Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Jean Labrecque"'
Autor:
Sidharth Gupta, Alexandros A. Sklavounos, Joshua Dahmer, Anthony K.C. Yong, Mohammed A. A. Abdullah, Gilberto Camacho, Keith Morton, Matthew Shiu, Jean Labrecque, Teodor Veres, Aaron R. Wheeler, Alex Mariakakis
Publikováno v:
2022 IEEE International Conference on Pervasive Computing and Communications Workshops and other Affiliated Events (PerCom Workshops).
Publikováno v:
Journal of Biological Chemistry. 290:11041-11051
The chemokine receptors CCR5 and CCR2b share 89% amino acid homology. CCR5 is a co-receptor for HIV and CCR5 antagonists have been investigated as inhibitors of HIV infection. We describe the use of two CCR5 antagonists, Schering-C (SCH-C), which is
Autor:
Dana Huskens, Marilyn C. Darkes, Gary Bridger, Jennifer H. Cox, Simon P. Fricker, Zefferino Santucci, Renee Mosi, Jean Labrecque, Kim L. Nelson, Renato Skerlj, Stefan R. Idzan, Virginia Anastassova, Dominique Schols, Ketan Patel, Rebecca S.Y. Wong, Gloria Lau
Publikováno v:
Biochemical Pharmacology. 83:472-479
In order to enter and infect human cells HIV must bind to CD4 in addition to either the CXCR4 or the CCR5 chemokine receptor. AMD11070 was the first orally available small molecule antagonist of CXCR4 to enter the clinic. Herein we report the molecul
Autor:
Zefferino Santucci, Gary Bridger, Gloria Lau, Dominique Schols, Elyse Bourque, Wen Yang, Simon P. Fricker, Markus Metz, Curtis Harwig, Marilyn C. Darkes, Renato T. Skerlj, Jonathan Langille, Jean Labrecque, Sanjay Danthi
Publikováno v:
Journal of the American Chemical Society. 133:16477-16485
The viral resistance of marketed antiviral drugs including the emergence of new viral resistance of the only marketed CCR5 entry inhibitor, maraviroc, makes it necessary to develop new CCR5 allosteric inhibitors. A mutagenesis/modeling approach was u
Autor:
Tong-Shuang Li, Simon P. Fricker, Gang Chen, Renato Skerlj, David Bogucki, Markus Metz, Gary Bridger, Susan Nan, Rebecca S.Y. Wong, Dominique Schols, Jean Labrecque, Gloria Lau, Marilyn C. Darkes, Bryon Carpenter
Publikováno v:
Virology. 413(2):231-243
Based on the attrition rate of CCR5 small molecule antagonists in the clinic the discovery and development of next generation antagonists with an improved pharmacology and safety profile is necessary. Herein, we describe a combined molecular modeling
Autor:
Renato Skerlj, Gary Bridger, Yuanxi Zhou, Elyse Bourque, Jonathan Langille, Maria Di Fluri, David Bogucki, Wen Yang, Tongshuang Li, Letian Wang, Susan Nan, Ian Baird, Markus Metz, Marilyn Darkes, Jean Labrecque, Gloria Lau, Simon Fricker, Dana Huskens, Dominique Schols
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2450-2455
A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of CCR5 (RANTES) binding and these compounds exhibited potent inhibition of R5 HIV-1 replication in peripheral blood mo
Autor:
Ling Qin, Rebecca Wong, Virginia Anastassov, Simon P. Fricker, Jennifer H. Cox, Renee Mosi, Stefan R. Idzan, Jean Labrecque, Kim L. Nelson, Ognjen Grujic, Gloria Lau, Marilyn C. Darkes, Zeffy Santucci
Publikováno v:
Biochemical Pharmacology. 72:588-596
The chemokine receptor CXCR4 is widely expressed on different cell types, is involved in leukocyte chemotaxis, and is a co-receptor for HIV. AMD3100 has been shown to be a CXCR4 receptor antagonist, and to block HIV infection of T-tropic, X4-using, v
Autor:
Pierre-André Fournier, Leanne Bedard, Jeffrey S. Albert, Jean Labrecque, Frederic Vallee, Sébastien Laliberté
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(14)
We describe the discovery and advancement of a novel series of TRPA1 antagonist having an aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamide scaffold. The physical and in vitro DMPK profiles are discussed.
Autor:
Frederic Vallee, Jean Labrecque, Leanne Bedard, Jeffrey S. Albert, Sébastien Laliberté, Shujuan Jin, Yun-Jin Hu, Miguel St.-Onge
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(14)
A series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and favorable physical properties and may thus serve as scaffolds for further opt
Publikováno v:
Journal of Biological Chemistry. 274:9752-9759
Natriuretic peptide receptor-A (NPR-A), a particulate guanylyl cyclase receptor, is composed of an extracellular domain (ECD) with a ligand binding site, a transmembrane spanning, a kinase homology domain (KHD), and a guanylyl cyclase domain. Atrial