Results 131 to 140 of about 2,782 (157)

Discovery of BGM1812, a Novel Dual Amylin and Calcitonin Receptor Agonist for Obesity Treatment

Journal of Medicinal Chemistry
Parallel activation of the calcitonin receptor (CTR) and amylin receptor (AMYR) is considered a more effective weight-loss strategy. Although the novel dual amylin and calcitonin receptor agonist (DACRA), petrelintide, is currently undergoing phase II clinical trials, its agonistic activity remains insufficient compared with natural agonists.
Leilei Zong, Zhoudong Zhang, Xionghao Li, Jie Jia, Xiaohui Jiang, Zitong Wang, Wenlang Liu, Xinyi Shen, Xiangyang Feng, Yangqing Huang, Haifeng Ding, Yunsong Song, Zheng Zheng, Jiandong Yuan, Huanqiu Li   +14 more
openaire   +2 more sources

A novel oral dual amylin and calcitonin receptor agonist (KBP-042) exerts antiobesity and antidiabetic effects in rats

American Journal of Physiology - Endocrinology and Metabolism, 2014
The present study investigated a novel oral dual amylin and calcitonin receptor agonist (DACRA), KBP-042, in head-to-head comparison with salmon calcitonin (sCT) with regard to in vitro receptor pharmacology, ex vivo pancreatic islet studies, and in vivo proof of concept studies in diet-induced obese (DIO) and Zucker diabetic fatty (ZDF) rats. In vitro,
Morten Karsdal, Jan Erik Henriksen, Kim Henriksen   +2 more
exaly   +3 more sources

211-OR: Dual Amylin and Calcitonin Receptor Agonists Increase Mitochondrial Respiratory Capacity in Adipose Tissues of Obese Rat

Diabetes, 2023
Dual amylin and calcitonin receptor agonists (DACRAs) are potential therapeutic candidates for treatment of obesity. Preclinical studies have shown favorable effects of DACRAs on appetite regulation contributing to a reduction in body weight. Interestingly, the DACRA-induced effects on weight loss are superior to the effects of a suppressed food intake,
EMILIE A. PETERSEN, IDA BLOM, SIMONE A. MELANDER, MORTEN A. KARSDAL, STEEN LARSEN, KIM HENRIKSEN, ANNA T. LARSEN   +6 more
openaire   +1 more source

894-P: MET-233 Is an Ultra-Long-Acting Amylin Receptor Agonist

Diabetes
Introduction and Objective: MET-233 is an ultra-long acting (ULA) amylin analog being evaluated in clinical trials for the treatment of obesity. We sought preclinical proof of concept that MET-233, designed to be combined with GLP-1R agonist MET-097, is an effective candidate for obesity treatment. Methods: MET-233 emerged from an amylin
JAMES S. MINNION, CHARLOTTE HINDS, BEATA REGLINSKA   +2 more
openaire   +1 more source

Development of a Long-Acting and Stapled Dual Amylin and Calcitonin Receptor Agonist as Monotherapy and Combination with GLP-1R Agonists for the Treatment of Obesity

Bioconjugate Chemistry
Dual amylin and calcitonin receptor agonists (DACRAs) offer a promising strategy for treating obesity and related metabolic disorders but are limited by aggregation and the short half-lives of native peptides. Here, we report the design of a long-acting and stapled DACRA via a streamlined on-resin Ugi macrocyclization strategy based on a salmon ...
Yaqi Zhou, Pu Xu, Jiang Lu, Shujing Xu, Wenting Qiu, Xiao Ning, Jiean Xu, Nan Zheng   +7 more
openaire   +2 more sources

Engineering of an Ultralong-Acting and Nonaggregating Dual Amylin and Calcitonin Receptor Agonist with Durable Efficacy in Obesity and Diabetes

Journal of Medicinal Chemistry
Synergistic activation of amylin and calcitonin receptors represents a distinct strategy for the treatment of obesity and diabetes. However, the inherent fibrillogenic aggregation propensity and short half-life pose significant challenges for their therapeutic translation.
Nan Zheng, Rongfang Chen, Luying Yang, Pu Xu, Xueying Wang, Xin Sun, Yanxia Lin, Jinying Qiu, Xiao-xuan Su, You Wang, Leiming Wang, Weijun Shen   +11 more
openaire   +2 more sources

789-P: Discovery of a Novel, Long-Acting Amylin Receptor Agonist for Body Weight Control

Diabetes
Introduction & Objective: Amylin, a hormone co-secreted with insulin from pancreatic beta-cells, reduces food intake and glucagon levels. Combination of GLP-1 and amylin analogs promotes weight loss and glucose control. However, treatment is complicated by the need to formulate the peptides in different buffers.
YAN LI, HAIXIA ZOU, XINLE WU, RUI ZHU, RUIPENG WANG, SUJUAN HAO, ZHAOYING LI, YAXU WANG, JIANHUI DENG, HONGYANG WANG, FEI PENG, CATHERINE L. JONES, MARTIJN FENAUX   +12 more
openaire   +1 more source

The enduring metabolic improvement of combining dual amylin and calcitonin receptor agonist and semaglutide treatments in a rat model of obesity and diabetes

American Journal of Physiology-Endocrinology and Metabolism
These studies describe the benefit of combining dual amylin and calcitonin receptor agonists (DACRA) with semaglutide for long-term treatment of obesity and type 2 diabetes. Combination treatment induced sustained weight loss and improved glucose control.
Anna Thorsø Larsen, Khaled Elhady Mohamed, Simone Anna Melander, Morten Asser Karsdal, Kim Henriksen   +4 more
openaire   +3 more sources

882-P: Eloralintide, a Selective, Long-Acting Amylin Receptor Agonist for Obesity—Phase 1 Proof of Concept

Diabetes
Introduction and Objective: Eloralintide (Elora; LY3841136) is a potent, long acting once weekly (QW) amylin receptor agonist under development for obesity. Unlike other amylin agonist molecules (e.g. Cagrilintide), it is designed to have minimal calcitonin activity in the clinic.
SHOBHA N. BHATTACHAR, LAI-SAN THAM, BETH TIDEMANN-MILLER, DANIEL A. BRIERE, HONGCHANG QU, AXEL HAUPT, EDWARD J. PRATT, KIEREN J. MATHER   +7 more
openaire   +1 more source

A structural basis for amylin receptor phenotype

Science, 2022
Madeleine Fletcher, Radostin Danev, Rachael Johnson   +2 more
exaly