title: CCR5 chemokine receptors: gatekeepers of HIV-1 infection.
abstract: With the discovery that CCR5 is the critical protein required for infection by M-tropic HIV, has come huge research efforts, both in academia and industry, to try to exploit this finding. Thus, research advances in the fields of virology, structural protein chemistry, and receptor pharmacology have combined to add a new understanding to the process of HIV fusion and possible mechanisms to prevent HIV entry. This review will approach this field from a receptor pharmacology viewpoint and outline some concepts of receptor allosterism and protein-protein interaction which may be relevant to CCR5 blockade. Many of these ideas may be explored in a practical sense with the advent of new small molecule CCR5 inhibitors currently entering the clinic.
authors.affiliation: Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA.
authors.forename: Wieslaw M
authors.initials: WM
authors.lastname: Kazmierski
authors.forename: Larry
authors.initials: L
authors.lastname: Boone
authors.forename: Wendell
authors.initials: W
authors.lastname: Lawrence
authors.forename: Chris
authors.initials: C
authors.lastname: Watson
authors.forename: Terry
authors.initials: T
authors.lastname: Kenakin
mesh_terms: D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy*; D019380:Anti-HIV Agents / Q000494:pharmacology*; D065100:CCR5 Receptor Antagonists; D019281:Dimerization; D004705:Endocytosis; D015497:HIV-1 / Q000187:drug effects*; D019713:Receptors, CCR5 / Q000737:chemistry / Q000378:metabolism; D014759:Viral Envelope Proteins / Q000378:metabolism
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D019713:Receptors, CCR5; D014759:Viral Envelope Proteins