CCR5 pharmacology methodologies and associated applications.

摘要: Abstract The G protein–coupled chemokine (C‐C motif) receptor, CCR5, was originally characterized as a protein responding functionally to number of CC chemokines. As with receptors in general, studies indicate that CCR5 plays role inflammatory responses infection, although its exact normal immune function is not completely defined. vast majority research into has been focused on an essential and predominant coreceptor for HIV‐1 entry host cells. Discovery this prompted by the elucidation individuals homozygous 32 bp deletion gene do express receptor at cell surface, consequence, are remarkably resistant apparently possess no other clear phenotype. Multiple followed ultimate aim identifying drugs physically blocked prevent entry, thus provide new approach treating infection AIDS, world's biggest infectious disease killer. To end, functional antagonists potent anti–HIV‐1 activity have discovered, best exemplified maraviroc, first oral drug treatment 10 years. In chapter, specific methods used characterize primary pharmacology apply data generated enable discovery, notably HIV potentially inflammatory‐based indications, described.