 complications, Spinal Cord Neoplasms complications, Atlanto-Occipital Joint abnormalities, Klippel-Feil Syndrome complications, Meningeal Neoplasms complications, Meningioma complications, Neoplasms, Multiple Primary complications
- Abstract
A case of multiple meningiomas confined solely to the cervical spinal canal in association with multiple bony abnormalities of the cervical spine is presented. The relationship of this entity to neurofibromatosis, whether the central type or a form fruste, is explored. It is suggested that multiple meningiomas unassociated with other central or peripheral tumors may present a distinct clinical entity and may occur in an as yet uncharacterized familial pattern.
- Published
- 1984
- Full Text
- View/download PDF
36. Determination of lead in blood using electrothermal atomisation atomic absorption spectrometry with a L'vov platform and matrix modifier.
- Author
-
Miller DT, Paschal DC, Gunter EW, Stroud PE, and D'Angelo J
- Subjects
- Humans, Indicators and Reagents, Spectrophotometry, Atomic, Lead blood
- Published
- 1987
- Full Text
- View/download PDF
37. Protection from irreversible hypoxic injury by potassium cardioplegia and hypothermia: effects on contracture, morphology and O2-enzyme release.
- Author
-
Ganote CE, Angelo J, Safavi S, and Kaltenbach JP
- Subjects
- Animals, Coronary Circulation drug effects, Male, Myocardial Contraction drug effects, Myocardium enzymology, Myocardium pathology, Oxygen physiology, Perfusion, Rats, Rats, Inbred Strains, Temperature, Creatine Kinase metabolism, Heart drug effects, Heart Arrest, Induced, Hypothermia, Induced, Potassium pharmacology
- Published
- 1982
- Full Text
- View/download PDF
38. Eikenella corrodens infections in drug abusers.
- Author
-
Silpa M and D'Angelo J
- Subjects
- Adult, Bacteroides Infections drug therapy, Eikenella corrodens, Female, Humans, Male, Middle Aged, Bacteroides Infections etiology, Substance-Related Disorders complications
- Published
- 1980
- Full Text
- View/download PDF
39. Syringobulbia-myelia with obstructive sleep apnea.
- Author
-
Haponik EF, Givens D, and Angelo J
- Subjects
- Adult, Female, Humans, Medulla Oblongata abnormalities, Sleep Apnea Syndromes etiology, Syringomyelia complications
- Abstract
Central nervous system disorders may cause obstructive sleep apnea, but this sleep-related breathing disorder is rarely associated with a structural abnormality of the medulla. We present a patient with obstructive apnea resulting from autopsy-proven syringobulbia-myelia.
- Published
- 1983
- Full Text
- View/download PDF
40. Neurilemoma and the urologist.
- Author
-
Johenning PW and D'Angelo J
- Subjects
- Female, Humans, Male, Middle Aged, Muscles pathology, Neurilemmoma diagnostic imaging, Neurilemmoma pathology, Radiography, Retroperitoneal Neoplasms diagnostic imaging, Retroperitoneal Neoplasms pathology, Schwann Cells, Urogenital Neoplasms diagnostic imaging, Urogenital Neoplasms pathology, Neurilemmoma diagnosis, Retroperitoneal Neoplasms diagnosis, Urogenital Neoplasms diagnosis
- Published
- 1973
- Full Text
- View/download PDF
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