PMID- 26075286 OWN - NLM STAT- MEDLINE DCOM- 20160203 LR - 20240324 IS - 2314-6753 (Electronic) IS - 2314-6745 (Print) VI - 2015 DP - 2015 TI - The Place of Dipeptidyl Peptidase-4 Inhibitors in Type 2 Diabetes Therapeutics: A "Me Too" or "the Special One" Antidiabetic Class? PG - 806979 LID - 10.1155/2015/806979 [doi] LID - 806979 AB - Incretin-based therapies, the most recent therapeutic options for type 2 diabetes mellitus (T2DM) management, can modify various elements of the disease, including hypersecretion of glucagon, abnormal gastric emptying, postprandial hyperglycaemia, and, possibly, pancreatic beta cell dysfunction. Dipeptidyl peptidase-4 (DPP-4) inhibitors (gliptins) increase glucagon-like peptide-1 (GLP-1) availability and correct the "incretin defect" seen in T2DM patients. Clinical studies have shown good glycaemic control with minimal risk of hypoglycaemia or any other adverse effects, despite the reports of pancreatitis, whose association remains to be proved. Recent studies have been focusing on the putative ability of DPP-4 inhibitors to preserve pancreas function, in particular due to the inhibition of apoptotic pathways and stimulation of beta cell proliferation. In addition, other cytoprotective effects on other organs/tissues that are involved in serious T2DM complications, including the heart, kidney, and retina, have been increasingly reported. This review outlines the therapeutic potential of DPP-4 inhibitors for the treatment of T2DM, focusing on their main features, clinical applications, and risks, and discusses the major challenges for the future, in particular the possibility of becoming the preferred therapy for T2DM due to their ability to modify the natural history of the disease and ameliorate nephropathy, retinopathy, and cardiovascular complications. FAU - Godinho, Ricardo AU - Godinho R AD - Laboratory of Pharmacology and Experimental Therapeutics, Institute for Biomedical Imaging and Life Sciences (IBILI), Faculty of Medicine, Coimbra University, 3000-548 Coimbra, Portugal. FAU - Mega, Cristina AU - Mega C AUID- ORCID: 0000-0002-9913-875X AD - Laboratory of Pharmacology and Experimental Therapeutics, Institute for Biomedical Imaging and Life Sciences (IBILI), Faculty of Medicine, Coimbra University, 3000-548 Coimbra, Portugal ; ESAV, Polytechnic Institute of Viseu, 3504-510 Viseu, Portugal. FAU - Teixeira-de-Lemos, Edite AU - Teixeira-de-Lemos E AUID- ORCID: 0000-0002-6346-8319 AD - Laboratory of Pharmacology and Experimental Therapeutics, Institute for Biomedical Imaging and Life Sciences (IBILI), Faculty of Medicine, Coimbra University, 3000-548 Coimbra, Portugal ; ESAV, Polytechnic Institute of Viseu, 3504-510 Viseu, Portugal. FAU - Carvalho, Eugenia AU - Carvalho E AD - Center for Neuroscience and Cell Biology-Institute for Biomedical Imaging and Life Sciences (CNC.IBILI) Research Unit, University of Coimbra, 3000-548 Coimbra, Portugal ; The Portuguese Diabetes Association (APDP), 1250-189 Lisbon, Portugal. FAU - Teixeira, Frederico AU - Teixeira F AD - Laboratory of Pharmacology and Experimental Therapeutics, Institute for Biomedical Imaging and Life Sciences (IBILI), Faculty of Medicine, Coimbra University, 3000-548 Coimbra, Portugal. FAU - Fernandes, Rosa AU - Fernandes R AUID- ORCID: 0000-0001-7828-2296 AD - Laboratory of Pharmacology and Experimental Therapeutics, Institute for Biomedical Imaging and Life Sciences (IBILI), Faculty of Medicine, Coimbra University, 3000-548 Coimbra, Portugal ; Center for Neuroscience and Cell Biology-Institute for Biomedical Imaging and Life Sciences (CNC.IBILI) Research Unit, University of Coimbra, 3000-548 Coimbra, Portugal. FAU - Reis, Flavio AU - Reis F AUID- ORCID: 0000-0003-3401-9554 AD - Laboratory of Pharmacology and Experimental Therapeutics, Institute for Biomedical Imaging and Life Sciences (IBILI), Faculty of Medicine, Coimbra University, 3000-548 Coimbra, Portugal ; Center for Neuroscience and Cell Biology-Institute for Biomedical Imaging and Life Sciences (CNC.IBILI) Research Unit, University of Coimbra, 3000-548 Coimbra, Portugal. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review DEP - 20150517 PL - England TA - J Diabetes Res JT - Journal of diabetes research JID - 101605237 RN - 0 (Blood Glucose) RN - 0 (Dipeptidyl-Peptidase IV Inhibitors) SB - IM MH - Blood Glucose/*metabolism MH - Diabetes Mellitus, Type 2/*drug therapy/metabolism MH - Dipeptidyl-Peptidase IV Inhibitors/*therapeutic use MH - Humans MH - Hyperglycemia/*drug therapy/metabolism MH - Insulin-Secreting Cells/metabolism PMC - PMC4449938 EDAT- 2015/06/16 06:00 MHDA- 2016/02/04 06:00 PMCR- 2015/05/17 CRDT- 2015/06/16 06:00 PHST- 2015/01/11 00:00 [received] PHST- 2015/04/09 00:00 [revised] PHST- 2015/04/11 00:00 [accepted] PHST- 2015/06/16 06:00 [entrez] PHST- 2015/06/16 06:00 [pubmed] PHST- 2016/02/04 06:00 [medline] PHST- 2015/05/17 00:00 [pmc-release] AID - 10.1155/2015/806979 [doi] PST - ppublish SO - J Diabetes Res. 2015;2015:806979. doi: 10.1155/2015/806979. Epub 2015 May 17.