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CCR5 receptor antagonists are a class of small molecules that antagonize the CCR5 receptor. The C-C motif chemokine receptor CCR5 is involved in the process by which HIV, the virus that causes AIDS, enters cells. Hence antagonists of this receptor are entry inhibitors and have potential therapeutic applications in the treatment of HIV infections.
The life cycle of the HIV presents potential targets for drug therapy, one of them being the viral entry pathway. CCR5 and CXCR4 are the main receptors involved in the HIV entry process. These receptors belong to the seven transmembrane G-protein-coupled receptor (GPCR) family and are predominantly expressed on human T-cells, dendritic cells and macrophages, Langerhans cells.[1] They play an important role as co-receptors that HIV type 1 (HIV-1) uses to attach to cells before viral fusion and entry into host cells.[1] HIV isolates can be divided into R5 and X4 strains. R5 strain is when the virus uses the co-receptor CCR5 and X4 strain is when it uses CXCR4.[2] The location of CCR5 receptors at the cell surface, both large and small molecules have the potential to interfere with the CCR5-viral interaction and inhibit viral entry into human cells.[3]
^ abLederman MM, Penn-Nicholson A, Cho M, Mosier D (August 2006). "Biology of CCR5 and its role in HIV infection and treatment". JAMA. 296 (7): 815–26. doi:10.1001/jama.296.7.815. PMID 16905787.
^De Clercq E (December 2007). "The design of drugs for HIV and HCV". Nature Reviews Drug Discovery. 6 (12): 1001–18. doi:10.1038/nrd2424. PMID 18049474. S2CID 37859193.
^Pulley, Shon (2007). "CCR5 antagonists: from discovery to clinical efficacy". In Neote, Kuldeep; Letts, Gordon L.; Moser, Bernhard (eds.). Chemokine Biology — Basic Research and Clinical Application. Progress in Inflammation Research. Vol. 2. Birkhauser Basel. pp. 145–163. doi:10.1007/978-3-7643-7437-2_11. ISBN 978-3-7643-7195-1.
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