Results 261 to 270 of about 22,784 (283)

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
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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
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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 ...
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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
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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
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Do Dipeptidyl Peptidase IV (DPP-IV) Inhibitors Cause Heart Failure?

Clinical Therapeutics, 2014
Although recent reports suggest an association between saxagliptin and an increased risk of admissions for heart failure, it is not clear whether dipeptidyl peptidase IV (DPP-IV) inhibition contributes to heart failure in high-risk patients. The purpose of this research is to understand heart failure risk among high-risk patients with type 2 diabetes ...
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Dipeptidyl peptidase IV inhibitors.

IDrugs : the investigational drugs journal, 2003
The patent literature for dipeptidyl peptidase IV (DPP-IV) inhibitors for the period of January 2001 to May 2002 is reviewed. There has been increased interest in DPP-IV inhibitors since their potential for the treatment of diabetes was identified. This review will focus on reversible inhibitors of the enzyme, for which the primary interest has been ...
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New Fluorogenic Dipeptidyl Peptidase IV/CD26 Substrates and Inhibitors

1997
Dipeptidyl peptidase IV (DP IV, CD26) is a membrane bound serine protease which ubiquitously occurs in epithelial tissues of mammalian organisms, above all in kidney, liver and intestine1,2 but also on the surface of immune cells3. DP IV is involved not only in activation of B- and T-lymphocytes4,5 and NK-cells6 with peptidase activity but also in the ...
S, Lorey, J, Faust, U, Hermanns, F, Bühling, S, Ansorge, K, Neubert   +5 more
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Suppression of arthritis by the inhibitors of dipeptidyl peptidase IV

International Journal of Immunopharmacology, 1997
Dipeptidyl peptidase IV (DP IV, CD26) is a serine exoprotease which selectively cleaves the penultimate proline residue of polypeptides. This enzyme is also expressed as a surface marker on activated T cells. In order to assess the relevance of DP IV in immunological disorders, we evaluated the in vivo effects of specific DP IV inhibitors using two ...
S, Tanaka, T, Murakami, H, Horikawa, M, Sugiura, K, Kawashima, T, Sugita   +5 more
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Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors

Bioorganic & Medicinal Chemistry Letters, 2008
The synthesis, selectivity, rat pharmacokinetic profile, and drug metabolism profiles of a series of potent fluoroolefin-derived DPP-4 inhibitors (4) are reported. A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors.
Scott D, Edmondson, Lan, Wei, Jinyou, Xu, Jackie, Shang, Shiyao, Xu, Jianmei, Pang, Ashok, Chaudhary, Dennis C, Dean, Huaibing, He, Barbara, Leiting, Kathryn A, Lyons, Reshma A, Patel, Sangita B, Patel, Giovanna, Scapin, Joseph K, Wu, Maria G, Beconi, Nancy A, Thornberry, Ann E, Weber   +17 more
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