Inferences from the ADME analysis of predicted inhibitors to DPPIV

Author(s): Kanchanamala P.*, Srinivasa Rao P., Appa Rao Allam, Rama Narasinga Rao Manda

Abstract

The incretin hormone glucagon-like peptide 1 (GLP-1) stimulates insulin biosynthesis and secretion, and inhibits glucagon release in a glucose-dependent manner. However, active GLP-1 is rapidly degraded in vivo through the action of dipeptidyl peptidase IV (DPP-4), a serine protease that cleaves a dipeptide from the N-terminus to give the inactive GLP-1 amide. Small-molecule inhibitors of DPP-4 have been shown to prolong the beneficial effects of this incretin hormone. The interactions between the DPPIV and their corresponding receptors are highly selective. Therefore, the structure of this protein was screened using molecular docking techniques. This exercise indentified compounds with better binding and ADME (Absorption, Digestion, Metabolism, and Excretion) properties compared to known standard compounds. These observations find application for the consideration of such compounds for further validation towards inhibiting DPPIV.

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