Results 41 to 50 of about 79,680 (194)

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

Minor Contribution of Endogenous GLP-1 and GLP-2 to Postprandial Lipemia in Obese Men. [PDF]

PLoS ONE, 2016
Glucose and lipids stimulate the gut-hormones glucagon-like peptide (GLP)-1, GLP-2 and glucose-dependent insulinotropic polypeptide (GIP) but the effect of these on human postprandial lipid metabolism is not fully clarified.To explore the responses of ...
Niina Matikainen, Elias Björnson, Sanni Söderlund, Christofer Borén, Björn Eliasson, Kirsi H Pietiläinen, Leonie H Bogl, Antti Hakkarainen, Nina Lundbom, Angela Rivellese, Gabriele Riccardi, Jean-Pierre Després, Natalie Alméras, Jens Juul Holst, Carolyn F Deacon, Jan Borén, Marja-Riitta Taskinen   +16 more
doaj   +1 more source

A Microgel Platform Enables Site‐Specific Intestinal Delivery of Lactoferrin, Improving its Bioavailability for Targeted Alleviating Liver Injury and Colitis

Advanced Science, EarlyView.
This work first time reports an eco‐friendly desert plant food‐based polysaccharide ASKP microgels which have intestinal site‐specific release properties which can achieve small‐intestine or colon targeting capability via different cross‐linking chemistry.
Huiling Yan, Yixuan Li, Shanan Chen, Pengcheng Du, Kaiwen Wu, Hui Zhang, Kasper Hettinga, Lina Zhang, Gergely Toldi, Fazheng Ren, Yuan Li   +10 more
wiley   +1 more source

GLP-1 based therapeutics: Simultaneously combating T2DM and obesity

Frontiers in Neuroscience, 2015
Glucagon-like peptide-1 (GLP-1) enhances meal-related insulin secretion, which lowers blood glucose excursions. In addition to its incretin action, GLP-1 acts on the GLP-1 receptor (GLP-1R) in the brain to suppress feeding. These combined actions of GLP-
Kristy M Heppner, Diego ePerez-Tilve
doaj   +1 more source

Targeting ANGPTL3 and IL‐33/ST2 Ameliorates Diabetic Kidney Disease by Reducing Lipotoxicity, Alleviating Inflammation and Inhibiting Fibrosis

Advanced Science, EarlyView.
Dual targeting of ANGPTL3 and IL‐33/ST2 attenuates diabetic kidney disease by reprogramming lipid–inflammatory crosstalk. This strategy reduces renal lipotoxicity, suppresses inflammatory activation, and limits fibrotic remodeling, thereby preserving kidney structure and function and highlighting a mechanism‐guided therapeutic approach for metabolic ...
Zhuojin Li, Zhonglian Cao, Rongrui Zhou, Xu Cheng, Xiaozhi Hu, Shuwen Xu, Zihan Dou, Ling Du, Dianwen Ju   +8 more
wiley   +1 more source

Glucagon receptor antagonist upregulates circulating GLP-1 level by promoting intestinal L-cell proliferation and GLP-1 production in type 2 diabetes

BMJ Open Diabetes Research & Care, 2020
ObjectiveGlucagon receptor (GCGR) blockage improves glycemic control and increases circulating glucagon-like peptide-1 (GLP-1) level in diabetic animals and humans.
Shan Lang, Liangbiao Gu, Xiaona Cui, Tianjiao Wei, Junling Liu, Yunyi Le, Rui Wei, Tianpei Hong   +7 more
doaj   +1 more source

SuFEx‐Enabled Reprogramming of Flavonoids for Selective α‐Glucosidase Covalent Inhibition

Advanced Science, EarlyView.
Selective inhibition of intestinal α‐glucosidase remains limited by poor enzyme specificity and off‐target metabolic effects. Here, SuFEx click chemistry is used to reprogram natural flavonoids into covalent inhibitors with enhanced α‐glucosidase selectivity and controlled reactivity. This strategy enables effective regulation of carbohydrate digestion
Fengyu Guo, Liwei Zhang, Minlong Wang, Yanjin Du, Tianyu Zhang, Hao Chen, Jiazeng Sun, Yang Yu, Zude He, Jie An, Xiaoxu Zhang, Weilin Lin, Fazheng Ren, Pengjie Wang, Ping Liu   +14 more
wiley   +1 more source

Differential effects of glucose‐dependent insulinotropic polypeptide receptor/glucagon‐like peptide‐1 receptor heteromerization on cell signaling when expressed in HEK‐293 cells

Pharmacology Research & Perspectives, 2022
The incretin hormones: glucose‐dependent insulinotropic polypeptide (GIP) and glucagon‐like peptide‐1 (GLP‐1) are important regulators of many aspects of metabolism including insulin secretion.
Bashaier Al‐Zaid, Siby Chacko, Charles Ifeamalume Ezeamuzie, Moritz Bünemann, Cornelius Krasel, Tina Karimian, Peter Lanzerstorfer, Suleiman Al‐Sabah   +7 more
doaj   +1 more source

Adipocyte Myoglobin Is a Determinant of Energy Expenditure and a Potential Target to Limit Obesity

Advanced Science, EarlyView.
Myoglobin, known as a muscle oxygen‐carrying protein, is shown to play a key role in fat cells that burn energy. Loss of myoglobin reduces the body's ability to generate heat and increases obesity risk, while restoring it improves metabolism. The study identifies myoglobin as a regulator of fat burning and a potential target to enhance energy ...
Christian Strehlau, Helen Broghammer, Claudia Gebhardt, Anne Hoffmann, Tobias Hagemann, Şeyma Midilli, Rachel S. Zimmer, Kristin Schubert, Vasiliki Karagiannakou, Anastasia Georgiadi, Mario Ost, Martin Krüger, Lisa Roth, Kerstin Krause, Nora Klöting, Maria Keller, Martin Wabitsch, Rima Nuwayhid, Roland H. Stimson, Michael Stumvoll, Matthias Blüher, Juliane Weiner, John T. Heiker   +22 more
wiley   +1 more source

Ferulic acid reduces GLP‐1 degradation to ameliorate diet‐induced obesity‐associated hepatic steatosis

Food Frontiers
GLP‐1 is a vital candidate for stimulating insulin secretion in a glucose‐dependent manner, reducing body weight and eliminating nonalcoholic fatty liver disease with few side effects.
Yuxuan An, Lichao Zhang, Xiaxia Fan, Kaili Cui, Shuiling He, Pengyu Ji, Jinmiao Tian, Zhuoyu Li   +7 more
doaj   +1 more source