Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Sabine, Schlyer"'
Autor:
Sabine Schlyer, Graeme Milligan, Laura Jenkins, Meritxell Canals, Kate Campbell, Elisa Alvarez-Curto, Sabrina de Munnik
Publikováno v:
British Journal of Pharmacology. 162:733-748
BACKGROUND AND PURPOSE GPR35 is a poorly characterized G protein-coupled receptor at which kynurenic acid has been suggested to be the endogenous ligand. We wished to test this and develop assays appropriate for the study of this receptor. EXPERIMENT
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c71d2eb86a53d234a38eb2124393c8bb
https://doi.org/10.1111/j.1476-5381.2010.01082.x
https://doi.org/10.1111/j.1476-5381.2010.01082.x
Autor:
Stanley Kugler, John D. Ginn, Xiang Li, Todd Bosanac, Mohammed A. Kashem, Steven Kerr, Anthony S. Prokopowicz, Michael Robert Turner, Frank Wu, Erick R. R. Young, James D. Smith, Eugene R. Hickey, Sabine Schlyer, Charles L. Cywin, Rhonda Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5153-5156
Phenylglycine substituted isoquinolones 1 and 2 have previously been described as potent dual ROCK1/ROCK2 inhibitors. Here we describe the further SAR of this series to improve metabolic stability and rat oral exposure. Piperidine analog 20 which dem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c1691612ce33705cab799aaae34b250
https://doi.org/10.1016/j.bmcl.2010.07.014
https://doi.org/10.1016/j.bmcl.2010.07.014
Autor:
Amy Liang, Dao Lentz, Bin Ye, David D. Davey, Karen May, John Parkinson, Beverly King, Hong Ye, Gary Phillips, Robert G. Wei, William J. Guilford, Sabine Schlyer, Lisa M. Mendoza, Selchau Victor, Seock-Kyu Khim, Jih-Lie Tseng, John G. Bauman, Kochanny Monica, Thomas A. Kirkland, Ming Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3891-3894
The synthesis and biological evaluation of a series of N-alkyl glycine amide analogs as LTA(4)-h inhibitors and the importance of the introduction of a benzoic acid group to the potency and pharmacokinetic parameters of our analogs are described. The
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56a67c0a4315dcbeaa6a8190f571d4d2
https://doi.org/10.1016/j.bmcl.2008.06.046
https://doi.org/10.1016/j.bmcl.2008.06.046
Autor:
Richard Horuk, Sabine Schlyer
Publikováno v:
Drug Discovery Today. 11:481-493
Huey Lewis and the News summed it up nicely in their 1980s hit record: 'I want a new drug, one that won't make me sick, one that won't make me crash my car, or make me feel three feet thick'. The song could be an anthem for drug discovery in the phar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3969b6e487c4a900626856a7b831ab58
https://doi.org/10.1016/j.drudis.2006.04.008
https://doi.org/10.1016/j.drudis.2006.04.008
Autor:
Laura, Jenkins, Elisa, Alvarez-Curto, Kate, Campbell, Sabrina, de Munnik, Meritxell, Canals, Sabine, Schlyer, Graeme, Milligan
Publikováno v:
British journal of pharmacology. 162(3)
GPR35 is a poorly characterized G protein-coupled receptor at which kynurenic acid has been suggested to be the endogenous ligand. We wished to test this and develop assays appropriate for the study of this receptor.Human and rat orthologues of GPR35
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::5c3b7a6378e489d8c1ebef08ee668939
https://pubmed.ncbi.nlm.nih.gov/20958291
https://pubmed.ncbi.nlm.nih.gov/20958291
Autor:
Shuang Liang, Kathleen Haverty, Donghong Amy Gao, Jun Li, Xiang Li, Sabine Schlyer, Alexander Heim-Riether, Melissa Hill-Drzewi, Steven John Taylor, Steluta Mariana Margarit, Lana Louise Smith Keenan, Neil Moss, Nelamangala V. Nagaraja, Xianhua Cao, Dieter Wiedenmayer, Neil A. Farrow, Kyle E. Harrington, Brandon Collins, E. Michael August, Leonard Ciccarelli, Rene Roman, Bernd Wellenzohn, Zhaoming Xiong, Laura Amodeo, John R. Proudfoot
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(17)
SAR studies to improve the selectivity and metabolic stability of a class of recently discovered MMP-13 inhibitors are reported. Improved selectivity was achieved by modifying interactions with the S1' pocket. Metabolic stability was improved through
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e5361dabb2993b47e9d3285e7d2bb2c7
https://pubmed.ncbi.nlm.nih.gov/20675133
https://pubmed.ncbi.nlm.nih.gov/20675133
Autor:
Steven Kerr, Erick R. R. Young, Eugene R. Hickey, Todd Bosanac, Alan Olague, John D. Ginn, Sabine Schlyer, Stanley Kugler, Xiang Li, Mohammed A. Kashem
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(12)
The discovery and SAR of a series of beta-aryl substituted pyrrolidine 2H-isoquinolin-1-one inhibitors of Rho-kinase (ROCK) derived from 2 is herein described. SAR studies have shown that aryl groups in the beta-position are optimal for potency. Our
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f9c2c4f36334933f05f7838dd863ba1
https://pubmed.ncbi.nlm.nih.gov/20471253
https://pubmed.ncbi.nlm.nih.gov/20471253
Autor:
Richard Horuk, Wely B. Floriano, Sunil Koovakat, Sabine Schlyer, Nagarajan Vaidehi, Laura Dunning, James M. Fox, Ravinder Abrol, Filipa Lopes de Mendonça, James E. Pease, Rene J. Trabanino, Monica Kochanny, Meina Liang, William A. Goddard, Shantanu Sharma
Publikováno v:
The Journal of biological chemistry. 281(37)
A major challenge in the application of structure-based drug design methods to proteins belonging to the superfamily of G protein-coupled receptors (GPCRs) is the paucity of structural information (1). The 19 chemokine receptors, belonging to the Cla
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af53fcebb2f9c3de7d4ee6314190994b
https://pubmed.ncbi.nlm.nih.gov/16837468
https://pubmed.ncbi.nlm.nih.gov/16837468