CCX832
CCX832 is an orally active molecule used as a tool compound in experimental pharmacology. It antagonises the effect of chemerin at the chemokine receptor CMKLR1 (ChemR23).[1][2][3] It is listed on the Guide to Pharmacology database as the only example of a CMKLR1 antagonist. Its chemical structure is undisclosed.[4]
History[edit]
The substance was originally developed for use as a pharmaceutical drug against inflammatory diseases by ChemoCentryx, a pharmaceutical firm based in California, in alliance with GlaxoSmithKline (GSK).[5] Development was terminated after a Phase I clinical trial in 2012.[6]
References[edit]
- ↑ Ramos-Junior, ES; Leite, GA; Carmo-Silva, CC; Taira, TM; Neves, KB; Colón, DF; da Silva, LA; Salvador, SL; Tostes, RC; Cunha, FQ; Fukada, SY (28 December 2016). "Adipokine Chemerin Bridges Metabolic Dyslipidemia and Alveolar Bone Loss in Mice". Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research. doi:10.1002/jbmr.3072. PMID 28029186.
- ↑ Kennedy, AJ; Yang, P; Read, C; Kuc, RE; Yang, L; Taylor, EJ; Taylor, CW; Maguire, JJ; Davenport, AP (14 October 2016). "Chemerin Elicits Potent Constrictor Actions via Chemokine-Like Receptor 1 (CMKLR1), not G-Protein-Coupled Receptor 1 (GPR1), in Human and Rat Vasculature". Journal of the American Heart Association. 5 (10): e004421. doi:10.1161/JAHA.116.004421. PMC 5121526. PMID 27742615.
- ↑ Darios, ES; Winner, BM; Charvat, T; Krasinksi, A; Punna, S; Watts, SW (1 August 2016). "The adipokine chemerin amplifies electrical field-stimulated contraction in the isolated rat superior mesenteric artery". American journal of physiology. Heart and circulatory physiology. 311 (2): H498–507. PMID 27371688.
- ↑ "Chemerin receptor – IUPHAR/BPS Guide to Pharmacology". www.guidetopharmacology.org. Retrieved 7 April 2017.
- ↑ "ChemoCentryx Identifies Novel Small Molecule ChemR23 Antagonist for the Treatment of Inflammatory Diseases". ChemoCentryx. 2010-04-10.
- ↑ "ChemoCentryx, GSK discontinue ChemR23 antagonist". BioCentury. 7 February 2012.
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