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Design and Synthesis of Prolylcarboxypeptidase (PrCP) Inhibitors to Validate PrCP as a Potential Target for Obesity

Design and Synthesis of Prolylcarboxypeptidase (PrCP) Inhibitors to Validate PrCP as a Potential Target for Obesity

Changyou Zhou, Margareta Garcia-Calvo, Shirly Pinto, Matthew Lombardo, Zhe Feng, Kate Bender, Kellyann D Pryor, Urmi R Bhatt, Renee M Chabin, Wayne M Geissler, Zhu Shen, Xinchun Tong, Zhoupeng Zhang, Kenny K Wong, etc.

J Med Chem. 2010 Oct 14;53(19):7251-63.

PMID: 20857914

Abstract:

Prolylcarboxypeptidase (PrCP) is a serine protease that may have a role in metabolism regulation. A class of reversible, potent, and selective PrCP inhibitors was developed starting from a mechanism based design for inhibiting this serine protease. Compound 8o inhibits human and mouse PrCP at IC(50) values of 1 and 2 nM and is not active (IC(50) > 25 μM) against a panel of closely related proteases. It has lower serum binding than its close analogues and is bioavailable in mouse. Subchronic dosing of 8o in PrCP(-/-) and WT mice at 100 mg/kg for 5 days resulted in a 5% reduction in body weight in WT mice and a 1% reduction in PrCP KO mice.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR4241391	PrCP active human			Price

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