Pharmacology of AMD3465: A small molecule antagonist of the chemokine receptor CXCR4

2009 ◽  
Vol 78 (8) ◽  
pp. 993-1000 ◽  
Author(s):  
Veronique Bodart ◽  
Virginia Anastassov ◽  
Marilyn C. Darkes ◽  
Stefan R. Idzan ◽  
Jean Labrecque ◽  
...  
Keyword(s):  
Small Molecule ◽  
Chemokine Receptor ◽  
Small Molecule Antagonist ◽  
Chemokine Receptor Cxcr4

scholarly journals A Small-molecule Inhibitor Directed against the Chemokine Receptor CXCR4 Prevents its Use as an HIV-1 Coreceptor

1997 ◽  
Vol 186 (8) ◽  
pp. 1395-1400 ◽  
Author(s):  
Benjamin J. Doranz ◽  
Kathie Grovit-Ferbas ◽  
Matthew P. Sharron ◽  
Si-Hua Mao ◽  
Matthew Bidwell Goetz ◽  
...  
Keyword(s):  
Membrane Fusion ◽  
Small Molecule ◽  
Chemokine Receptor ◽  
Viral Entry ◽  
Small Molecule Inhibitor ◽  
Chemokine Receptor Cxcr4 ◽  
Mechanism Of Inhibition ◽  
Molecule Inhibitor ◽  
Immunodeficiency Virus ◽  
Hiv 1

The chemokine receptor CXCR4 is the major coreceptor used for cellular entry by T cell– tropic human immunodeficiency virus (HIV)-1 strains, whereas CCR5 is used by macrophage (M)-tropic strains. Here we show that a small-molecule inhibitor, ALX40-4C, inhibits HIV-1 envelope (Env)-mediated membrane fusion and viral entry directly at the level of coreceptor use. ALX40-4C inhibited HIV-1 use of the coreceptor CXCR4 by T- and dual-tropic HIV-1 strains, whereas use of CCR5 by M- and dual-tropic strains was not inhibited. Dual-tropic viruses capable of using both CXCR4 and CCR5 were inhibited by ALX40-4C only when cells expressed CXCR4 alone. ALX40-4C blocked stromal-derived factor (SDF)-1α–mediated activation of CXCR4 and binding of the monoclonal antibody 12G5 to cells expressing CXCR4. Overlap of the ALX40-4C binding site with that of 12G5 and SDF implicates direct blocking of Env interactions, rather than downregulation of receptor, as the mechanism of inhibition. Thus, ALX40-4C represents a small-molecule inhibitor of HIV-1 infection that acts directly against a chemokine receptor at the level of Env-mediated membrane fusion.

Small molecule antagonist of C-C chemokine receptor 1 (CCR1) reduces disc inflammation in the rabbit model

2020 ◽  
Vol 20 (12) ◽  
pp. 2025-2036
Author(s):  
Po-Hsin Chou ◽  
Ana Chee ◽  
Peng Shi ◽  
Cheng-Li Lin ◽  
Yibo Zhao ◽  
...  
Keyword(s):  
Small Molecule ◽  
Chemokine Receptor ◽  
Rabbit Model ◽  
Small Molecule Antagonist ◽  
Chemokine Receptor 1

Pharmacological Characterization of CXC Chemokine Receptor 3 Ligands and a Small Molecule Antagonist

2005 ◽  
Vol 313 (3) ◽  
pp. 1263-1271 ◽  
Author(s):  
Christopher E. Heise ◽  
Anil Pahuja ◽  
Sarah C. Hudson ◽  
Monica S. Mistry ◽  
Amy L. Putnam ◽  
...  
Keyword(s):  
Small Molecule ◽  
Chemokine Receptor ◽  
Pharmacological Characterization ◽  
Small Molecule Antagonist ◽  
Cxc Chemokine

Species selectivity of a small molecule antagonist for the CCR1 chemokine receptor

2000 ◽  
Vol 389 (1) ◽  
pp. 41-49 ◽  
Author(s):  
Meina Liang ◽  
Mary Rosser ◽  
Howard P Ng ◽  
Karen May ◽  
John G Bauman ◽  
...  
Keyword(s):  
Small Molecule ◽  
Chemokine Receptor ◽  
Small Molecule Antagonist ◽  
Species Selectivity

scholarly journals Computational analysis of the structural mechanism of inhibition of chemokine receptor CXCR4 by small molecule antagonists

2011 ◽  
Vol 236 (7) ◽  
pp. 844-850 ◽  
Author(s):  
Sameer P Kawatkar ◽  
Maocai Yan ◽  
Harsukh Gevariya ◽  
Mi Youn Lim ◽  
Steven Eisold ◽  
...  
Keyword(s):  
Small Molecule ◽  
Chemokine Receptor ◽  
Computational Analysis ◽  
Structural Mechanism ◽  
Chemokine Receptor Cxcr4 ◽  
Mechanism Of Inhibition
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