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92 results on '"Patane, M. A."'

1. First Ex-Vivo Validation of a Radioguided Surgery Technique with beta- Radiation

Author

Camillocci, E. Solfaroli, Schiariti, M., Bocci, V., Carollo, A., Chiodi, G., Colandrea, M., Collamati, F., Cremonesi, M., Donnarumma, R., Ferrari, M. E., Ferroli, P., Ghielmetti, F., Grana, C. M., Marafini, M., Morganti, S., Terracciano, C. Mancini, Patanè, M., Pedroli, G., Pollo, B., Recchia, L., Russomando, A., Toppi, M., Traini, G., and Faccini, R.

Subjects
Physics - Instrumentation and Detectors, Physics - Medical Physics
Abstract

Purpose: A radio-guided surgery technique with beta- -emitting radio-tracers was suggested to overcome the effect of the large penetration of gamma radiation. The feasibility studies in the case of brain tumors and abdominal neuro-endocrine tumors were based on simulations starting from PET images with several underlying assumptions. This paper reports, as proof-of-principle of this technique, an ex-vivo test on a meningioma patient. This test allowed to validate the whole chain, from the evaluation of the SUV of the tumor, to the assumptions on the bio-distribution and the signal detection. Methods: A patient affected by meningioma was administered 300 MBq of 90Y-DOTATOC. Several samples extracted from the meningioma and the nearby Dura Mater were analyzed with a beta- probe designed specifically for this radio-guided surgery technique. The observed signals were compared both with the evaluation from the histology and with the Monte Carlo simulation. Results: we obtained a large signal on the bulk tumor (105 cps) and a significant signal on residuals of $\sim$0.2 ml (28 cps). We also show that simulations predict correctly the observed yields and this allows us to estimate that the healthy tissues would return negligible signals (~1 cps). This test also demonstrated that the exposure of the medical staff is negligible and that among the biological wastes only urine has a significant activity. Conclusions: This proof-of-principle test on a patient assessed that the technique is feasible with negligible background to medical personnel and confirmed that the expectations obtained with Monte Carlo simulations starting from diagnostic PET images are correct., Comment: 17 pages, 4 Figs, Accepted by Physica Medica

Published
2016
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3. Radio-Guided Surgery with β − Radiation: Tests on Ex-Vivo Specimens

Author

Mancini-Terracciano, C., Bocci, V., Colandrea, M., Collamati, F., Cremonesi, M., Faccini, R., Ferrari, M. E., Ferroli, P., Ghielmetti, F., Grana, C. M., Marafini, M., Morganti, S., Papi, S., Patané, M., Pedroli, G., Pollo, B., Russomando, A., Schiariti, M., Traini, G., Solfaroli Camillocci, E., Magjarevic, Ratko, Editor-in-Chief, Ładyżyński, Piotr, Series Editor, Ibrahim, Fatimah, Series Editor, Lacković, Igor, Series Editor, Rock, Emilio Sacristan, Series Editor, Lhotska, Lenka, editor, Sukupova, Lucie, editor, and Ibbott, Geoffrey S., editor

Published
2019
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9. Symptoms of anxiety and depression during the COVID-19 pandemic in six European countries and Australia - differences by prior mental disorders and migration status

Author

Acartürk, Zeynep Ceren (ORCID 0000-0001-7093-1554 & YÖK ID 39271), Gemes, K.; Bergstrom, J.; Papola, D.; Barbui, C.; Lam, A.I.F.; Hall, B.J.; Seedat, S.; Morina, N.; Quero, S.; Campos, D.; Pinucci, I.; Tarsitani, L.; Deguen, S.; van der Waerden, J.; Patane, M.; Sijbrandij, M.; Burchert, S.; Bryant, R.A.; Mittendorfer-Rutz, E., College of Social Sciences and Humanities, Department of Psychology, Acartürk, Zeynep Ceren (ORCID 0000-0001-7093-1554 & YÖK ID 39271), Gemes, K.; Bergstrom, J.; Papola, D.; Barbui, C.; Lam, A.I.F.; Hall, B.J.; Seedat, S.; Morina, N.; Quero, S.; Campos, D.; Pinucci, I.; Tarsitani, L.; Deguen, S.; van der Waerden, J.; Patane, M.; Sijbrandij, M.; Burchert, S.; Bryant, R.A.; Mittendorfer-Rutz, E., College of Social Sciences and Humanities, and Department of Psychology

Abstract

Background: little is known about changes of mental health during the COVID-19 pandemic in potentially disadvantaged groups. We investigated changes in anxiety and depression symptoms during the first year of the pandemic in six European countries and Australia by prior mental disorders and migration status. Methods: overall, 4674 adults answered a web-based survey in May-June 2020 and were followed by three repeated surveys up to February 2021. Information on psychosocial, financial and demographic, living conditions, prior mental disorders, depression and anxiety symptoms during the pandemic and migration status was collected. Weighted general estimation equations modelling was used to investigate the association between prior mental disorders, migration status, and symptoms over time. Results: most participants were <40 years old (48%), women (78%) and highly educated (62%). The baseline prevalence of depressive and anxiety symptoms ranged between 19%-45% and 13%-35%, respectively. In most countries, prevalence rates remained unchanged throughout the pandemic and were higher among people with prior mental disorders than without even after adjustment for several factors. We observed interactions between previous mental disorders and symptoms of anxiety or depression over time in two countries. No difference by migration status was noted. Limitations: convenience sampling limits generalizability. Self-assessed symptoms of depression and anxiety might involve some misclassification. Conclusions: depression and anxiety symptoms were worse among individuals with prior mental disorders than without, but there was no clear trend of worsening mental health in the observed groups during the observed period., European Union (EU); Horizon 2020; Research and Innovation Programme Societal Challenges

Published
2022

11. Disease activity assessment of rheumatic diseases during pregnancy: a comprehensive review of indices used in clinical studies

Author

Andreoli, L, Gerardi, M, Fernandes, M, Bortoluzzi, A, Bellando-Randone, S, Brucato, A, Caporali, R, Chighizola, C, Chimenti, M, Conigliaro, P, Cutolo, M, Cutro, M, D'Angelo, S, Doria, A, Elefante, E, Fredi, M, Galeazzi, M, Gerosa, M, Govoni, M, Iuliano, A, Larosa, M, Lazzaroni, M, Matucci-Cerinic, M, Meroni, M, Meroni, P, Mosca, M, Patane, M, Pazzola, G, Pendolino, M, Perricone, R, Ramoni, V, Salvarani, C, Sebastiani, G, Selmi, C, Spinelli, F, Valesini, G, Scire, C, Tincani, A, Andreoli L., Gerardi M. C., Fernandes M., Bortoluzzi A., Bellando-Randone S., Brucato A., Caporali R., Chighizola C. B., Chimenti M. S., Conigliaro P., Cutolo M., Cutro M. S., D'Angelo S., Doria A., Elefante E., Fredi M., Galeazzi M., Gerosa M., Govoni M., Iuliano A., Larosa M., Lazzaroni M. G., Matucci-Cerinic M., Meroni M., Meroni P. L., Mosca M., Patane M., Pazzola G., Pendolino M., Perricone R., Ramoni V., Salvarani C., Sebastiani G. D., Selmi C., Spinelli F. R., Valesini G., Scire C. A., Tincani A., Andreoli, L, Gerardi, M, Fernandes, M, Bortoluzzi, A, Bellando-Randone, S, Brucato, A, Caporali, R, Chighizola, C, Chimenti, M, Conigliaro, P, Cutolo, M, Cutro, M, D'Angelo, S, Doria, A, Elefante, E, Fredi, M, Galeazzi, M, Gerosa, M, Govoni, M, Iuliano, A, Larosa, M, Lazzaroni, M, Matucci-Cerinic, M, Meroni, M, Meroni, P, Mosca, M, Patane, M, Pazzola, G, Pendolino, M, Perricone, R, Ramoni, V, Salvarani, C, Sebastiani, G, Selmi, C, Spinelli, F, Valesini, G, Scire, C, Tincani, A, Andreoli L., Gerardi M. C., Fernandes M., Bortoluzzi A., Bellando-Randone S., Brucato A., Caporali R., Chighizola C. B., Chimenti M. S., Conigliaro P., Cutolo M., Cutro M. S., D'Angelo S., Doria A., Elefante E., Fredi M., Galeazzi M., Gerosa M., Govoni M., Iuliano A., Larosa M., Lazzaroni M. G., Matucci-Cerinic M., Meroni M., Meroni P. L., Mosca M., Patane M., Pazzola G., Pendolino M., Perricone R., Ramoni V., Salvarani C., Sebastiani G. D., Selmi C., Spinelli F. R., Valesini G., Scire C. A., and Tincani A.

Abstract

Pregnancy requires a special management in women with inflammatory rheumatic diseases (RDs), with the aim of controlling maternal disease activity and avoiding fetal complications. Despite the heterogeneous course of RDs during pregnancy, their impact on pregnancy largely relates to the extent of active inflammation at the time of conception. Therefore, accurate evaluation of disease activity is crucial for the best management of pregnant patients. Nevertheless, there are limitations in using conventional measures of disease activity in pregnancy, as some items included in these instruments can be biased by symptoms or by physiological changes related to pregnancy and the pregnancy itself may influence laboratory parameters used to assess disease activity. This article aims to summarize the current literature about the available instruments to measure disease activity during pregnancy in RDs. Systemic lupus erythematosus is the only disease with instruments that have been modified to account for several adaptations which might interfere with the attribution of signs or symptoms to disease activity during pregnancy. No modified-pregnancy indices exist for women affected by other RDs, but standard indices have been applied to pregnant patients. The current body of knowledge shows that the physiologic changes that occur during pregnancy need to be either adapted from existing instruments or developed to improve the management of pregnant women with RDs. Standardized instruments to assess disease activity during pregnancy would be helpful not only for clinical practice but also for research purposes.

Published
2019

15. Mutations targeting the coagulation pathway are enriched in brain metastases

Author

Richichi, C, Fornasari, L, Melloni, GEM, Brescia, P, Patane, M, Del Bene, M, Mustafa, Dana, Kros, J.M., Pollo, B, Pruneri, G, Sciandivasci, A, Munzone, E, DiMeco, F, Pelicci, PG, Riva, L, Pelicci, G, Richichi, C, Fornasari, L, Melloni, GEM, Brescia, P, Patane, M, Del Bene, M, Mustafa, Dana, Kros, J.M., Pollo, B, Pruneri, G, Sciandivasci, A, Munzone, E, DiMeco, F, Pelicci, PG, Riva, L, and Pelicci, G

Published
2017

16. Novel integrated 3D multidetector computed tomography and fluoroscopy fusion for left atrial appendage occlusion procedures

Author

Roy, A.K., primary, Horvilleur, J., additional, Cormier, B., additional, Cazalas, M., additional, Fernandez, L., additional, Patane, M., additional, Neylon, A., additional, Spaziano, M., additional, Sawaya, F.J., additional, Arai, T., additional, Bouvier, E., additional, Hovasse, T., additional, Lefèvre, T., additional, Chevalier, B., additional, and Garot, P., additional

Published
2017
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17. Acute Kidney Injury With the RenalGuard System in Patients Undergoing Transcatheter Aortic Valve Replacement: The PROTECT-TAVI Trial (PROphylactic effecT of furosEmide-induCed diuresis with matched isotonic intravenous hydraTion in Transcatheter Aortic Valve Implantation)

Author

Barbanti, M, Gulino, S, Capranzano, P, Imme, S, Sgroi, C, Tamburino, Corrado, Ohno, Y, Attizzani, Gf, Patane, M, Sicuso, R, Pilato, G, DI LANDRO, A, Todaro, D, DI SIMONE, E, Picci, A, Giannetto, G, Costa, G, Deste, W, Grasso, C, Capodanno, DAVIDE FRANCESCO MARIA, and Tamburino, C.

Published
2015

18. The AGILE Mission

Author

Tavani M, Barbiellini G, Argan A, Boffelli F, Bulgarelli A, Caraveo P, Cattaneo PW, Chen AW, Cocco V, Costa E, Del Monte E, De Paris G, Di Cocco G, Di Persio G, Donnarumma I, Evangelista Y, Feroci M, Ferrari A, Fiorini M, Fornari F, Fuschino F, Froysland T, Frutti M, Galli M, Gianotti F, Giuliani A, Labanti C, Lapshov I, Lazzarotto F, Liello F, Lipari P, Longo F, Mattaini E, Marisaldi M, Mastropietro M, Mauri A, Mauri F, Mereghetti S, Morelli E, Morselli A, Pacciani L, Pellizzoni A, Perotti F, Piano G, Picozza P, Pontoni C, Porrovecchio G, Prest M, Pucella G, Rapisarda M, Rappoldi A, Rossi E, Rubini A, Soffitta P, Traci A, Trifoglio M, Trois A, Vallazza E, Vercellone S, Vittorini V, Zambra A, Zanello D, Pittori C, Preger B, Santolamazza P, Verrecchia F, Giommi P, Colafrancesco S, Antonelli A, Cutini S, Gasparrini D, Stellato S, Fanari G, Primavera R, Tamburelli F, Viola F, Guarrera G, Salotti L, D'Amico F, Marchetti E, Crisconio M, Sabatini P, Annoni G, Alia S, Longoni A, Sanquerin R, Battilana M, Concari P, Dessimone E, Grossi R, Parise A, Monzani F, Artina E, Pavesi R, Marseguerra G, Nicolini L, Scandelli L, Soli L, Vettorello V, Zardetto E, Bonati A, Maltecca L, D'Alba E, Patane M, Babini G, Onorati F, Acquaroli L, Angelucci M, Morelli B, Agostara C, Cerone M, Michetti A, Tempesta P, D'Eramo S, Rocca F, Giannini F, Borghi G, Garavelli B, Conte M, Balasini M, Ferrario I, Vanotti M, Collavo E, Giacomazzo M., D'AMMANDO, FILIPPO, M., Tavani, G., Barbiellini, A., Argan, F., Boffelli, A., Bulgarelli, P., Caraveo, P. W., Cattaneo, A. W., Chen, V., Cocco, E., Costa, F., D'Ammando, E. D., Monte, G. D., Pari, G. D., Cocco, G. D., Persio, I., Donnarumma, Y., Evangelista, M., Feroci, A., Ferrari, M., Fiorini, F., Fornari, F., Fuschino, T., Froysland, M., Frutti, M., Galli, F., Gianotti, A., Giuliani, C., Labanti, I., Lapshov, F., Lazzarotto, F., Liello, P., Lipari, Longo, Francesco, E., Mattaini, M., Marisaldi, M., Mastropietro, A., Mauri, F., Mauri, S., Mereghetti, E., Morelli, A., Morselli, L., Pacciani, A., Pellizzoni, F., Perotti, G., Piano, P., Picozza, C., Pontoni, G., Porrovecchio, M., Prest, G., Pucella, M., Rapisarda, A., Rappoldi, E., Rossi, A., Rubini, P., Soffitta, A., Traci, M., Trifoglio, A., Troi, E., Vallazza, S., Vercellone, V., Vittorini, A., Zambra, D., Zanello, C., Pittori, B., Preger, P., Santolamazza, F., Verrecchia, P., Giommi, S., Colafrancesco, A., Antonelli, S., Cutini, D., Gasparrini, S., Stellato, G., Fanari, R., Primavera, F., Tamburelli, F., Viola, G., Guarrera, L., Salotti, F., D'Amico, E., Marchetti, M., Crisconio, P., Sabatini, G., Annoni, S., Alia, A., Longoni, R., Sanquerin, M., Battilana, P., Concari, E., Dessimone, R., Grossi, A., Parise, F., Monzani, E., Artina, R., Pavesi, G., Marseguerra, L., Nicolini, L., Scandelli, L., Soli, V., Vettorello, E., Zardetto, A., Bonati, L., Maltecca, E., D'Alba, M., Patane, G., Babini, F., Onorati, L., Acquaroli, M., Angelucci, B., Morelli, C., Agostara, M., Cerone, A., Michetti, P., Tempesta, S., D'Eramo, F., Rocca, F., Giannini, G., Borghi, B., Garavelli, M., Conte, M., Balasini, I., Ferrario, M., Vanotti, E., Collavo, M., Giacomazzo, Tavani M, Barbiellini G, Argan A, Boffelli F, Bulgarelli A, Caraveo P, Cattaneo PW, Chen AW, Cocco V, Costa E, DAmmando F, Del Monte E, De Paris G, Di Cocco G, Di Persio G, Donnarumma I, Evangelista Y, Feroci M, Ferrari A, Fiorini M, Fornari F, Fuschino F, Froysland T, Frutti M, Galli M, Gianotti F, Giuliani A, Labanti C, Lapshov I, Lazzarotto F, Liello F, Lipari P, Longo F, Mattaini E, Marisaldi M, Mastropietro M, Mauri A, Mauri F, Mereghetti S, Morelli E, Morselli A, Pacciani L, Pellizzoni A, Perotti F, Piano G, Picozza P, Pontoni C, Porrovecchio G, Prest M, Pucella G, Rapisarda M, Rappoldi A, Rossi E, Rubini A, Soffitta P, Traci A, Trifoglio M, Trois A, Vallazza E, Vercellone S, Vittorini V, Zambra A, Zanello D, Pittori C, Preger B, Santolamazza P, Verrecchia F, Giommi P, Colafrancesco S, Antonelli A, Cutini S, Gasparrini D, Stellato S, Fanari G, Primavera R, Tamburelli F, Viola F, Guarrera G, Salotti L, D'Amico F, Marchetti E, Crisconio M, Sabatini P, Annoni G, Alia S, Longoni A, Sanquerin R, Battilana M, Concari P, Dessimone E, Grossi R, Parise A, Monzani F, Artina E, Pavesi R, Marseguerra G, Nicolini L, Scandelli L, Soli L, Vettorello V, Zardetto E, Bonati A, Maltecca L, D'Alba E, Patane M, Babini G, Onorati F, Acquaroli L, Angelucci M, Morelli B, Agostara C, Cerone M, Michetti A, Tempesta P, D'Eramo S, Rocca F, Giannini F, Borghi G, Garavelli B, Conte M, Balasini M, Ferrario I, Vanotti M, Collavo E, and Giacomazzo M

Subjects
Agile, Active galactic nucleus, gamma and X ray detection, Astrophysics::High Energy Astrophysical Phenomena, media_common.quotation_subject, satellite, FOS: Physical sciences, Astrophysics, High Energy Gamma-ray Astronomy, Pulsar, astro-ph, Angular resolution, media_common, Physics, Calorimeter (particle physics), Astrophysics (astro-ph), Detector, AGILE satellite, Detectors, Astronomy and Astrophysics, Universe, Supernova, Space and Planetary Science, Orbit (dynamics), instrumentation: detectors – techniques: high angular resolution – techniques: image processing – gamma rays: observations – X-rays: general
Abstract

AGILE is an Italian Space Agency mission dedicated to the observation of the gamma-ray Universe. The AGILE very innovative instrumentation combines for the first time a gamma-ray imager (sensitive in the energy range 30 MeV - 50 GeV), a hard X-ray imager (sensitive in the range 18-60 keV) together with a Calorimeter (sensitive in the range 300 keV - 100 MeV) and an anticoincidence system. AGILE was successfully launched on April 23, 2007 from the Indian base of Sriharikota and was inserted in an equatorial orbit with a very low particle background. AGILE provides crucial data for the study of Active Galactic Nuclei, Gamma-Ray Bursts, pulsars, unidentified gamma-ray sources, Galactic compact objects, supernova remnants, TeV sources, and fundamental physics by microsecond timing. An optimal angular resolution (reaching 0.1-0.2 degrees in gamma-rays, 1-2 arcminutes in hard X-rays) and very large fields of view (2.5 sr and 1 sr, respectively) are obtained by the use of Silicon detectors integrated in a very compact instrument. The paper describes the AGILE Mission and its space and ground segments., 20 pages, 26 figures. submitted to Astron. & Astrophys

Published
2009

28. Genetic and molecular signature of glioblastoma stem-like cells

Author

Patane', M, PATANE', MONICA, Patane', M, and PATANE', MONICA

Abstract

In the past years it was made a very huge effort to understand the genetic and molecular signatures of glioblastoma in order to improve targeted molecular therapy: but to date several things remain still unclear and new markers or new relationships have to been disclosed. Our aim is, therefore, to better clarify genetic signatures and pathways’ cross-talks in our glioblastoma-stem like cells model: actually we believe that these cells represent a real reservoir for the tumor of cells, which are able alone to maintain tumor growth, to give raise to a relapse and to determine radio- and chemo-resistance. First we presented a paper published in collaboration with our laboratory in 2012: in this study we found that the expression of MET oncogene was associated with a mesenchymal signature in our glioblastoma stem-like cells model and this expression is mutually exclusive with EGFR amplification; these cells also displayed different growth requirements in vitro and generated tumors with distinctive features in vivo; this suggested that MET could be a new target for therapy of a specific subset of GBMs (De Bacco et al 2012). Then we tried to better understand the possible cross-talk between EGFR and NF-kB signalling through a specific genetic signature disclosed in a precedent paper (Bredel et al 2011): a heterozygous deletion of NFKBIA gene, mutually exclusive with EGFR amplification. Surprisingly we found that this signature is a rare event in the primary tumor, but it is very frequent in our glioblastoma stem-like cells model in vitro and has also clear functional consequences. Our results raise the possibility that this deletion may be amplified in vitro, favored by the presence of EGF, mostly in that lines in which EGFR pathway is predominant; furthermore in these cells seems to be favored the constitutive active mutant of EGFR gene, EGFRvIII, probably in order to preserve EGFR-NF-kB axis. All these data suggest that our model is a much better system than serum-depen

Published
2013

29. OMICS AND PROGNSTIC MARKERS

Author

Adachi, K., primary, Sasaki, H., additional, Nagahisa, S., additional, Yoshida, K., additional, Hattori, N., additional, Nishiyama, Y., additional, Kawase, T., additional, Hasegawa, M., additional, Abe, M., additional, Hirose, Y., additional, Alentorn, A., additional, Marie, Y., additional, Poggioli, S., additional, Alshehhi, H., additional, Boisselier, B., additional, Carpentier, C., additional, Mokhtari, K., additional, Capelle, L., additional, Figarella-Branger, D., additional, Hoang-Xuan, K., additional, Sanson, M., additional, Delattre, J.-Y., additional, Idbaih, A., additional, Yust-Katz, S., additional, Anderson, M., additional, Olar, A., additional, Eterovic, A., additional, Ezzeddine, N., additional, Chen, K., additional, Zhao, H., additional, Fuller, G., additional, Aldape, K., additional, de Groot, J., additional, Andor, N., additional, Harness, J., additional, Lopez, S. G., additional, Fung, T. L., additional, Mewes, H. W., additional, Petritsch, C., additional, Arivazhagan, A., additional, Somasundaram, K., additional, Thennarasu, K., additional, Pandey, P., additional, Anandh, B., additional, Santosh, V., additional, Chandramouli, B., additional, Hegde, A., additional, Kondaiah, P., additional, Rao, M., additional, Bell, R., additional, Kang, R., additional, Hong, C., additional, Song, J., additional, Costello, J., additional, Nagarajan, R., additional, Zhang, B., additional, Diaz, A., additional, Wang, T., additional, Bie, L., additional, Li, Y., additional, Liu, H., additional, Luyo, W. F. C., additional, Carnero, M. H., additional, Iruegas, M. E. P., additional, Morell, A. R., additional, Figueiras, M. C., additional, Lopez, R. L., additional, Valverde, C. F., additional, Chan, A. K.-Y., additional, Pang, J. C.-S., additional, Chung, N. Y.-F., additional, Li, K. K.-W., additional, Poon, W. S., additional, Chan, D. T.-M., additional, Wang, Y., additional, Ng, H.-a. K., additional, Chaumeil, M., additional, Larson, P., additional, Yoshihara, H., additional, Vigneron, D., additional, Nelson, S., additional, Pieper, R., additional, Phillips, J., additional, Ronen, S., additional, Clark, V., additional, Omay, Z. E., additional, Serin, A., additional, Gunel, J., additional, Omay, B., additional, Grady, C., additional, Youngblood, M., additional, Bilguvar, K., additional, Baehring, J., additional, Piepmeier, J., additional, Gutin, P., additional, Vortmeyer, A., additional, Brennan, C., additional, Pamir, M. N., additional, Kilic, T., additional, Krischek, B., additional, Simon, M., additional, Yasuno, K., additional, Gunel, M., additional, Cohen, A. L., additional, Sato, M., additional, Aldape, K. D., additional, Mason, C., additional, Diefes, K., additional, Heathcock, L., additional, Abegglen, L., additional, Shrieve, D., additional, Couldwell, W., additional, Schiffman, J. D., additional, Colman, H., additional, D'Alessandris, Q. G., additional, Cenci, T., additional, Martini, M., additional, Ricci-Vitiani, L., additional, De Maria, R., additional, Larocca, L. M., additional, Pallini, R., additional, Theeler, B., additional, Lang, F., additional, Rao, G., additional, Gilbert, M., additional, Sulman, E., additional, Luthra, R., additional, Eterovic, K., additional, Routbort, M., additional, Verhaak, R., additional, Mills, G., additional, Mendelsohn, J., additional, Meric-Bernstam, F., additional, Yung, A., additional, MacArthur, K., additional, Hahn, S., additional, Kao, G., additional, Lustig, R., additional, Alonso-Basanta, M., additional, Chandrasekaran, S., additional, Wileyto, E. P., additional, Reyes, E., additional, Dorsey, J., additional, Fujii, K., additional, Kurozumi, K., additional, Ichikawa, T., additional, Onishi, M., additional, Ishida, J., additional, Shimazu, Y., additional, Kaur, B., additional, Chiocca, E. A., additional, Date, I., additional, Geisenberger, C., additional, Mock, A., additional, Warta, R., additional, Schwager, C., additional, Hartmann, C., additional, von Deimling, A., additional, Abdollahi, A., additional, Herold-Mende, C., additional, Gevaert, O., additional, Achrol, A., additional, Gholamin, S., additional, Mitra, S., additional, Westbroek, E., additional, Loya, J., additional, Mitchell, L., additional, Chang, S., additional, Steinberg, G., additional, Plevritis, S., additional, Cheshier, S., additional, Xu, J., additional, Napel, S., additional, Zaharchuk, G., additional, Harsh, G., additional, Gutman, D., additional, Holder, C., additional, Colen, R., additional, Dunn, W., additional, Jain, R., additional, Cooper, L., additional, Hwang, S., additional, Flanders, A., additional, Brat, D., additional, Hayes, J., additional, Droop, A., additional, Thygesen, H., additional, Boissinot, M., additional, Westhead, D., additional, Short, S., additional, Lawler, S., additional, Bady, P., additional, Kurscheid, S., additional, Delorenzi, M., additional, Hegi, M. E., additional, Crosby, C., additional, Faulkner, C., additional, Smye-Rumsby, T., additional, Kurian, K., additional, Williams, M., additional, Hopkins, K., additional, Palmer, A., additional, Williams, H., additional, Wragg, C., additional, Haynes, H. R., additional, Kurian, K. M., additional, White, P., additional, Oka, T., additional, Jalbert, L., additional, Elkhaled, A., additional, Jensen, R., additional, Salzman, K., additional, Schabel, M., additional, Gillespie, D., additional, Mumert, M., additional, Johnson, B., additional, Mazor, T., additional, Barnes, M., additional, Yamamoto, S., additional, Ueda, H., additional, Tatsuno, K., additional, Aihara, K., additional, Bollen, A., additional, Hirst, M., additional, Marra, M., additional, Mukasa, A., additional, Saito, N., additional, Aburatani, H., additional, Berger, M., additional, Taylor, B., additional, Popov, S., additional, Mackay, A., additional, Ingram, W., additional, Burford, A., additional, Jury, A., additional, Vinci, M., additional, Jones, C., additional, Jones, D. T. W., additional, Hovestadt, V., additional, Picelli, S., additional, Wang, W., additional, Northcott, P. 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P., additional, and Koul, D., additional

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31. Poster Session 1: Thursday 8 December 2011, 08:30-12:30 * Location: Poster Area

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Vijayan, S., primary, Khanji, M., additional, Ionescu, A., additional, Vijayan, S., additional, Podoleanu, C., additional, Frigy, A., additional, Ugri, A., additional, Varga, A., additional, Podoleanu, D., additional, Incze, A., additional, Carasca, E., additional, Dobreanu, D., additional, Mjolstad, O., additional, Dalen, H., additional, Graven, T., additional, Kleinau, J., additional, Hagen, B., additional, Fu, H., additional, Liu, T., additional, Li, J., additional, Liu, C., additional, Zhou, C., additional, Li, G., additional, Bordese, R., additional, Capriolo, M., additional, Brero, D., additional, Salvetti, I., additional, Cannillo, M., additional, Antolini, M., additional, Grosso Marra, W., additional, Frea, S., additional, Morello, M., additional, Gaita, F., additional, Maffessanti, F., additional, Caiani, E., additional, Muraru, D., additional, Tuveri, F., additional, Dal Bianco, L., additional, Badano, L., additional, Majid, A., additional, Soesanto, A., additional, Ario Suryo Kuncoro, B., additional, Sukmawan, R., additional, Ganesja, M. H., additional, Benedek, T., additional, Chitu, M., additional, Beata, J., additional, Suciu, Z., additional, Kovacs, I., additional, Bucur, O., additional, Benedek, I., additional, Hrynkiewicz-Szymanska, A., additional, Szymanski, F., additional, Karpinski, G., additional, Filipiak, K., additional, Radunovic, Z., additional, Lande Wekre, L., additional, Steine, K., additional, Bech-Hanssen, O., additional, Rundqvist, B., additional, Lindgren, F., additional, Selimovic, N., additional, Jedrzychowska-Baraniak, J., additional, Jozwa, R., additional, Larysz, B., additional, Kasprzak, J., additional, Ripp, T., additional, Mordovin, V., additional, Ripp, E., additional, Ciobanu, A., additional, Dulgheru, R., additional, Dragoi, R., additional, Magda, S., additional, Florescu, M., additional, Mihaila, S., additional, Rimbas, R., additional, Cinteza, M., additional, Vinereanu, D., additional, Benavides-Vallve, C., additional, Pelacho, B., additional, Iglesias, O., additional, Castano, S., additional, Munoz-Barrutia, A., additional, Prosper, F., additional, Ortiz De Solorzano, C., additional, Manouras, A., additional, Sahlen, A., additional, Winter, R., additional, Vardas, P., additional, Brodin, L., additional, Sarvari, S. 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W., additional, Brandon Bravo Bruinsma, G., additional, Van 'T Hof, A., additional, Spanjersberg, S., additional, Nierich, A., additional, Bombardini, T., additional, Gherardi, S., additional, Picano, E., additional, Ciarka, A., additional, Herbots, L., additional, Eroglu, E., additional, Van Cleemput, J., additional, Droogne, W., additional, Jasityte, R., additional, Meyns, B., additional, D'hooge, J., additional, Vanhaecke, J., additional, Al Barjas, M., additional, Iskreva, R., additional, Morris, R., additional, Davar, J., additional, Zhao, Y., additional, Holmgren, A., additional, Morner, S., additional, Stepanovic, J., additional, Beleslin, B., additional, Nedeljkovic, M., additional, Mazic, S., additional, Stojanov, V., additional, Piatkowski, R., additional, Kochanowski, J., additional, Scislo, P., additional, Grabowski, M., additional, Marchel, M., additional, Roik, M., additional, Kosior, D., additional, Opolski, G., additional, Tomaszewski, A., additional, Kutarski, A., additional, Tomaszewski, M., additional, Eibel, S., additional, Hasheminejad, E., additional, Mukherjee, C., additional, Tschernich, H., additional, Ender, J., additional, Delithanasis, I., additional, Celutkiene, J., additional, Kenny, C., additional, Monaghan, M., additional, Van Den Oord, S., additional, Ten Kate, G., additional, Akkus, Z., additional, Renaud, G., additional, Sijbrands, E., additional, Ten Cate, F., additional, De Jong, N., additional, Bosch, J., additional, Van Der Steen, A., additional, Schinkel, A., additional, Lisowska, A., additional, Knapp, M., additional, Tycinska, A., additional, Sawicki, R., additional, Kralisz, P., additional, Sobkowicz, B., additional, Chang, S.-A., additional, Lee, S.-C., additional, Kim, E.-Y., additional, Hahm, S.-H., additional, Ahn, G.-T., additional, Sohn, M.-K., additional, Park, S.-J., additional, Choi, J.-O., additional, Park, S.-W., additional, Oh, J.-K., additional, Gursoy, M. O., additional, Gokdeniz, T., additional, Astarcioglu, M., additional, Bayram, Z., additional, Cakal, B., additional, Karakoyun, S., additional, Kalcik, M., additional, Kahveci, G., additional, Yildiz, M., additional, Ozkan, M., additional, Skidan, V., additional, Borowski, A., additional, Park, M., additional, Thomas, J., additional, Ranjbar, S., additional, Hassantash, S., additional, Karvandi, M., additional, Foroughi, M., additional, Davidsen, E. S., additional, Cramariuc, D., additional, Bleie, O., additional, Gerdts, E., additional, Matre, K., additional, Cusma' Piccione, M., additional, Bagnato, G., additional, Mohammed, M., additional, Piluso, S., additional, Oreto, L., additional, Bitter, T., additional, Carvalho, S., additional, Canada, M., additional, Santisteban Sanchez De Puerta, M., additional, Mesa Rubio, M. D., additional, Ruiz Ortiz, M., additional, Delgado Ortega, M., additional, Pena Pena, M. L., additional, Puentes Chiachio, M., additional, Suarez De Lezo Cruz-Conde, J., additional, Pan Alvarez-Ossorio, M., additional, Mazuelos Bellido, F., additional, Suarez De Lezo Herreros De Tejada, J., additional, Altekin, E., additional, Yanikoglu, A., additional, Karakas, S., additional, Oncel, C., additional, Akdemir, B., additional, Belgi Yildirim, A., additional, Cilli, A., additional, Yilmaz, H., additional, Lenartowska, L., additional, Furdal, M., additional, Knysz, B., additional, Konieczny, A., additional, Lewczuk, J., additional, Severino, S., additional, Cavallaro, M., additional, Coppola, M., additional, Motoki, H., additional, To, A., additional, Bhargava, M., additional, Wazni, O., additional, Marwick, T., additional, Klein, A., additional, Sinkovskaya, E., additional, Horton, S., additional, Abuhamad, A., additional, Mingo Santos, S., additional, Monivas Palomero, V., additional, Beltran Correas, B., additional, Mitroi, C., additional, Gutierrez Landaluce, C., additional, Garcia Lunar, I., additional, Gonzalez Mirelis, J., additional, Cavero, M., additional, Segovia Cubero, J., additional, Alonso Pulpon, L., additional, Gurel, E., additional, Karaahmet, T., additional, Tigen, K., additional, Kirma, C., additional, Dundar, C., additional, Pala, S., additional, Isiklar, I., additional, Cevik, C., additional, Kilicgedik, A., additional, Basaran, Y., additional, Brambatti, M., additional, Romandini, A., additional, Barbarossa, A., additional, Molini, S., additional, Urbinati, A., additional, Giovagnoli, A., additional, Cipolletta, L., additional, Capucci, A., additional, Park, S., additional, Choi, E., additional, Ahn, C., additional, Hong, S., additional, Kim, M., additional, Lim, D., additional, Shim, W., additional, Xie, J., additional, Fang, F., additional, Zhang, Q., additional, Chan, J., additional, Yip, G., additional, Sanderson, J., additional, Lam, Y., additional, Yan, B., additional, Yu, C., additional, Jorge Perez, P., additional, De La Rosa Hernandez, A., additional, Hernandez Garcia, C., additional, Duque Garcia, A., additional, Barragan Acea, A., additional, Arroyo Ucar, E., additional, Jimenez Rivera, J., additional, Lacalzada Almeida, J., additional, Laynez Cerdena, I., additional, Carminati, C., additional, Capoulade, R., additional, Larose, E., additional, Clavel, M., additional, Dumesnil, J., additional, Arsenault, M., additional, Bedard, E., additional, Mathieu, P., additional, Pibarot, P., additional, Gargani, L., additional, Baldi, G., additional, Forfori, F., additional, Caramella, D., additional, D'errico, L., additional, Abramo, A., additional, Sicari, R., additional, Giunta, F., additional, Lee, W.-N., additional, Larrat, B., additional, Messas, E., additional, Pernot, M., additional, Tanter, M., additional, Velagic, V., additional, Cikes, M., additional, Matasic, R., additional, Skorak, I., additional, Samardzic, J., additional, Puljevic, D., additional, Lovric Bencic, M., additional, Biocina, B., additional, Milicic, D., additional, Roosens, B., additional, Bala, G., additional, Droogmans, S., additional, Hostens, J., additional, Somja, J., additional, Delvenne, E., additional, Schiettecatte, J., additional, Lahoutte, T., additional, Van Camp, G., additional, Cosyns, B., additional, Ghosh, A., additional, Hardy, R., additional, Chaturvedi, N., additional, Deanfield, J., additional, Pellerin, D., additional, Kuh, D., additional, Hughes, A., additional, Malmgren, A., additional, Dencker, M., additional, Stagmo, M., additional, Gudmundsson, P., additional, Seo, Y., additional, Ishizu, T., additional, Aonuma, K., additional, Schuuring, M. J., additional, Vis, J., additional, Van Dijk, A., additional, Van Melle, J., additional, Pieper, P., additional, Vliegen, H., additional, Sieswerda, G., additional, Foukarakis, E., additional, Pitarokilis, A., additional, Kafarakis, P., additional, Kiritsi, A., additional, Klironomos, E., additional, Manousakis, A., additional, Fragiadaki, X., additional, Papadakis, E., additional, and Dermitzakis, A., additional

Published
2011
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32. In Vitro and In Vivo Activities of Novel, Semisynthetic Thiopeptide Inhibitors of Bacterial Elongation Factor Tu

Author

Leeds, J. A., primary, LaMarche, M. J., additional, Brewer, J. T., additional, Bushell, S. M., additional, Deng, G., additional, Dewhurst, J. M., additional, Dzink-Fox, J., additional, Gangl, E., additional, Jain, A., additional, Lee, L., additional, Lilly, M., additional, Manni, K., additional, Mullin, S., additional, Neckermann, G., additional, Osborne, C., additional, Palestrant, D., additional, Patane, M. A., additional, Raimondi, A., additional, Ranjitkar, S., additional, Rann, E. M., additional, Sachdeva, M., additional, Shao, J., additional, Tiamfook, S., additional, Whitehead, L., additional, and Yu, D., additional

Published
2011
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38. Organotitanium compounds in organic synthesis

Author

Petasis, N. A., primary, Lu, S.-P., additional, Bzowej, E. I., additional, Fu, D.-K., additional, Staszewski, J. P., additional, Akritopoulou-Zanze, Irini, additional, Patane, M. A., additional, and Hu, Y.-H., additional

Published
1996
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42. In Vitroand In VivoActivities of Novel, Semisynthetic Thiopeptide Inhibitors of Bacterial Elongation Factor Tu

Author

Leeds, J. A., LaMarche, M. J., Brewer, J. T., Bushell, S. M., Deng, G., Dewhurst, J. M., Dzink-Fox, J., Gangl, E., Jain, A., Lee, L., Lilly, M., Manni, K., Mullin, S., Neckermann, G., Osborne, C., Palestrant, D., Patane, M. A., Raimondi, A., Ranjitkar, S., Rann, E. M., Sachdeva, M., Shao, J., Tiamfook, S., Whitehead, L., and Yu, D.

Abstract

ABSTRACTRecently, we identified aminothiazole derivatives of GE2270 A. These novel semisynthetic congeners, like GE2270 A, target the essential bacterial protein elongation factor Tu (EF-Tu). Medicinal chemistry optimization of lead molecules led to the identification of preclinical development candidates 1 and 2. These cycloalklycarboxylic acid derivatives show activity against difficult to treat Gram-positive pathogens and demonstrate increased aqueous solubility compared to GE2270 A. We describe here the in vitroand in vivoactivities of compounds 1 and 2 compared to marketed antibiotics. Compounds 1 and 2 were potent against clinical isolates of methicillin-resistant Staphylococcus aureusand vancomycin-resistant enterococci (MIC90≤ 0.25 μg/ml) but weaker against the streptococci (MIC90≥ 4 μg/ml). Like GE2270 A, the derivatives inhibited bacterial protein synthesis and selected for spontaneous loss of susceptibility via mutations in the tufgene, encoding EF-Tu. The mutants were not cross-resistant to other antibiotic classes. In a mouse systemic infection model, compounds 1 and 2 protected mice from lethal S. aureusinfections with 50% effective doses (ED50) of 5.2 and 4.3 mg/kg, respectively. Similarly, compounds 1 and 2 protected mice from lethal systemic E. faecalisinfections with ED50of 0.56 and 0.23 mg/kg, respectively. In summary, compounds 1 and 2 are active in vitroand in vivoactivity against difficult-to-treat Gram-positive bacterial infections and represent a promising new class of antibacterials for use in human therapy.

Published
2011
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43. Discovery and Characterization of Aminopiperidinecoumarin Melanin Concentrating Hormone Receptor 1 Antagonists

Author

Kym, P. R., Iyengar, R., Souers, A. J., Lynch, J. K., Judd, A. S., Gao, J., Freeman, J., Mulhern, M., Zhao, G., Vasudevan, A., Wodka, D., Blackburn, C., Brown, J., Che, J. L., Cullis, C., Lai, S. J., LaMarche, M. J., Marsilje, T., Roses, J., Sells, T., Geddes, B., Govek, E., Patane, M., Fry, D., Dayton, B. D., Brodjian, S., Falls, D., Brune, M., Bush, E., Shapiro, R., Knourek-Segel, V., Fey, T., McDowell, C., Reinhart, G. A., Preusser, L. C., Marsh, K., Hernandez, L., Sham, H. L., and Collins, C. A.

Abstract

4-(1-Benzo[1,3]dioxol-5-ylmethylpiperidine-4-ylmethyl)-6-chlorochromen-2-one (7) is a potent, orally bioavailable melanin concentrating hormone receptor 1 (MCHr1) antagonist that causes dose-dependent weight loss in diet-induced obese mice. Further evaluation of 7 in an anesthetized dog model of cardiovascular safety revealed adverse hemodynamic effects at a plasma concentration comparable to the minimally effective therapeutic concentration. These results highlight the need for scrutiny of the cardiovascular safety profile of MCHr1 antagonists.

Published
2005

45. Design and Synthesis of Novel α<INF>1</INF><INF>a</INF> Adrenoceptor-Selective Antagonists. 2. Approaches To Eliminate Opioid Agonist Metabolites via Modification of Linker and 4-Methoxycarbonyl-4-phenylpiperidine Moiety<SUP>1,2</SUP><BBR RID="jm990201hb00001"><BBR RID="jm990201hb00002">

Author

Dhar, T. G. Murali, Nagarathnam, D., Marzabadi, M. R., Lagu, B., Wong, W. C., Chiu, G., Tyagarajan, S., Miao, S. W., Zhang, F., Sun, W., Tian, D., Shen, Q., Zhang, J., Wetzel, J. M., Forray, C., Chang, R. S. L., Broten, T. P., Schorn, T. W., Chen, T. B., O'Malley, S., Ransom, R., Schneck, K., Bendesky, R., Harrell, C. M., Vyas, K. P., Zhang, K., Gilbert, J., Pettibone, D. J., Patane, M. A., Bock, M. G., Freidinger, R. M., and Gluchowski, C.

Abstract

We have previously described compound 1a as a high-affinity subtype selective α1a antagonist. In vitro and in vivo evaluation of compound 1a showed its major metabolite to be a μ-opioid agonist, 4-methoxycarbonyl-4-phenylpiperidine (3). Several dihydropyrimidinone analogues were synthesized with the goal of either minimizing the formation of 3 by modification of the linker or finding alternative piperidine moieties which when cleaved as a consequence of metabolism would not give rise to μ-opioid activity. Modification of the linker gave several compounds with good α1a binding affinity (Ki = &lt; 1 nM) and selectivity (>300-fold over α1b and α1d). In vitro analysis in the microsomal assay revealed these modifications did not significantly affect N-dealkylation and the formation of the piperidine 3. The second approach, however, yielded several piperidine replacements for 3, which did not show significant μ-opioid activity. Several of these compounds maintained good affinity at the α1a adrenoceptor and selectivity over α1b and α1d. For example, the piperidine fragments of (+)-73 and (+)-83, viz. 4-cyano-4-phenylpiperidine and 4-methyl-4-phenylpiperidine, were essentially inactive at the μ-opioid receptor (IC50 > 30 μM vs 3 μM for 3). Compounds (+)-73 and (+)-83 were subjected to detailed in vitro and in vivo characterization. Both these compounds, in addition to their excellent selectivity (>880-fold) over α1b and α1d, also showed good selectivity over several other recombinant human G-protein coupled receptors. Compounds (+)-73 and (+)-83 showed good functional potency in isolated human prostate tissues, with Kbs comparable to their in vitro α1a binding data. In addition, compound (+)-73 also exhibited good uroselectivity (DBP Kb/IUP Kb > 20-fold) in the in vivo experiments in dogs, similar to 1a.

Published
1999

48. Identification of 2-{2-[2-(5-Bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl}-4,5-dihydro-1H-imidazole (ML00253764), a Small Molecule Melanocortin 4 Receptor Antagonist That Effectively Reduces Tumor-Induced Weight Loss in a Mouse Model

Author

Vos, T. J., Caracoti, A., Che, J. L., Dai, M., Farrer, C. A., Forsyth, N. E., Drabic, S. V., Horlick, R. A., Lamppu, D., Yowe, D. L., Balani, S., Li, P., Zeng, H., Joseph, I. B. J. K., Rodriguez, L. E., Maguire, M. P., Patane, M. A., and Claiborne, C. F.

Abstract

The melanocortin 4 receptor (MC4R) plays an important role in body weight regulation and energy homeostasis. Administration of peptidic MC4R antagonists (usually by intracerebro ventricular injection) has been shown in the literature to increase body weight and/or food intake in several rodent models. We report here the identification of a novel nonpeptidic MC4R antagonist and its effects on tumor-induced weight loss in mice following peripheral administration.

Published
2004

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