CCR5 receptor

FIGURE 3.12 Dependence of constitutive receptor activity as ordinates (expressed as a percent of the maximal response to a full agonist for each receptor) versus magnitude of receptor expression (expressed as the amount of human cDNA used for transient transfection, logarithmic scale) in Xenopus laevis melanophores. Data shown for human chemokine CCR5 receptors (open circles), chemokine CXCR receptors (filled triangles), neuropeptide Y type 1 receptors (filled diamonds), neuropeptide Y type 2 receptors (open squares), and neuropeptide Y type 4 receptors (open inverted triangles). Data recalculated and redrawn from [27],... 

FIGURE 7.3 Diversity of structures that interact with the (a) HIV reverse transcriptase inhibitor binding site [8] and (b) the CCR5 receptor mediating HIV-1 fusion [9],... 

Watson, C., Jenkinson, S., Kazmierski,W., and Kenakin, T. P. (2005). The CCR5 receptor-based mechanism of action of 873140, a potent allosteric non-competitive HIV entry-inhibitor. Mol. Pharmacol. 67 1268—1282. 

Finke, P. E., Oates, B., Mills, S. G., MacCoss, M., Malkowitz, L., Springer, M. S., Gould, S. L., DeMartino, J. A., Carella, A. Carver, G., et al. (2001). Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4 synthesis and structure—Activity relationships for l-[7V-(Methyl)-7V-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(7V-(alkyl)-7V-(benzylox-ycarbonyl)amino)piperidin-l-yl)butanes. Bioorg. Med. Chem. Lett. 11 2475-2479. 

CCR5 receptors, 177 high-throughput screening of drugs for,... 

Wood A, Armour D (2005) The discovery of the CCR5 receptor antagonist, UK-427,857, a new agent for the treatment of HIV infection and AIDS, Prog Med Chem 43 239-271... 

Isik N, Hereld D, Jin T (2008) Fluorescence resonance energy transfer imaging reveals that chemokine-binding modulates heterodimers of CXCR4 and CCR5 receptors. PLoS ONE... 

Chao CC, Hu S, Shark KB, Sheng WS, Gekker G, Peterson PK (1997) Activation of mu opioid receptors inhibits microglial cell chemotaxis. J Pharmacol Exp Ther 281 998-1004 Chen SR, Pan HL (2006) Blocking mu opioid receptors in the spinal cord prevents the analgesic action by subsequent systemic opioids. Brain Res 1081 119-125 Chen C, Li J, Bot G, Szabo I, Rogers TJ, Liu-Chen LY (2004) Heterodimerization and crossdesensitization between the mu-opioid receptor and the chemokine CCR5 receptor. Eur J Pharmacol 483 175-186... 

In another example from the literature [40], we see a strong correlation between potency and PSA. In this case a series of 53 CCR5 receptor agonists have been... 

Vila-Coro AJ, Mellado M, Martin de Ana A, et al. HIV-1 infection through the CCR5 receptor is blocked by receptor dimerization. Proc Natl Acad Sci U S A 2000 97(7) 3388-3393. 

Cooke SP, Forrest G, Venables PJ, Hajeer A. The delta32 deletion of CCR5 receptor in rheumatoid arthritis. Arthritis Rheum 1998 41(6) 1135-1136. 

Karlsson I, Antonsson L, Shi Y, et al. Coevolution of RANTES sensitivity and mode of CCR5 receptor use by human immunodeficiency virus type 1 of the R5 phenotype. J Virol 2004 78(21) 11807-11815. 

Ditzel HI, Rosenkilde MM, Garred P, et al. The CCR5 receptor acts as an alloantigen in CCR5Delta32 homozygous individuals identification of chemokine and HIV-1-blocking human antibodies. Proc Natl Acad Sci U S A 1998 95 5241-5245. 

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