Results 31 to 40 of about 28,823 (297)

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 pleiotropic cardiovascular effects of dipeptidyl peptidase‐4 inhibitors [PDF]

British Journal of Clinical Pharmacology, 2018
Patients with Type 2 diabetes have an excess risk for cardiovascular disease. One of the several approaches, included in the guidelines for the management of Type 2 diabetes, is based on dipeptidyl peptidase 4 (DPP‐4; also termed CD26) inhibitors, also called gliptins.
Avogaro, Angelo, Fadini, Gian Paolo
openaire   +3 more sources

An open-label pilot study on preventing glucocorticoid-induced diabetes mellitus with linagliptin

Journal of Medical Case Reports, 2018
Background Numerous patients develop diabetes in response to glucocorticoid therapy. This study explored the efficacy, safety, and preventive potential of the dipeptidyl peptidase-4 inhibitor, linagliptin (TRADJENTA®), in the development of ...
Yoshia Miyawaki, Ken-Ei Sada, Yosuke Asano, Keigo Hayashi, Yuriko Yamamura, Sumie Hiramatsu, Keiji Ohashi, Michiko Morishita, Haruki Watanabe, Yoshinori Matsumoto, Katsue Sunahori-Watanabe, Tomoko Kawabata, Jun Wada   +12 more
doaj   +1 more source

Dipeptidyl-Peptidase 4 Inhibitor-Induced Variants of Bullous Pemphigoid: A Case Series of Four Patients. [PDF]

Case Rep Dermatol, 2022
Bullous pemphigoid is the most common acquired bullous disease with an autoimmune basis and a tendency to involve mostly old people. By rising incidence of diabetes all over the world, consumption of antidiabetes medications has also increased.
Balighi K, Heidari S, Kavyani M, Kamyab Hesari K, Tootoonchi N.   +4 more
europepmc   +2 more sources

Comparing sodium-glucose cotransporter 2 inhibitors and dipeptidyl peptidase-4 inhibitors on new-onset depression: a propensity score-matched study in Hong Kong. [PDF]

, 2023
The risk of new onset depression associated with sodium-glucose co-transporter 2 inhibitor (SGLT2I) use in patients with type 2 diabetes mellitus (T2DM) remains unclear.
Li, Lifang, Hui, Jeremy, Azfar, Nida, Tse, Gary, Mui, Jonathan V, Chou, O., Lee, Athena, Lee, Sharen, Zhou, Jiandong   +8 more
core   +1 more source

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

Crystal structures of trypanosoma brucei oligopeptidase B broaden the paradigm of catalytic regulation in prolyl oligopeptidase family enzymes [PDF]

, 2013
Oligopeptidase B cleaves after basic amino acids in peptides up to 30 residues. As a virulence factor in bacteria and trypanosomatid pathogens that is absent in higher eukaryotes, this is a promising drug target.
Rory E Morty, Canning Peter, Rea, Dean, Dean Rea (483664), Morty Rory E., Morty, Rory E., Dean Rea, Vilmos Fülöp, Rory E. Morty (341515), Canning, Peter, Fülöp, Vilmos, Peter Canning, Peter Canning (483663), Vilmos Fülöp (483665), Rea Dean, Fülöp Vilmos   +15 more
core   +1 more source

Impact of endogenous insulin secretion on the improvement of glucose variability in Japanese patients with type 2 diabetes treated with canagliflozin plus teneligliptin

Journal of Diabetes Investigation, 2021
Aims/Introduction To identify the effect of combination therapy with a dipeptidyl peptidase‐4 inhibitor and a sodium–glucose cotransporter 2 inhibitor compared with switching from a dipeptidyl peptidase‐4 inhibitor to a sodium–glucose cotransporter 2 ...
Aika Miya, Akinobu Nakamura, Kyu Yong Cho, Shinichiro Kawata, Hiroshi Nomoto, So Nagai, Hajime Sugawara, Shinji Taneda, Kazuhisa Tsuchida, Kazuno Omori, Hiroki Yokoyama, Jun Takeuchi, Shin Aoki, Yoshio Kurihara, Tatsuya Atsumi, Hideaki Miyoshi   +15 more
doaj   +1 more source

Dipeptidyl Peptidase-4 Inhibitor Induced Angioedema - An Overlooked Adverse Drug Reaction? [PDF]

, 2018
INTRODUCTION: Angioedema is a potentially fatal adverse drug reaction of some medications, as swellings of the upper airways can cause death by asphyxiation.
Andersen, Michelle F, Buchwald, Christian Von, Christian Von Buchwald, Susanne I. Scott, Aagaard, Lise, Lise Aagaard, Scott, Susanne I, Michelle F. Andersen, Rasmussen, Eva R, Eva R. Rasmussen   +9 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