Mechanism of action of inhibitors of dipeptidyl-peptidase-4 (DPP-4)

Nancy A. Thornberry1, Baptist Gallwitz2
1Department of Metabolic Disorders, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USA
2Department of Medicine IV, Eberhard-Karls-University, Otfried-Müller-Str. 10, 72076 Tübingen, Germany

Tóm tắt

Từ khóa


Tài liệu tham khảo

Mest, 2005, Dipeptidyl peptidase inhibitors as new drugs for the treatment of type 2 diabetes, Diabetologia, 48, 616, 10.1007/s00125-005-1707-5

Mentlein, 1999, Dipeptidyl-peptidase IV (CD26)–role in the inactivation of regulatory peptides, Regulatory Peptides, 85, 9, 10.1016/S0167-0115(99)00089-0

Gault, 2002, Evidence that the major degradation product of glucose-dependent insulinotropic polypeptide, GIP(3–42), is a GIP receptor antagonist in vivo, The Journal of Endocrinology, 175, 525, 10.1677/joe.0.1750525

Knudsen, 1996, Glucagon-like peptide-1-(9–36) amide is a major metabolite of glucagon-like peptide-1-(7–36) amide after in vivo administration to dogs, and it acts as an antagonist on the pancreatic receptor, European Journal of Pharmacology, 318, 429, 10.1016/S0014-2999(96)00795-9

De Meester, 1999, CD26, let it cut or cut it down, Immunology Today, 20, 367, 10.1016/S0167-5699(99)01486-3

Drucker, 2006, The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes, Lancet, 368, 1696, 10.1016/S0140-6736(06)69705-5

Williams-Herman, 2008, Safety and tolerability of sitagliptin in patients with type 2 diabetes: a pooled analysis, BMC Endocrine Disorders, 8, 14, 10.1186/1472-6823-8-14

Lankas, 2005, Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9, Diabetes, 54, 2988, 10.2337/diabetes.54.10.2988

Gallwitz, 2008, Saxagliptin, a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes, IDrugs, 11, 906

Deacon, 2008, Alogliptin, a potent and selective dipeptidyl peptidase-IV inhibitor for the treatment of type 2 diabetes, Current Opinion in Investigational Drugs, 9, 402

Huttner, 2008, Safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of BI 1356, an inhibitor of dipeptidyl peptidase 4, in healthy male volunteers, Journal of Clinical Pharmacology, 48, 1171, 10.1177/0091270008323753

Ahren, 2008, Emerging dipeptidyl peptidase-4 inhibitors for the treatment of diabetes, Expert Opinion on Emerging Drugs, 13, 593, 10.1517/14728210802584126

Gallwitz, 2007, Sitagliptin: profile of a novel DPP-4 inhibitor for the treatment of type 2 diabetes, Drugs of Today (Barcelona), 43, 13, 10.1358/dot.2007.43.1.1043909

Ristic, 2006, Vildagliptin: a novel DPP-4 inhibitor with pancreatic islet enhancement activity for treatment of patients with type 2 diabetes, Drugs of Today (Barcelona), 42, 519, 10.1358/dot.2006.42.8.996570

Mentlein, 1993, Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7–36)amide, peptide histidine methionine and is responsible for their degradation in human serum, European Journal of Biochemistry, 214, 829, 10.1111/j.1432-1033.1993.tb17986.x

Kieffer, 1995, Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV, Endocrinology, 136, 3585, 10.1210/en.136.8.3585

Vilsboll, 2003, Similar elimination rates of glucagon-like peptide-1 in obese type 2 diabetic patients and healthy subjects, The Journal of Clininical Endocrinology an Metabolism, 88, 220, 10.1210/jc.2002-021053

Holst, 1998, Inhibition of the activity of dipeptidyl-peptidase IV as a treatment for type 2 diabetes, Diabetes, 47, 1663, 10.2337/diabetes.47.11.1663

Balkan, 1999, Inhibition of dipeptidyl peptidase IV with NVP-DPP728 increases plasma GLP-1 (7–36 amide) concentrations and improves oral glucose tolerance in obese Zucker rats, Diabetologia, 42, 1324, 10.1007/s001250051445

Reimer, 2002, Long-term inhibition of dipeptidyl peptidase IV improves glucose tolerance and preserves islet function in mice, European Journal of Endocrinology, 146, 717, 10.1530/eje.0.1460717

Ahren, 2002, Inhibition of dipeptidyl peptidase IV improves metabolic control over a 4-week study period in type 2 diabetes, Diabetes Care, 25, 869, 10.2337/diacare.25.5.869

Marguet, 2000, Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26, Proceedings of the National Academy of Sciences of the United States of America, 97, 6874, 10.1073/pnas.120069197

Conarello, 2003, Mice lacking dipeptidyl peptidase IV are protected against obesity and insulin resistance, Proceedings of the National Academy of Sciences of the United States of America, 100, 6825, 10.1073/pnas.0631828100

Hansotia, 2004, Double incretin receptor knockout (DIRKO) mice reveal an essential role for the enteroinsular axis in transducing the glucoregulatory actions of DPP-IV inhibitors, Diabetes, 53, 1326, 10.2337/diabetes.53.5.1326

De Meester, 2000, Natural substrates of dipeptidyl peptidase IV, Advances in Experimental Medicine and Biology, 477, 67, 10.1007/0-306-46826-3_7

Sedo, 2001, Dipeptidyl peptidase IV-like molecules: homologous proteins or homologous activities?, Biochimica et Biophysica Acta, 1550, 107, 10.1016/S0167-4838(01)00278-3

Abbott, 2000, Cloning, expression and chromosomal localization of a novel human dipeptidyl peptidase (DPP) IV homolog, DPP8, European Journal of Biochemistry, 267, 6140, 10.1046/j.1432-1327.2000.01617.x

Ajami, 2004, Dipeptidyl peptidase 9 has two forms, a broad tissue distribution, cytoplasmic localization and DPIV-like peptidase activity, Biochimica et Biophysica Acta, 1679, 18, 10.1016/j.bbaexp.2004.03.010

Ahren, 2008, The islet enhancer vildagliptin: mechanisms of improved glucose metabolism, International Journal of Clinical Practice. Supplement, 8, 10.1111/j.1742-1241.2007.01685.x

Pospisilik, 2003, Dipeptidyl peptidase IV inhibitor treatment stimulates beta-cell survival and islet neogenesis in streptozotocin-induced diabetic rats, Diabetes, 52, 741, 10.2337/diabetes.52.3.741

Mu, 2006, Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic beta-cell mass and function in a rodent model of type 2 diabetes, Diabetes, 55, 1695, 10.2337/db05-1602

Nathan, 2005, Intensive diabetes treatment and cardiovascular disease in patients with type 1 diabetes, New England Journal of Medicine, 353, 2643, 10.1056/NEJMoa052187

1996, The absence of a glycemic threshold for the development of long-term complications: the perspective of the Diabetes Control and Complications Trial, Diabetes, 45, 1289, 10.2337/diabetes.45.10.1289

Stratton, 2000, Association of glycaemia with macrovascular and microvascular complications of type 2 diabetes (UKPDS 35): prospective observational study, BMJ, 321, 405, 10.1136/bmj.321.7258.405

Khaw, 2001, Glycated haemoglobin, diabetes, and mortality in men in Norfolk cohort of european prospective investigation of cancer and nutrition (EPIC-Norfolk), BMJ, 322, 15, 10.1136/bmj.322.7277.15

2001, Glucose tolerance and cardiovascular mortality: comparison of fasting and 2-hour diagnostic criteria, Archives of Internal Medicine, 161, 397, 10.1001/archinte.161.3.397

Monnier, 2003, Contributions of fasting and postprandial plasma glucose increments to the overall diurnal hyperglycemia of type 2 diabetic patients: variations with increasing levels of HbA(1c), Diabetes Care, 26, 881, 10.2337/diacare.26.3.881

Gerstein, 2008, Effects of intensive glucose lowering in type 2 diabetes, New England Journal of Medicine, 358, 2545, 10.1056/NEJMoa0802743

Patel, 2008, Intensive blood glucose control and vascular outcomes in patients with type 2 diabetes, New England Journal of Medicine, 358, 2560, 10.1056/NEJMoa0802987

Holman, 2008, 10-Year follow up of intensive glucose control in type 2 diabetes, New England Journal of medicine, 359, 1577, 10.1056/NEJMoa0806470

Qi, 2008, Two-year treatment with sitagliptin and initial combination therapy of sitagliptin and metformin provides substantial and durable glycaemic control in patients with type 2 diabetes, Diabetologia, 51