21 results on '"Kamdem, N."'
Search Results
2. Studies of adsorption of 2,2′-bipyridyl on the surface of highly regulated silica matrix of the MCM-41 type by means of 15N NMR spectroscopy
- Author
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Lesnichin, S. B., Kamdem, N., Mauder, D., Denisov, G. S., and Shenderovich, I. G.
- Published
- 2010
- Full Text
- View/download PDF
3. Additive influences of soil and climate gradients drive tree community composition of Central African rain forests
- Author
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Libalah, M. B., Droissart, Vincent, Sonke, B., Barbier, Nicolas, Dauby, Gilles, Fortunel, Claire, Kamdem, G., Kamdem, N., Lewis, S. L., Mofack, G. I. I., Momo, S. T., Pélissier, Raphaël, Ploton, Pierre, Texier, Nicolas, Zebaze, D., and Couteron, Pierre
- Subjects
tropical rain forests ,climate gradient ,soil gradient ,species ,Cameroon ,occurrence ,species abundance - Abstract
Aim Examining tree species-environment association can offer insight into the drivers of vegetation patterns and key information of practical relevance to forest management. Here, we aim to quantify the contribution of climate and soil gradients to variation in Central African tree species composition (abundance and occurrence). Location Tropical rain forests of southern and eastern Cameroon. Methods We established 82 1-ha permanent plots across seven localities and censused all trees >= 10 cm in diameter, representing a total of 37,733 trees and 455 species. In 60 of those plots, we measured 10 soil variables describing texture and nutrients levels and extracted 10 bioclimatic variables from global-gridded climate databases. We synthesized the main environmental gradients by conducting principal component analyses on climate and soil data, respectively. We performed unconstrained and constrained non-symmetric correspondence analyses to account for the individual and joint contributions of climate and soil on species abundance and occurrence. Results Climate and soil contributed similarly to variances of species abundance and occurrence (12-15% variance for climate vs 11-12% variance for soil). Climate influence mostly concerns some abundant species, while some of the less abundant species were mainly driven by soil. Fractions of species variances accounted for by climate and soil show strong correlation when assessed from species occurrence and abundance data. Conclusion Variation in occurrence and abundance of tropical forest trees can be partly shaped by both climate and soil gradients in Cameroon, which emphasizes the importance to jointly consider soil and climate in species distribution modeling. Less abundant species may express environmental influence differently than abundant species and convey complementary information about community assemblage. Though showing congruent patterns here, species abundance and occurrence reflect different interacting community processes and both should be examined to better understand vegetation patterns.
- Published
- 2020
4. Phylogenomic approaches reveal how climate shapes patterns of genetic diversity in an African rain forest tree species
- Author
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Helmstetter, A. J., Amoussou, B. E. N., Bethune, Kévin, Kamdem, N. G., Kakai, R. G., Sonke, B., and Couvreur, Thomas
- Subjects
refugia ,nuclear baiting ,immigrant inviability ,Annonaceae ,kit ,phylogeography ,climatic inversion - Abstract
The world's second largest expanse of tropical rainforest is in Central Africa, and it harbours enormous species diversity. Population genetic studies have consistently revealed significant structure across Central African rainforest plants. In particular, previous studies have repeatedly demonstrated a north-south genetic discontinuity around the equatorial line, in a continuous expanse of rainforest where a climatic inversion is documented. Here, we took a phylogeographic approach by sequencing 351 nuclear markers in 112 individuals across the distribution of the African rainforest tree speciesAnnickia affinis(Annonaceae). We showed for the first time that the north-south divide is the result of a single, major colonization event across the climatic inversion from an ancestral population located in Gabon. We suggested that differences in ecological niche of populations located on either side of this inversion may have contributed to this phylogenetic discontinuity. We found evidence for inland dispersal, predominantly in northern areas, and variable demographic histories among genetic clusters, indicating that populations responded differently to past climate change. We show how newly developed genomic tools can provide invaluable insights into our understanding of tropical rainforest evolutionary dynamics.
- Published
- 2020
5. Individualistic evolutionary responses of Central African rain forest plants to Pleistocene climatic fluctuations
- Author
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Helmstetter, A. J., Bethune, K., Kamdem, N. G., Sonke, B., and Couvreur, Thomas
- Subjects
phylogenetics ,demography ,tropical rain forests ,climate change - Abstract
Understanding the evolutionary dynamics of genetic diversity is fundamental for species conservation in the face of climate change, particularly in hyper-diverse biomes. Species in a region may respond similarly to climate change, leading to comparable evolutionary dynamics, or individualistically, resulting in dissimilar patterns. The second-largest expanse of continuous tropical rain forest (TRF) in the world is found in Central Africa. Here, present-day patterns of genetic structure are thought to be dictated by repeated expansion and contraction of TRFs into and out of refugia during Pleistocene climatic fluctuations. This refugia model implies a common response to past climate change. However, given the unrivalled diversity of TRFs, species could respond differently because of distinct environmental requirements or ecological characteristics. To test this, we generated genome-wide sequence data for >700 individuals of seven codistributed plants from Lower Guinea in Central Africa. We inferred species' evolutionary and demographic histories within a comparative phylogeographic framework. Levels of genetic structure varied among species and emerged primarily during the Pleistocene, but divergence events were rarely concordant. Demographic trends ranged from repeated contraction and expansion to continuous growth. Furthermore, patterns in genetic variation were linked to disparate environmental factors, including climate, soil, and habitat stability. Using a strict refugia model to explain past TRF dynamics is too simplistic. Instead, individualistic evolutionary responses to Pleistocene climatic fluctuations have shaped patterns in genetic diversity. Predicting the future dynamics of TRFs under climate change will be challenging, and more emphasis is needed on species ecology to better conserve TRFs worldwide.
- Published
- 2020
6. Additive influences of soil and climate gradients drive tree community composition of Central African rain forests
- Author
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Libalah, Moses, Droissart, Vincent, Sonke, Bonaventure, Barbier, Nicolas Serge, Dauby, Gilles, Fortunel, Claire, Kamdem, G., Kamdem, N., Lewis, Simon S.L., Mofack, Gislain II, Momo, Stéphane Takoudjou, Pélissier, Raphaël, Ploton, Pierre, Texier, Nicolas, Zebaze, Donatien, Couteron, Piere, Libalah, Moses, Droissart, Vincent, Sonke, Bonaventure, Barbier, Nicolas Serge, Dauby, Gilles, Fortunel, Claire, Kamdem, G., Kamdem, N., Lewis, Simon S.L., Mofack, Gislain II, Momo, Stéphane Takoudjou, Pélissier, Raphaël, Ploton, Pierre, Texier, Nicolas, Zebaze, Donatien, and Couteron, Piere
- Abstract
Aim: Examining tree species–environment association can offer insight into the drivers of vegetation patterns and key information of practical relevance to forest management. Here, we aim to quantify the contribution of climate and soil gradients to variation in Central African tree species composition (abundance and occurrence). Location: Tropical rain forests of southern and eastern Cameroon. Methods: We established 82 1-ha permanent plots across seven localities and censused all trees ≥10 cm in diameter, representing a total of 37,733 trees and 455 species. In 60 of those plots, we measured 10 soil variables describing texture and nutrients levels and extracted 10 bioclimatic variables from global-gridded climate databases. We synthesized the main environmental gradients by conducting principal component analyses on climate and soil data, respectively. We performed unconstrained and constrained non-symmetric correspondence analyses to account for the individual and joint contributions of climate and soil on species abundance and occurrence. Results: Climate and soil contributed similarly to variances of species abundance and occurrence (12–15% variance for climate vs 11–12% variance for soil). Climate influence mostly concerns some abundant species, while some of the less abundant species were mainly driven by soil. Fractions of species variances accounted for by climate and soil show strong correlation when assessed from species occurrence and abundance data. Conclusion: Variation in occurrence and abundance of tropical forest trees can be partly shaped by both climate and soil gradients in Cameroon, which emphasizes the importance to jointly consider soil and climate in species distribution modeling. Less abundant species may express environmental influence differently than abundant species and convey complementary information about community assemblage. Though showing congruent patterns here, species abundance and occurrence reflect different interacting commu, SCOPUS: ar.j, info:eu-repo/semantics/published
- Published
- 2020
7. Bilan des études relatives au sanglier en Wallonie avant le foyer de peste porcine africaine - Novembre 2018
- Author
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A. M. Licoppe, Della Libera, F., Linden, Annick, Volpe, Rosario, Lesenfants, Christophe, Paternostre, Julien, Gilliaux, G., Kamdem, N., Flamand, Marie Christine, Nizet, S., Bertouille, Sabine, Morelle, Kevin, Prévot, Céline, Balligand, Bruno, Denies, L., Malengreaux, Céline, Lievens Julien, Widar, J., Hansenne, F., Terneus, A., and Herman, M.
- Published
- 2019
- Full Text
- View/download PDF
8. Using volume-weighted average wood specific gravity of trees reduces bias in aboveground biomass predictions from forest volume data
- Author
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Sagang, L. B. T., Momo, S. T., Libalah, M. B., Rossi, V., Fonton, N., Mofack, G. I., Kamdem, N. G., Nguetsop, V. F., Sonke, B., Pierre, P., and Barbier, Nicolas
- Subjects
Error propagation ,Terrestrial LiDAR ,Linear model ,Cameroon eastern forest ,Aboveground biomass ,Remote sensing ,Wood specific gravity - Abstract
With the improvement of remote sensing techniques for forest inventory application such as terrestrial LiDAR, tree volume can now be measured directly, without resorting to allometric equations. However, wood specific gravity (WSG) remains a crucial factor for converting these precise volume measurements into unbiased biomass estimates. In addition to this WSG values obtained from samples collected at the base of the tree (WSG(Base)) or from global repositories such as Dryad (WSG(Dryad)) can be substantially biased relative to the overall tree value. Our aim was to assess and mitigate error propagation at tree and stand level using a pragmatic approach that could be generalized to National Forest Inventories or other carbon assessment efforts based on measured volumetric data. In the semi-deciduous forests of Eastern Cameroon, we destructively sampled 130 trees belonging to 15 species mostly represented by large trees (up to 45 Mg). We also used stand-level dendrometric parameters from 21 1-ha plots inventoried in the same area to propagate the tree-level bias at the plot level. A new descriptor, volume average-weighted WSG (WWSG) of the tree was computed by weighting the WSG of tree compartments by their relative volume prior to summing at tree level. As WWSG cannot be assessed non-destructively, linear models were adjusted to predict field WWSG and revealed that a combination of WSG(Dryad), diameter at breast height (DBH) and species stem morphology (S-m) were significant predictors explaining together 72% of WWSG variation. At tree level, estimating tree aboveground biomass using WSG(Base) and WSG(Dryad) yielded overestimations of 10% and 7% respectively whereas predicted WWSG only produced an underestimation of less than 1%. At stand-level, WSG(Base) and WSG(Dryad) gave an average simulated bias of 9% (S.D. = +/- 7) and 3% (S.D. = +/- 7) respectively whereas predicted WWSG reduced the bias by up to 0.1% (S.D. = +/- 8). We also observed that the stand-level bias obtained with WSG(Base) and WSG(Dryad) decreased with total plot size and plot area. The systematic bias induced by WSG(Base) and WSG(Dryad) for biomass estimations using measured volumes are clearly not negligible but yet generally overlooked. A simple corrective approach such as the one proposed with our predictive WWSG model is liable to improve the precision of remote sensing-based approaches for broader scale biomass estimations.
- Published
- 2018
9. Allometric Models to Estimate Leaf Area for Tropical African Broadleaved Forests
- Author
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Sirri, N. F., primary, Libalah, M. B., additional, Momo Takoudjou, S., additional, Ploton, P., additional, Medjibe, V., additional, Kamdem, N. G., additional, Mofack, G., additional, Sonké, B., additional, and Barbier, N., additional
- Published
- 2019
- Full Text
- View/download PDF
10. Spatio-temporal patterns of orchids flowering in Cameroonian rainforests
- Author
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Texier, Nicolas, Deblauwe, Vincent, Stévart, Tariq, Sonke, Bonaventure, Simo-Droissart, Murielle, Azandi Ngnintedem, Laura, Bose, Ruksan, Djuikouo, Marie Noël, Kamdem, G., Kamdem, N., Mayogo, S., Zemagho, Lise L.A., Droissart, Vincent, Texier, Nicolas, Deblauwe, Vincent, Stévart, Tariq, Sonke, Bonaventure, Simo-Droissart, Murielle, Azandi Ngnintedem, Laura, Bose, Ruksan, Djuikouo, Marie Noël, Kamdem, G., Kamdem, N., Mayogo, S., Zemagho, Lise L.A., and Droissart, Vincent
- Abstract
We characterized the flowering patterns of 45 epiphytic orchid species occurring in Cameroonian rainforests to explore the environmental and evolutionary forces driving their phenology. We used a dataset of 3470 flowering events recorded over a period of 11 years in the Yaoundé living collection (82% of the flowering events) and from in situ observations (18% of the flowering events) to (i) describe flowering frequency and timing and synchronization among taxa; (ii) test flowering patterns for phylogenetic relatedness at the generic level; and (iii) investigate the spatial patterns of phenology. An annual flowering pattern prevailed among the species selected for this study. The species-rich African genera Angraecum and Polystachya are characterized by subannual and annual frequency patterns, respectively. However, in terms of flowering time, no phylogenetic signal was detected for the four most diverse genera (Ancistrorhynchus, Angraecum, Bulbophyllum, and Polystachya). Results suggest also an important role of photoperiod and precipitation as climatic triggers of flowering patterns. Moreover, 16% of the taxa cultivated ex situ, mostly Polystachya, showed significant differences in flowering time between individuals originating from distinct climatic regions, pointing toward the existence of phenological ecotypes. Phenological plasticity, suggested by the lack of synchronized flowering in spatially disjunct populations of Polystachya, could explain the widespread radiation of this genus throughout tropical Africa. Our study highlights the need to take the spatial pattern of flowering time into account when interpreting phylogeographic patterns in central African rainforests., SCOPUS: ar.j, info:eu-repo/semantics/published
- Published
- 2018
11. New taxonomic and conservation status of Ossiculum (Vandeae, Orchidaceae), a highly threatened and narrow-endemic angraecoid orchid from Central Africa
- Author
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Simo-Droissart, Murielle, Stevart, Tariq, Sonke, Bonaventure, Mayogo, S., Kamdem, N., Droissart, Vincent, Simo-Droissart, Murielle, Stevart, Tariq, Sonke, Bonaventure, Mayogo, S., Kamdem, N., and Droissart, Vincent
- Abstract
In the context of producing a revised phylogenetic Linnean taxonomy of angraecoid orchids, the monotypic and narrow-endemic genus Ossiculum is synonymised with Calyptrochilum. Accordingly, a new combination in Calyptrochilum is proposed for Ossiculum aurantiacum. The morphological and DNA-based evidence for this transfer is discussed. Moreover, Calyptrochilum aurantiacum is here firstly reported outside Cameroon, with a record from the Republic of the Congo. The Red List conservation status of this species is reassessed and it is to be downgraded from "Critically Endangered" (CR) to "Endangered" (EN), following the recent discovery of additional subpopulations in Cameroon., SCOPUS: ar.j, info:eu-repo/semantics/published
- Published
- 2018
12. Closing a gap in tropical forest biomass estimation: accounting for crown mass variation in pantropical allometries
- Author
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Ploton, P., primary, Barbier, N., additional, Momo, S. T., additional, Réjou-Méchain, M., additional, Boyemba Bosela, F., additional, Chuyong, G., additional, Dauby, G., additional, Droissart, V., additional, Fayolle, A., additional, Goodman, R. C., additional, Henry, M., additional, Kamdem, N. G., additional, Katembo Mukirania, J., additional, Kenfack, D., additional, Libalah, M., additional, Ngomanda, A., additional, Rossi, V., additional, Sonké, B., additional, Texier, N., additional, Thomas, D., additional, Zebaze, D., additional, Couteron, P., additional, Berger, U., additional, and Pélissier, R., additional
- Published
- 2015
- Full Text
- View/download PDF
13. Supplementary material to "Closing a gap in tropical forest biomass estimation: accounting for crown mass variation in pantropical allometries"
- Author
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Ploton, P., primary, Barbier, N., additional, Momo, S. T., additional, Réjou-Méchain, M., additional, Boyemba Bosela, F., additional, Chuyong, G., additional, Dauby, G., additional, Droissart, V., additional, Fayolle, A., additional, Goodman, R. C., additional, Henry, M., additional, Kamdem, N. G., additional, Katembo Mukirania, J., additional, Kenfack, D., additional, Libalah, M., additional, Ngomanda, A., additional, Rossi, V., additional, Sonké, B., additional, Texier, N., additional, Thomas, D., additional, Zebaze, D., additional, Couteron, P., additional, Berger, U., additional, and Pélissier, R., additional
- Published
- 2015
- Full Text
- View/download PDF
14. Closing a gap in tropical forest biomass estimation: accounting for crown mass variation in pantropical allometries.
- Author
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Ploton, P., Barbier, N., Momo, S. T., Réjou-Méchain, M., Bosela, F. Boyemba, Chuyong, G., Dauby, G., Droissart, V., Fayolle, A., Goodman, R. C., Henry, M., Kamdem, N. G., Mukirania, J. Katembo, Kenfack, D., Libalah, M., Ngomanda, A., Rossi, V., Sonké, B., Texier, N., and Thomas, D.
- Subjects
TROPICAL forests ,FOREST biomass ,ALLOMETRY in plants ,CARBON dioxide ,CROWNS (Botany) - Abstract
Accurately monitoring tropical forest carbon stocks is an outstanding challenge. Allometric models that consider tree diameter, height and wood density as predictors are currently used in most tropical forest carbon studies. In particular, a pantropical biomass model has been widely used for approximately a decade, and its most recent version will certainly constitute a reference in the coming years. However, this reference model shows a systematic bias for the largest trees. Because large trees are key drivers of forest carbon stocks and dynamics, understanding the origin and the consequences of this bias is of utmost concern. In this study, we compiled a unique tree mass dataset on 673 trees measured in five tropical countries (101 trees > 100 cm in diameter) and an original dataset of 130 forest plots (1 ha) from central Africa to quantify the error of biomass allometric models at the individual and plot levels when explicitly accounting or not accounting for crown mass variations. We first showed that the proportion of crown to total tree aboveground biomass is highly variable among trees, ranging from 3 to 88%. This proportion was constant on average for trees < 10 Mg (mean of 34%) but, above this threshold, increased sharply with tree mass and exceeded 50% on average for trees = 45 Mg. This increase coincided with a progressive deviation between the pantropical biomass model estimations and actual tree mass. Accounting for a crown mass proxy in a newly developed model consistently removed the bias observed for large trees (> 1 Mg) and reduced the range of plot-level error from -23-16 to 0-10%. The disproportionally higher allocation of large trees to crown mass may thus explain the bias observed recently in the reference pantropical model. This bias leads to far-from-negligible, but often overlooked, systematic errors at the plot level and may be easily corrected by accounting for a crown mass proxy for the largest trees in a stand, thus suggesting that the accuracy of forest carbon estimates can be significantly improved at a minimal cost. [ABSTRACT FROM AUTHOR]
- Published
- 2015
- Full Text
- View/download PDF
15. Tetrahydroquinoline carboxylates are potent inhibitors of the Shank PDZ domain, a putative target in autism disorders
- Author
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Saupe, J., primary, Roske, Y., additional, Schillinger, C., additional, Kamdem, N., additional, Radetzki, S., additional, Diehl, A., additional, Oschkinat, H., additional, Krause, G., additional, Heinemann, U., additional, and Rademann, J., additional
- Published
- 2011
- Full Text
- View/download PDF
16. Studies of adsorption of 2,2′-bipyridyl on the surface of highly regulated silica matrix of the MCM-41 type by means of N NMR spectroscopy.
- Author
-
Lesnichin, S. B., Kamdem, N., Mauder, D., Denisov, G. S., and Shenderovich, I. G.
- Subjects
SILICA ,ADSORPTION (Chemistry) ,BIPYRIDINIUM compounds ,NUCLEAR magnetic resonance spectroscopy ,ISOTROPY subgroups ,CHEMICAL structure ,HYDROGEN bonding ,MONOMOLECULAR films - Abstract
The study of 2,2′-bipyridyl adsorption on the surface of highly regular MCM-41 silica at 300 and 130 K was carried out by the N NMR spectroscopy. It was shown that at 300 K the adsorbed molecules were involved in the processes of isotropic reorientation accompanied by the formation and rupture of hydrogen bonds with the surface-located hydroxy groups. Each molecule of 2,2′-bipyridyl forms no more than one hydrogen bond at a time, and their surface density is about one molecule per 1 nm of the surface. At 130 K 2,2′-bipyridyl forms a monolayer on the surface of silica including about 1.6 molecule per 1 nm. In this monolayer each molecule forms a hydrogen bond with one hydroxy group and prevents the interaction of the other bipyridyl molecules with one more hydroxy group. [ABSTRACT FROM AUTHOR]
- Published
- 2010
- Full Text
- View/download PDF
17. Interactions between soil and other environmental variables modulate forest expansion and ecotone dynamics in humid savannas of Central Africa.
- Author
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Sagang LBT, Tcheferi I, Ploton P, Libalah M, Simo-Droissart M, Sirri N, Dauby G, Ngansop E, Bissek JP, Kamdem N, Mofack GII, Zebaze D, Leblanc H, Djonko F, Sonké B, Barbier N, and Couteron P
- Subjects
- Africa, Central, Trees, Biomass, Poaceae physiology, Fires, Ecosystem, Soil chemistry, Forests, Grassland
- Abstract
Forest expansion into savanna is a pervasive phenomenon in West and Central Africa, warranting comparative studies under diverse environmental conditions. We collected vegetation data from the woody and grassy components within 73 plots of 0.16 ha distributed along a successional gradient from humid savanna to forest in Central Africa. We associated spatially collocated edaphic parameters and fire frequency derived from remote sensing to investigate their combined influence on the vegetation. Soil texture was more influential in shaping savanna structure and species distribution than soil fertility, with clay-rich soils promoting higher grass productivity and fire frequency. Savanna featuring woody aboveground biomass surpassing 40 Mg ha
-1 could escape the grass-fire feedback loop, by depressing grass biomass below 4 Mg ha-1 . This thicker woody layer also favoured the establishment of fire-tolerant forest pioneers, which synergically contributed to the expansion of forests. Conversely, savannas below this fire suppression threshold sustained a balance between trees and grasses through the grass-fire feedback mechanism. This hysteresis loop, particularly pronounced on clayey soils, suggests that the contrast between grassy savanna and young forests might represent alternative ecosystem states, although savannas with low woody biomass remained vulnerable to forest edge encroachment.- Published
- 2024
- Full Text
- View/download PDF
18. Small-molecule inhibitors of the PDZ domain of Dishevelled proteins interrupt Wnt signalling.
- Author
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Kamdem N, Roske Y, Kovalskyy D, Platonov MO, Balinskyi O, Kreuchwig A, Saupe J, Fang L, Diehl A, Schmieder P, Krause G, Rademann J, Heinemann U, Birchmeier W, and Oschkinat H
- Abstract
Dishevelled (Dvl) proteins are important regulators of the Wnt signalling pathway, interacting through their PDZ domains with the Wnt receptor Frizzled. Blocking the Dvl PDZ-Frizzled interaction represents a potential approach for cancer treatment, which stimulated the identification of small-molecule inhibitors, among them the anti-inflammatory drug Sulindac and Ky-02327. Aiming to develop tighter binding compounds without side effects, we investigated structure-activity relationships of sulfonamides. X-ray crystallography showed high complementarity of anthranilic acid derivatives in the GLGF loop cavity and space for ligand growth towards the PDZ surface. Our best binding compound inhibits Wnt signalling in a dose-dependent manner as demonstrated by TOP-GFP assays (IC 50 ∼ 50 µ M ) and Western blotting of β -catenin levels. Real-time PCR showed reduction in the expression of Wnt-specific genes. Our compound interacted with Dvl-1 PDZ (K D = 2.4 µ M ) stronger than Ky-02327 and may be developed into a lead compound interfering with the Wnt pathway., Competing Interests: The authors declare that they have no conflict of interest., (Copyright: © 2021 Nestor Kamdem et al.)
- Published
- 2021
- Full Text
- View/download PDF
19. New taxonomic and conservation status of Ossiculum (Vandeae, Orchidaceae), a highly threatened and narrow-endemic angraecoid orchid from Central Africa.
- Author
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Simo-Droissart M, Stévart T, Sonké B, Sandrine Mayogo, Kamdem N, and Droissart V
- Abstract
In the context of producing a revised phylogenetic Linnean taxonomy of angraecoid orchids, the monotypic and narrow-endemic genus Ossiculum is synonymised with Calyptrochilum . Accordingly, a new combination in Calyptrochilum is proposed for Ossiculum aurantiacum . The morphological and DNA-based evidence for this transfer is discussed. Moreover, Calyptrochilum aurantiacum is here firstly reported outside Cameroon, with a record from the Republic of the Congo. The Red List conservation status of this species is reassessed and it is to be downgraded from "Critically Endangered" (CR) to "Endangered" (EN), following the recent discovery of additional subpopulations in Cameroon.
- Published
- 2018
- Full Text
- View/download PDF
20. Small-molecule inhibitors of AF6 PDZ-mediated protein-protein interactions.
- Author
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Vargas C, Radziwill G, Krause G, Diehl A, Keller S, Kamdem N, Czekelius C, Kreuchwig A, Schmieder P, Doyle D, Moelling K, Hagen V, Schade M, and Oschkinat H
- Subjects
- Amino Acid Sequence, Binding Sites, Humans, Kinesins metabolism, Ligands, Molecular Docking Simulation, Myosins metabolism, PDZ Domains, Peptides chemistry, Peptides metabolism, Protein Interaction Domains and Motifs, Receptor, EphB2 chemistry, Signal Transduction drug effects, Small Molecule Libraries metabolism, Structure-Activity Relationship, Kinesins antagonists & inhibitors, Myosins antagonists & inhibitors, Small Molecule Libraries chemistry
- Abstract
PDZ (PSD-95, Dlg, ZO-1) domains are ubiquitous interaction modules that are involved in many cellular signal transduction pathways. Interference with PDZ-mediated protein-protein interactions has important implications in disease-related signaling processes. For this reason, PDZ domains have gained attention as potential targets for inhibitor design and, in the long run, drug development. Herein we report the development of small molecules to probe the function of the PDZ domain from human AF6 (ALL1-fused gene from chromosome 6), which is an essential component of cell-cell junctions. These compounds bind to AF6 PDZ with substantially higher affinity than the peptide (Ile-Gln-Ser-Val-Glu-Val) derived from its natural ligand, EphB2. In intact cells, the compounds inhibit the AF6-Bcr interaction and interfere with epidermal growth factor (EGF)-dependent signaling., (© 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Published
- 2014
- Full Text
- View/download PDF
21. Discovery, structure-activity relationship studies, and crystal structure of nonpeptide inhibitors bound to the Shank3 PDZ domain.
- Author
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Saupe J, Roske Y, Schillinger C, Kamdem N, Radetzki S, Diehl A, Oschkinat H, Krause G, Heinemann U, and Rademann J
- Subjects
- Amino Acid Sequence, Binding Sites, Carrier Proteins genetics, Carrier Proteins metabolism, Crystallography, X-Ray, Drug Evaluation, Preclinical, Humans, Nerve Tissue Proteins, PDZ Domains drug effects, Peptides chemical synthesis, Peptides chemistry, Protein Interaction Domains and Motifs, Quinolines chemical synthesis, Quinolines pharmacology, Recombinant Proteins chemistry, Recombinant Proteins genetics, Recombinant Proteins metabolism, Structure-Activity Relationship, Carrier Proteins chemistry, Quinolines chemistry
- Abstract
Shank is the central scaffolding protein of the postsynaptic density (PSD) protein complex found in cells of the central nervous system. Cellular studies indicate a prominent role of the protein in the organization of the PSD, in the development of neuronal morphology, in neuronal signaling, and in synaptic plasticity, thus linking Shank functions to the molecular basis of learning and memory. Mutations in the Shank gene have been found in several neuronal disorders including mental retardation, typical autism, and Asperger syndrome. Shank is linked to the PSD complex via its PDZ domain that binds to the C-terminus of guanylate-kinase-associated protein (GKAP). Here, small-molecule inhibitors of Shank3 PDZ domain are developed. A fluorescence polarization assay based on an identified high-affinity peptide is established, and tetrahydroquinoline carboxylates are identified as inhibitors of this protein-protein interaction. Chemical synthesis via a hetero-Diels-Alder strategy is employed for hit optimization, and structure-activity relationship studies are performed. Best hits possess K(i) values in the 10 μM range, and binding to the PDZ domain is confirmed by ¹H,¹⁵N HSQC NMR experiments. One of the hits crystallizes with the Shank3 PDZ domain. The structure, analyzed at a resolution of 1.85 Å, reveals details of the binding mode. Finally, binding to PDZ domains of PSD-95, syntrophin, and DVL3 was studied using ¹H,¹⁵N HSQC NMR spectroscopy., (Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Published
- 2011
- Full Text
- View/download PDF
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