Small molecule antagonists of the chemokine receptor CCR5.
This review will focus on the discovery and clinical development of small molecule antagonists of CCR5 for the treatment of HIV-1/AIDS, as well as for the potential treatment of inflammatory diseases. In particular, we will focus on the specific medicinal chemistry problems that were faced during the discovery of the molecules. We will also describe limited data from clinical development phases focusing on specific issues that arose during the clinical trials. Finally, we will touch on the mechanism of action of CCR5 antagonists.
Lemoine
Rémy C
RC
Medicinal Chemistry, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304 USA. remy.lemoine@roche.com
Wanner
Jutta
J
D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology*; D065100:CCR5 Receptor Antagonists; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008970:Molecular Weight
D000894:Anti-Inflammatory Agents, Non-Steroidal; D065100:CCR5 Receptor Antagonists