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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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

Author(s): E. Matteucci and O. Giampietro

Volume 18, Issue 31, 2011

Page: [4753 - 4760] Pages: 8

DOI: 10.2174/092986711797535290

Price: $65


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, molecular mechanisms, dipeptidyl, peptidase-4, hypoglycaemia, biological activity, hormones, neuropeptides, cytokines, clinical studies

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