CCR receptor

A systematic nomenclature has been developed for the chemokine receptors (see Table 1). Thus, receptors for CC chemokines are referred to as CCR, receptors for CXC chemokines as CXCR, and the receptors for the XC and CX3C chemokines as XCR and CX3CR, respectively. To date, there are 10 CCRs (CCRs 1 to 10), 7 CXCRs, a single XCR, and a single CX3CR. The numbering is based on the date of deposition of the chemokine receptor sequence within the nucleic acid databases. For orphan receptors, this date refers to the point of identification of the orphan receptors as chemokine receptors and not to the date of initial deposition in the cDNA databases. 

Burrows, J.N. et al. (2005) Modulators of the human CCRS receptor. Part 1 Discovery and initial SAR of l-(3,3-diphenylpropyl)-piperidinyl amides and... 

Ma, D. et al. (2007) Synthesis and biological evaluation of 1,3,3,4-tetrasubstituted pyrrolidine CCRS receptor antagonists. Discovery of a potent and orally hioavailahle anti-HIV agent. ChemMedChem, 2 (2), 187-193. 

Cagnon, L., and Rossi, J. J. (2000). Down regulation of the CCRS beta-chemokine receptor and inhibition of HIV-1 infection by stable VAl-ribozyme chimeric transcripts. Antisen. Nuc. A. Drug Dev. 10 251—261. 

Samson M, Libert F, Doranz BJ, Rucker J, Liesnard C, Farber C-M, Saragosti S, Lapoumeroulie C, Cognaux J, Forceille C, Muyldermans G, Verhofstede C, Burtonboy G, Georges M, Imai T, Rana S, Yi Y, Smyth RJ, Collman RG, Dorns RW, Vassart G, Parmentier M (1996) Resistance to HIV-1 infection in Caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene. Nature 382 722-725... 

Reeves ID, McKnight A, Potempa S et al (1997) CD4-independent infection by HlV-2 (ROD/B) use of the 7-transmembrane receptors CXCR-4, CCR-3, and V28 for entry. Virology 231 130-134 Ribeiro JA (2005) What can adenosine neuromodulation do for neuroprotection Curr Drug Targets CNS Neurol Disord 4 325-329... 

Luttichau HR, Stine J, Boesen TP, et al. A highly selective CC chemokine receptor (CCR)8 antagonist encoded by the poxvirus molluscum contagiosum. J Exp Med 2000 191 171-80. 

Aramori I, Ferguson SS, Bieniasz PD, Zhang J, Cullen B, Cullen MG. Molecular mechanism of desensitization of the chemokine receptor CCR-5 receptor signaling... 

Zuurman MW, Heeroma J, Brouwer N, Boddeke UW, Biber K. LPS-induced expression of a novel chemokine receptor (L-CCR) in mouse glial cells in vitro and in vivo. Glia 2003 41 327-336. 

Reiss Y, Proudfoot AE, Power CA, Campbell JJ, Butcher EC. CC chemokine receptor (CCR)4 and the CCR10 ligand cutaneous T cell-attracting chemokine (CTACK) in lymphocyte trafficking to inflamed skin. J Exp Med 2001 194 1541-1547. 

Zamarchi R, Allavena P, Borsetti A, et al. Expression and functional activity of CXCR-4 and CCR-5 chemokine receptors in human thymocytes. Clin Exp Immunol... 

Anders HJ, Vielhauer V, Frink M, et al. A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation. J Clin Invest 2002 109 251-259. 

Sato N, Ahuja SK, Quinones M, et al. CC chemokine receptor (CCR)2 is required for langerhans cell migration and localization of T helper cell type 1 (Thl)-inducing dendritic cells. Absence of CCR2 shifts the Leishmania major-resistant phenotype to a susceptible state dominated by Th2 cytokines, b cell outgrowth, and sustained neutrophilic inflammation. J Exp Med 2000 192(2) 205-218. 

Quinones MP, Jimenez F, Martinez H, et al. CC chemokine receptor (CCR)-2 prevents arthritis development following infection by Mycobacterium avium. J Mol Med 2006 84(6) 503-512. 

Lloyd CM, Delaney T, Nguyen T, et al. CC chemokine receptor (CCR)3/eotaxin is followed by CCR4/monocyte-derived chemokine in mediating pulmonary T helper lymphocyte type 2 recruitment after serial antigen challenge in vivo. J Exp Med 2000 191(2) 265-274. 

Harriman, G.C.B., Carson, K.G., Flynn, D.L.,e al. (2002) Preparation of functionalized indoles, benzimida-zolones and related heterocycles as modulators of CCR-5 chemokine receptor and use in treating patients with HIV. WO, 2002072549. 

Samson M, Libert F, Doranz BJ, Rucker J, Liesnard C, Farber CM et al. Resistance to HIV-1 infection in Caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene. Nature 1996 382 722-725. 

The trCCR experiment has been apphed to study the boimd conformation of a nucleotide analog bound to Elongation Factor Tu [8,23]. Measurements of the CCR-rates /hi ci C2 H2 and /h3 c3 C4 H4 of the C-labelled nucleotide in the presence of its receptor, resulted in an unambiguous determination of the sugar conformation of the nucleotide. 

Measurements of the trCCR-rate have also been applied to small pep-tidic ligands. In a proof-of-concept study we have studied the STAT-6 bound conformation of an IL-4 receptor-derived peptide [9]. For this study a chemically synthesized N/ C-labelled tetrapeptide was used in conjunction with NHCH dipole-dipole CCR and /nhc dipole-CSA CCR experiments. 

Chemokine receptors are a family of G protein-coupled receptors that contain seven transmembrane domains. Chemokine receptors are present on the cell surface membrane of leukocytes. As was the case for chemokines, these receptors are also divided into four subgroups CCR is specific for CC chemokines, CXCR for CXC chemokines, XCR1 for C chemokines and CX3CR1 for CX3C chemokines. The CC chemokine receptor family has eleven members, the CXC chemokine receptor family has seven members, and both the C chemokine receptor family and the CX3C chemokine receptor family have one member each. The signal transduction is mediated via the standard G protein-dependent pathway. 

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