Target Validation Information
TTD ID	T10965
Target Name	P-selectin (SELP)
Type of Target	Successful
Drug Potency against Target	RPSGL-Ig	Drug Info	IC50 = 10 uM	[3]
	2,3,4-trihydroxybenzoic acid	Drug Info	IC50 = 11800 nM	[1]
	GALLICACID	Drug Info	IC50 = 19100 nM	[1]
Action against Disease Model	RPSGL-Ig	Drug Info	In mixed neutrophil/platelet suspensions, the percentage of neutrophils that bind platelets increased significantly , from 10.8 +/- 1.6% at baseline to 39.7 +/- 2.9% (P < 0.05) after perfusion over damaged arteries compared with 69.7 +/- 2.5% with thrombin. This binding was completely inhibited by a recombinant soluble PSGL-1 (rPSGL-Ig) and anti-P-selectin and PSGL-1-blocking monoclonal antibodies. The inhibitory effect of rPSGL-Ig correlated well with its binding to platelets (r = 0.98, P < 0.001). Circulating platelets are activated upon contact with damaged arteries, thereby enhancing their adhesive interactions with neutrophils via P-selectin and PSGL-1. Inhibition of this binding with rPSGL-Ig may constitute a target in the treatment of inflammatory and thrombotic reactions.	[2]
References
REF 1	Rational design of novel, potent small molecule pan-selectin antagonists. J Med Chem. 2007 Mar 22;50(6):1101-15.
REF 2	Prevention of experimental choroidal neovascularization with intravitreal anti-vascular endothelial growth factor antibody fragment. Arch Ophthalmol. 2002 Mar;120(3):338-46.
REF 3	Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] i... J Pharmacol Exp Ther. 2008 Feb;324(2):497-506.

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