Results 31 to 40 of about 46,900 (298)

Multicomponent Stapling of Glucagon‐Like Peptide‐1 Enables Receptor‐Guided PROTAC Delivery

Angewandte Chemie, EarlyView.
We report a stapled glucagon‐like peptide‐1 (GLP‐1) analogue created via multicomponent tryptophan‐mediated Petasis reaction (TMPR). This strategy yields a stabilised peptide with superior helicity and improved potency. Conjugation to a bromodomain‐containing protein 4 (BRD4) degrader creates the first GLP‐1‐guided targeted protein degrader (PROTAC ...
Jan L. Venne, Sona Krajcovicova, Graeme Davies, Hannah Bolt, Jefferson Revell, David R. Spring   +5 more
wiley   +2 more sources

The persistent inhibitory properties of saxagliptin on renal dipeptidyl peptidase-4: Studies with HK-2 cells in vitro and normal rats in vivo

Journal of Pharmacological Sciences, 2017
Saxagliptin, a potent and selective DPP-4 inhibitor, exhibits a slow dissociation from DPP-4. We investigated the sustained effects of saxagliptin on renal DPP-4 activity in a washout study using renal tubular (HK-2) cells, and in a pharmacodynamic study
Masako Uchii, Mariko Sakai, Yuhei Hotta, Satoshi Saeki, Naoya Kimoto, Akinori Hamaguchi, Tetsuya Kitayama, Shunji Kunori   +7 more
doaj   +1 more source

Phenylalanine 664 of dipeptidyl peptidase (DPP) 7 and Phenylalanine 671 of DPP11 mediate preference for P2-position hydrophobic residues of a substrate [PDF]

, 2013
Dipeptidyl peptidases (DPPs) are crucial for the energy metabolism in Porphyromonas gingivalis, a Gram-negative proteolytic and asaccharolytic anaerobic rod causing chronic periodontitis.
Takayuki K. Nemoto, Yuko Ohara-Nemoto, Rouf, Shakh M.A., Ohara-Nemoto, Yuko, Shigenobu Kimura, Ono, Toshio, Kimura, Shigenobu, Shimoyama, Yu, Shakh M.A. Rouf, Toshio Ono, Nemoto, Takayuki K., Yu Shimoyama   +11 more
core   +1 more source

The Role of Dipeptidyl Peptidase Inhibitors in Pulmonary Diseases

Biomedicines
The dipeptidyl peptidase (DPP) family comprises enzymes with important metabolic and immunomodulatory properties. This narrative review summarizes recent clinical and experimental evidence on the role of DPP-1, DPP-4, DPP-9, and DPP-10 in pulmonary ...
Theodoros Panou, Paschalis Steiropoulos, Fotios Drakopanagiotakis   +2 more
doaj   +1 more source

Dipeptidyl peptidase-4 levels are increased and partially related to body fat distribution in patients with familial partial lipodystrophy type 2

Diabetology & Metabolic Syndrome, 2017
Background Dipeptidyl peptidase-4 (DDP4) is an enzyme responsible for glucagon-like peptide-1 inactivation and plays an important role in glucose metabolism.
Cynthia Melissa Valerio, Juliana Severo de Almeida, Rodrigo Oliveira Moreira, Luiza Barreto. S. Aguiar, Priscila O. Siciliano, Denise P. Carvalho, Amelio F. Godoy-Matos   +6 more
doaj   +1 more source

Incident heart failure and myocardial infarction in sodium-glucose cotransporter-2 vs. dipeptidyl peptidase-4 inhibitor users [PDF]

, 2022
Aims This study aimed to compare the rates of major cardiovascular adverse events in sodium-glucose cotransporter-2 inhibitors (SGLT2I) and dipeptidyl peptidase-4 inhibitors (DPP4I) users in a Chinese population.
Dong Chang, Bernard Man Yung Cheung, Ying Liu, Gary Tse, Sharen Lee, Jiandong Zhou, Tong Liu, Ian Chi Kei Wong, Qingpeng Zhang, Keith Sai Kit Leung, Abraham Ka Chung Wai, Wing Tak Wong   +11 more
core  

In vitro evaluation of 2-pyrazoline derivatives as DPP-4 inhibitors

Türk Biyokimya Dergisi, 2022
In this study, the synthesis of three pyrazoline derivatives and the evaluation of their inhibitory effects on dipeptidyl peptidase (DPP-4) were aimed.
Temel Halide Edip, Altıntop Mehlika Dilek, Sever Belgin, Özdemir Ahmet, Akalın Çiftçi Gülşen   +4 more
doaj   +1 more source

Dipeptidyl peptidase-4 inhibitors and cardiovascular and renal disease in type 2 diabetes:What have we learned from the CARMELINA trial? [PDF]

, 2019
Dipeptidyl peptidase-4 inhibitors are a relatively new class of oral anti-hyperglycaemic drugs to treat type 2 diabetes through prevention of degradation of incretins by the dipeptidyl peptidase-4 enzyme.
Jandeleit-Dahm, Karin A. M., Hanssen, Nordin M. J., Hanssen, Nordin M.J., Jandeleit-Dahm, Karin A.M.   +3 more
core   +1 more source

Cardiac DPP-4 inhibition by saxagliptin ameliorates isoproterenol-induced myocardial remodeling and cardiac diastolic dysfunction in rats

Journal of Pharmacological Sciences, 2016
Saxagliptin, a potent and selective DPP-4 inhibitor, is characterized by its slow dissociation from DPP-4 and its long half-life and is expected to have a potent tissue membrane-bound DPP-4-inhibitory effect in various tissues.
Junichi Ikeda, Naoya Kimoto, Tetsuya Kitayama, Shunji Kunori   +3 more
doaj   +1 more source

The effect of Islamic fasting in Ramadan on osteoporosis [PDF]

Journal of Fasting and Health, 2017
Osteoporosis is considered as one of the most common diseases that women face after their menopause and is caused by both genetic and environmental factors.
Seyed Mohammad Amin Kormi, Shima Ardehkhani, Mohammad Amin Kerachian   +2 more
doaj   +1 more source