Uses
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects[1][2][3][4][5][6].
References
[1] Subramanian H, et al. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol Pharmacol. 2011 Jun;79(6):1005-13. DOI:
10.1124/mol.111.071472[2] Ting E, et al. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br J Pharmacol. 2008 Mar;153(5):1043-53. DOI:
10.1038/sj.bjp.0707640[3] Holland MC, et al. Synthetic small-molecule complement inhibitors. Curr Opin Investig Drugs. 2004 Nov;5(11):1164-73. PMID:15573867
[4] Finch AM, et al. Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J Med Chem. 1999 Jun 3;42(11):1965-74. DOI:
10.1021/jm9806594[5] Manthey HD, et al. Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J. 2011 Jul;25(7):2447-55. DOI:
10.1096/fj.10-174284[6] Vadrevu SK, et al. Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 2014 Jul 1;74(13):3454-65. DOI:
10.1158/0008-5472.CAN-14-0157
