Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Stéphane De Cesco"'
Autor:
Thomas Fontaine, Andreas Busch, Toon Laeremans, Stéphane De Cesco, Yi-Lynn Liang, Veli-Pekka Jaakola, Zara Sands, Sarah Triest, Simonas Masiulis, Lies Dekeyzer, Noor Samyn, Nicolas Loeys, Lisa Perneel, Melanie Debaere, Murielle Martini, Charlotte Vantieghem, Richa Virmani, Kamila Skieterska, Stephanie Staelens, Rosa Barroco, Maarten Van Roy, Christel Menet
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-14 (2024)
Abstract The melanocortin receptor 4 (MC4R) belongs to the melanocortin receptor family of G-protein coupled receptors and is a key switch in the leptin-melanocortin molecular axis that controls hunger and satiety. Brain-produced hormones such as α-
Externí odkaz:
https://doaj.org/article/f05dbb65117040f98bbf56edfbe2bf19
Publikováno v:
European Journal of Medicinal Chemistry. 138:96-114
In the history of therapeutics, covalent drugs occupy a very distinct category. While representing a significant fraction of the drugs on the market, very few have been deliberately designed to interact covalently with their biological target. In thi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::feaf4a09c21608231c211acc6cef7337
https://doi.org/10.1016/j.ejmech.2017.06.019
https://doi.org/10.1016/j.ejmech.2017.06.019
Autor:
Naëla Janmamode, Jessica Plescia, Stéphane De Cesco, Nicolas Moitessier, Mihai Burai Patrascu, Caroline Dufresne, Justin M. Di Trani, Anthony Mittermaier, Jerry Kurian, Alexander S. Wahba
Publikováno v:
Journal of medicinal chemistry. 62(17)
Over the past decade, there has been increasing interest in covalent inhibition as a drug design strategy. Our own interest in the development of prolyl oligopeptidase (POP) and fibroblast activation protein α (FAP) covalent inhibitors has led us to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9dd2722c866835dc57dbb5d5b333efff
https://pubmed.ncbi.nlm.nih.gov/31393718
https://pubmed.ncbi.nlm.nih.gov/31393718
Autor:
Anthony Mittermaier, Igor Huskić, Stéphane De Cesco, Karine Auclair, Francesco Airaghi, Sylvain Rocheleau, Jerry Kurian, Nicolas Moitessier, Gaëlle Mariaule, Paolo Schiavini
Publikováno v:
Journal of Medicinal Chemistry. 59:4221-4234
Bicyclic chiral scaffolds are privileged motifs in medicinal chemistry. Over the years, we have reported covalent bicyclic prolyl oligopeptidase inhibitors that were highly selective for POP over a number of homologous proteins. Herein, we wish to re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ed6c9397484713b61e4c2579832a7c6
https://doi.org/10.1021/acs.jmedchem.5b01296
https://doi.org/10.1021/acs.jmedchem.5b01296
Publikováno v:
Tetrahedron Letters. 56:6852-6856
In the process of improving the synthesis of a novel class of chiral drug scaffolds, first reported in 2010, we observed that the stereochemical outcome of the key chemical transformation appeared to be correlated to the solvophobicity of the reactio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1349cd679cc0275b7ad25dff66f36a98
https://doi.org/10.1016/j.tetlet.2015.10.086
https://doi.org/10.1016/j.tetlet.2015.10.086
Autor:
Stéphane De Cesco, Jessica Plescia, Claudia Jorge do Nascimento, Anthony Mittermaier, Nicolas Moitessier, Rebecca O'Leary, Justin M. Di Trani
Publikováno v:
Nature Communications
Nature Communications, Vol 9, Iss 1, Pp 1-7 (2018)
Nature Communications, Vol 9, Iss 1, Pp 1-7 (2018)
Although drug development typically focuses on binding thermodynamics, recent studies suggest that kinetic properties can strongly impact a drug candidate’s efficacy. Robust techniques for measuring inhibitor association and dissociation rates are
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf3af99378a37e730d3711ee9aa79dc1
http://europepmc.org/articles/PMC5832847
http://europepmc.org/articles/PMC5832847
Autor:
Manuel Lejeune, Alice Mattiuzzi, Benoit Colasson, Ivan Jabin, Olivia Reinaud, Andrea Brugnara, Stéphane De Cesco, David Coquière, Grégory Thiabaud, Angélique Lascaux, Jean-François Picron, Ulrich Darbost
Publikováno v:
The Journal of Organic Chemistry. 77:3838-3845
The ipso-nitration of calix[6]arene-based molecular receptors is a important synthetic pathway for the elaboration of more sophisticated systems. This reaction has been studied for a variety of capped calixarenes, and a general trend for the regiosel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b10e5e202ab1b75ecf58f2394458a083
https://doi.org/10.1021/jo300179h
https://doi.org/10.1021/jo300179h
Autor:
Toon Laeremans, Zara A. Sands, Pieter Claes, Ann De Blieck, Stephane De Cesco, Sarah Triest, Andreas Busch, David Felix, Abhinav Kumar, Veli-Pekka Jaakola, Christel Menet
Publikováno v:
Frontiers in Molecular Biosciences, Vol 9 (2022)
The human genome encodes 850 G protein-coupled receptors (GPCRs), half of which are considered potential drug targets. GPCRs transduce extracellular stimuli into a plethora of vital physiological processes. Consequently, GPCRs are an attractive drug
Externí odkaz:
https://doaj.org/article/ea4599d8f7de44b08618672b548d1833
Autor:
Marion Schuller, Tryfon Zarganes-Tzitzikas, James Bennett, Stephane De Cesco, Daren Fearon, Frank von Delft, Oleg Fedorov, Paul E. Brennan, Ivan Ahel
Publikováno v:
Pathogens, Vol 12, Iss 2, p 324 (2023)
The worldwide public health and socioeconomic consequences caused by the COVID-19 pandemic highlight the importance of increasing preparedness for viral disease outbreaks by providing rapid disease prevention and treatment strategies. The NSP3 macrod
Externí odkaz:
https://doaj.org/article/d095de8ed820404392759fd4296b33f6
Publikováno v:
PLoS ONE, Vol 15, Iss 9, p e0232644 (2020)
When trying to identify new potential therapeutic protein targets, access to data and knowledge is increasingly important. In a field where new resources and data sources become available every day, it is crucial to be able to take a step back and lo
Externí odkaz:
https://doaj.org/article/6d4e15cafb6d4933858ad78b832e3499