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Tag Archives: gpcr
GPCR structure and modeling
A recently published letter from scientists at Boehringer Ingelheim nicely summarizes recent advances in our understanding of G protein-coupled receptor (GPCR) structure and function. X-ray structures of the inactive forms of bovine rhodopsin (2000), β2 adrenergic receptor (2007 – with antibody … Continue reading
Discovery of PF-232798 (CCR5 Antagonist)
CCR5 antagonists prevent entry of HIV into host cells by binding to the CCR5 co-receptor and stopping the gp120-CD4 complex from making the crucial interaction with CCR5 that leads to fusion of the viral and host cell membranes (see Wikipedia article … Continue reading
Posted in Clinical Candidates, GPCR ligands
Tagged absorption, animal PK, antagonist, anti-viral, caco-2, CCR5, CYP450, fluorine, gp120, gpcr, hERG, HIV, logD, Maraviroc, PF-232798, Pfizer, Phase I, Phase II
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