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Dipeptidyl Peptidase-4 Inhibition: Linking Chemical Properties to Clinical Safety

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The new drug class of dipeptidyl peptidase-4 (DPP4) inhibitors has been widely accepted in the daily management of type 2 diabetes since its strategic advantages with regard to body weight, risk of hypoglycaemia, and beta cell survival. We have previously evaluated the theoretical implications of DPP4 inhibition given that the enzyme is involved in regulating biological activity of hormones, neuropeptides, and cytokines. We intend now 1) to provide a critical appraisal of safety and tolerability as they emerged from the available clinical studies, and 2) to establish, if possible, a relation between chemical properties, biological activity, and the observed side effects in vivo.

Keywords: DPP4 inhibitors; adverse effects; biological activity; clinical studies; cytokines; dipeptidyl; hormones; hypoglycaemia; molecular mechanisms; neuropeptides; peptidase-4

Document Type: Research Article


Publication date: November 1, 2011

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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