Drug discovery approaches targeting the incretin pathway

X Deng, MS Tavallaie, R Sun, J Wang, Q Cai… - Bioorganic …, 2020 - Elsevier
Incretin pathway plays an important role in the development of diabetes medications.
Interventions in DPP-4 and GLP-1 receptor have shown remarkable efficacy in experimental …

A GLP‐1/glucagon (GCG)/CCK2 receptors tri‐agonist provides new therapy for obesity and diabetes

S Zhao, Z Yan, Y Du, Z Li, C Tang, L Jing… - British Journal of …, 2022 - Wiley Online Library
Background and Purpose Glucagon‐like peptide‐1 (GLP‐1) and glucagon (GCG) receptor
dual agonist have promising therapeutic effects in the treatment of obesity and diabetes …

Design of Xenopus GLP-1-Based Long-Acting Dual GLP-1/Y2 Receptor Agonists

Q Yang, W Tang, L Sun, Z Yan, C Tang… - Journal of medicinal …, 2022 - ACS Publications
GLP-1 receptor (GLP-1R) and neuropeptide Y2 receptor (Y2R) dual agonists have shown
great potential to treat obesity and type 2 diabetes (T2DM). We developed a multitarget …

Discovery of a potent and long-acting Xenopus GLP-1-based GLP-1/glucagon/Y2 receptor triple agonist

Y Yuan, Z Yan, Q Lao, N Jiang, S Wu, Q Lu… - European Journal of …, 2023 - Elsevier
The combination of incretin-based therapies and PYY analogue has shown great potential
for the treatment of type 2 diabetes (T2DM) and obesity. In this study we developed the first …

Peptide-based long-acting co-agonists of GLP-1 and cholecystokinin 1 receptors as novel anti-diabesity agents

Q Yang, F Zhou, X Tang, J Wang, H Feng… - European journal of …, 2022 - Elsevier
The combined use of gastrointestinal hormones for treating metabolic diseases is gaining
increasing attention. It was documented previously that co-administration of a …

Design of novel Xenopus GLP-1-based dual glucagon-like peptide 1 (GLP-1)/glucagon receptor agonists

N Jiang, L Jing, Q Li, S Su, Q Yang, F Zhou… - European Journal of …, 2021 - Elsevier
Dual activation of the glucagon receptor (GCGR) and glucagon-like peptide 1 receptor (GLP-
1R) has the potential to lead to an effective therapy for the treatment of diabetes and obesity …

Stapled and Xenopus Glucagon-Like Peptide 1 (GLP-1)-Based Dual GLP-1/Gastrin Receptor Agonists with Improved Metabolic Benefits in Rodent Models of Obesity …

X Chen, J Fu, F Zhou, Q Yang, J Wang… - Journal of Medicinal …, 2020 - ACS Publications
Diabetes is characterized by pancreas dysfunction and is commonly associated with obesity.
Hypoglycemic agents capable of improving β-cell function and reducing body weight …

Preparation and Pharmaceutical Characterizations of Lipidated Dimeric Xenopus Glucagon-Like Peptide-1 Conjugates

J Han, F Zhou, Y Fei, X Chen, J Fu… - Bioconjugate …, 2018 - ACS Publications
A pair of glucagon-like peptide-1 (GLP-1) analogs (1 and 2) were synthesized by hybridizing
the key sequences of GLP-1, exendin-4, lixisenatide, and xenGLP-1B (Xenopus GLP-1 …

[HTML][HTML] Discovery of novel glucagon-like peptide 1/cholecystokinin 1 receptor dual agonists

Z Chenxu, S Lidan, H Guoqiang, G Binbin… - European Journal of …, 2024 - Elsevier
The combined use of gastrointestinal hormones for treating metabolic diseases is gaining
increasing attention. The potential of developing novel dual agonists targeting both …

Lithocholic Acid-Based Peptide Delivery System for an Enhanced Pharmacological and Pharmacokinetic Profile of Xenopus GLP-1 Analogs

J Han, X Chen, L Zhao, J Fu, L Sun… - Molecular …, 2018 - ACS Publications
GLP-1 analogs suffer from the main disadvantage of a short in vivo half-life. Lithocholic acid
(LCA), one of the four main bile acids in the human body, possesses a high albumin binding …