CCR5
CCR5 is a human CC chemokine receptor and G protein-coupled receptor that responds to chemokines including RANTES/CCL5, MIP-1α/CCL3, and MIP-1β/CCL4[1]. Mechanistically, ligand-bound CCR5 couples to Gᵢ1 and supports chemokine recognition, receptor activation, immune surveillance, and inflammation[2]. In HIV research models, CCR5 functions as the principal cofactor for entry mediated by envelope glycoproteins of primary macrophage-tropic HIV-1 strains[3]. CCR5, when coexpressed with CD4, enables infection by most primary HIV-1 isolates, whereas CCR3 supports only a more restricted subset, defining an experimentally important distinction from related chemokine receptors[4]. A homozygous CCR5 defect was identified in some multiply exposed individuals resistant to HIV-1 infection, linking receptor expression to viral-entry susceptibility[5]. Compared with related isoforms CCR1 and CCR3, natural LD78β/MIP-1α isoforms show diverging binding capacities that affect CCR5-linked anti-HIV activity and CCR1/CCR3-linked chemotactic responses. For inhibitor studies, maraviroc-bound CCR5 reveals a ligand-binding site distinct from chemokine and gp120 recognition sites, supporting allosteric inhibition of chemokine signaling and viral entry[6]. Maraviroc is a CCR5 antagonist used to block gp120 interaction with CCR5 in HIV/AIDS research and treatment contexts[7].
References:
- [1]. Samson M, et al. Molecular cloning and functional expression of a new human CC-chemokine receptor gene. Biochemistry. 1996 Mar 19;35(11):3362-7. [Content Brief]
- [2]. Zhang H, et al. Structural basis for chemokine recognition and receptor activation of chemokine receptor CCR5. Nat Commun. 2021 Jul 6;12(1):4151. [Content Brief]
- [3]. Deng H, et al. Identification of a major co-receptor for primary isolates of HIV-1. Nature. 1996 Jun 20;381(6584):661-6. [Content Brief]
- [4]. Choe H, et al. The beta-chemokine receptors CCR3 and CCR5 facilitate infection by primary HIV-1 isolates. Cell. 1996 Jun 28;85(7):1135-48. [Content Brief]
- [5]. Liu R, et al. Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection. Cell. 1996 Aug 9;86(3):367-77. [Content Brief]
- [6]. Tan Q, et al. Structure of the CCR5 chemokine receptor-HIV entry inhibitor maraviroc complex. Science. 2013 Sep 20;341(6152):1387-90. [Content Brief]
- [7]. Xu GG, et al. Chemokine receptor CCR5 antagonist maraviroc: medicinal chemistry and clinical applications. Curr Top Med Chem. 2014;14(13):1504-14. [Content Brief]
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CCR5 Related Products (31)
Related Products (31)
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Recombinant Proteins (5)
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PNU-177864
0 ImagesCat. No.: HY-103406CAS No.: 250266-51-4PNU-177864 is a potent, selective, orally active dopamine D3 receptor antagonist. PNU-177864 induces phospholipid metabolism in vivo and has anti-schizophrenia activity.
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CCR5 antagonist 2
0 ImagesCat. No.: HY-152131CAS No.: 1800570-93-7CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC50 of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities.
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CCR5 antagonist 1
0 ImagesCat. No.: HY-100261CAS No.: 716354-86-8CCR5 antagonist 1 is a CCR5 antagonist which can inhibit HIV replication extracted from WO 2004054974 A2.
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PF-4178903
0 ImagesCat. No.: HY-119658CAS No.: 1310796-72-5Synonyms: INCB10820
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CB-0821
0 ImagesCat. No.: HY-162512CAS No.: 81430-62-8
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Ophiobolin C
0 ImagesCat. No.: HY-123902CAS No.: 19022-51-6Synonyms: Zizanin AOphiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells. Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells.
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E913
0 ImagesCat. No.: HY-118962CAS No.: 342394-93-8E913 is a CCR5 antagonist that competes with the binding of antibodies to CCR5 which recognize the C-terminal half of the second extracellular loop (ECL2B) of CCR5. E913 can specifically block the binding of macrophage inflammatory protein-1alpha (MIP-1alpha) to CCR5 (IC50 = 0.002 μM) and MIP-1alpha-elicited cellular Ca2+ mobilization (IC50 = 0.02 μM). E913 inhibits the replication of laboratory and primary R5 HIV-1 strains as well as various multidrug-resistant monocyte/macrophage tropic (R5) HIV-1 (IC50 = 0.03-0.06 μM). E913 can be used for the research of infection, such as HIV-1 infection.
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