Discovery of a potent peptidic cyclophilin A inhibitor Trp-Gly-Pro.

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Pang X, Zhang M, Zhou L, Xie F, Lu H, He W, Jiang S, Yu L, Zhang X

Discovery of a potent peptidic cyclophilin A inhibitor Trp-Gly-Pro.

Eur J Med Chem. 2011 May;46(5):1701-5. doi: 10.1016/j.ejmech.2011.02.023. Epub 2011 Feb 22.

PubMed ID

21396746 [ View in PubMed

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Abstract

Through virtual screening of a rationally built database consisting of 40 peptides, we identified three short peptides. After testing these three synthetic peptides, we found that the peptide Trp-Gly-Pro (WGP) showed comparable inhibitory ability as positive control cyclosporine A (CsA) on CypA-mediated PPIase activity with IC50 values of 33.11 nM and 10.25 nM, respectively. The peptide WGP had same order of CypA-binding affinity as CsA with dissociation equilibrium constant KD of 3.41x10(-6) and 6.42x10(-6) M, respectively. This peptide could also inhibit HIV-1IIIB infection. This study provides a novel strategy for rational design and development of peptidic drugs.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Cyclosporine	Peptidyl-prolyl cis-trans isomerase A	IC 50 (nM)	10.25	N/A	N/A	Details
Cyclosporine	Peptidyl-prolyl cis-trans isomerase A	Kd (nM)	6420	N/A	N/A	Details