Results 171 to 180 of about 12,907 (206)

Potent Inhibitors of Dipeptidyl Peptidase iv and Their Mechanisms of Inhibition

2006
Dipeptidyl peptidase IV (DP IV) is a proline specific serine protease which cleaves Xaa-Pro-dipeptides from the N-terminus of longer peptides. A series of product analogous amino acid amides containing different structure modifications like substitution of a ring atom, variation of the ring size and/or the introduction of a thioxo amide bond, phosphono
A, Stöckel-Maschek, B, Stiebitz, I, Born, J, Faust, W, Mögelin, K, Neubert   +5 more
openaire   +2 more sources

Dipeptidyl Peptidase-IV Inhibitors for Diabetes Mellitus

Journal of Research in Medical Education & Ethics, 2012
Dipeptidyl peptidase (DPP) IV inhibitors are drugs which prolong the action of Glucagon like peptide-1 (GLP-1) and glucosedependent insulinotropic polypeptide (GIP). The DPP IV inhibitors have shown improved glycemic control, and reduction of glycosylated haemoglobin in patients with type-2 diabetes.
Prithpal S Matreja, Jaspreet Kaur, Ashwani K Gupta, Amandeep Singh, P M L Khanna, H P Kayath   +5 more
openaire   +1 more source

Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors

Bioorganic & Medicinal Chemistry Letters, 2004
In this paper, the synthesis and structure-activity relationships (SAR) of two classes of electrophile-based dipeptidyl peptidase IV (DPP IV) inhibitors, the ketopyrrolidines and ketoazetidines, is discussed. The SAR of these series demonstrate that the 2-thiazole, 2-benzothiazole, and 2-pyridylketones are optimal S1' binding groups for potency against
Dana, Ferraris, Yao-Sen, Ko, David, Calvin, Tiffany, Chiou, Susan, Lautar, Bert, Thomas, Krystyna, Wozniak, Camilo, Rojas, Vincent, Kalish, Sergei, Belyakov   +9 more
openaire   +2 more sources

Discovery of tight-binding competitive inhibitors of dipeptidyl peptidase IV

International Journal of Biological Macromolecules, 2022
Dipeptidyl peptidase IV (DPP-IV, EC 3.4.14.5) is an abundant serine aminopeptidase that preferentially cleaves N-terminal Xaa-Pro or Xaa-Ala dipeptides from oligopeptides. Inhibitors of DPP-IV activity are used for treating type 2 diabetes mellitus and other diseases. DPP-IV is also involved in tumor progression.
Isel, Pascual Alonso, Pedro A, Valiente, Mario E, Valdés-Tresanco, Yarini, Arrebola, Fabiola, Almeida García, Lisset, Díaz, Gabriela, García, Osmany, Guirola, Daniel, Pastor, Gretchen, Bergado, Belinda, Sánchez, Jean-Louis, Charli   +11 more
openaire   +2 more sources

Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes

Bioorganic & Medicinal Chemistry Letters, 2007
A series of substituted imidazopiperidine amides has been prepared and evaluated for inhibition of dipeptidyl peptidase IV (DPP-4). Substitution at the 1- and 3-positions produced increased selectivity for DPP-4 relative to DPP-8 and DPP-9. Compounds in this series had IC(50) values as low as 5.8 nM for inhibition of DPP-4.
Ping, Chen, Charles G, Caldwell, Robert J, Mathvink, Barbara, Leiting, Frank, Marsilio, Reshma A, Patel, Joseph K, Wu, Huaibing, He, Kathryn A, Lyons, Nancy A, Thornberry, Ann E, Weber   +10 more
openaire   +2 more sources

Metabolism and disposition of the dipeptidyl peptidase IV inhibitor teneligliptin in humans

Xenobiotica, 2013
1. The absorption, metabolism and excretion of teneligliptin were investigated in healthy male subjects after a single oral dose of 20 mg [(14)C]teneligliptin. 2. Total plasma radioactivity reached the peak concentration at 1.33 h after administration and thereafter disappeared in a biphasic manner.
Yoshinobu, Nakamaru, Yoshiharu, Hayashi, Ruriko, Ikegawa, Shuji, Kinoshita, Begonya, Perez Madera, Dave, Gunput, Atsuhiro, Kawaguchi, Martin, Davies, Stuart, Mair, Hiroshi, Yamazaki, Toshiyuki, Kume, Masayuki, Suzuki   +11 more
openaire   +2 more sources

Evaluation of Dipeptidyl Peptidase-IV Inhibitor Use in the Inpatient Setting

Journal of Pharmacy Practice, 2020
Background: The American Diabetes Association recommends discontinuing non-insulin antihyperglycemic therapy during hospitalization and utilizing a basal insulin-containing regimen for patients with type 2 diabetes mellitus (T2DM).
Sarah E. Petite, Maja C. Hill
openaire   +2 more sources

Type 2 diabetes—Therapy with dipeptidyl peptidase IV inhibitors

Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics, 2005
The sole application of an inhibitor of the dipeptidyl peptidase DP IV (also DP 4, CD26, DPP-IV or DPP-4) to a mammal subsequently leading to improved glucose tolerance marks a major breakthrough in metabolic research bearing the potential of a new revolutionary diabetes therapy.
Hans-Ulrich, Demuth, Christopher H S, McIntosh, Raymond A, Pederson   +2 more
openaire   +2 more sources

GLP-1 Agonists and Dipeptidyl-Peptidase IV Inhibitors

2011
Novel therapeutic options for type 2 diabetes based on the action of the incretin hormone glucagon-like peptide-1 (GLP-1) were introduced in 2005. Incretin-based therapies consist of two classes: (1) the injectable GLP-1 receptor agonists solely acting on the GLP-1 receptor and (2) dipeptidyl-peptidase inhibitors (DPP-4 inhibitors) as oral medications ...
openaire   +2 more sources

Inhibitors of Dipeptidyl Peptidase IV - Recent Advances and Structural Views

Current Topics in Medicinal Chemistry, 2005
Prevalence of type 2 diabetes has increased dramatically in the last decades. Current medicines are not yet capable to efficiently prevent or reverse progression of the disease and its associated comorbidities. As a consequence, there is a great need for novel antidiabetic drugs.
Daniel, Hunziker, Michael, Hennig, Jens-Uwe, Peters   +2 more
openaire   +2 more sources