The new biology and pharmacology of glucagon

TD Müller, B Finan, C Clemmensen… - Physiological …, 2017 - journals.physiology.org
In the last two decades we have witnessed sizable progress in defining the role of
gastrointestinal signals in the control of glucose and energy homeostasis. Specifically, the …

Future directions for peptide therapeutics development

AA Kaspar, JM Reichert - Drug discovery today, 2013 - Elsevier
Highlights•An unprecedented number of peptide therapeutics have recently been
approved.•Clinical pipeline analysis reveals an emphasis on peptides with enhanced …

The incretin hormone GLP‐1 and mechanisms underlying its secretion: 肠促胰岛素激素GLP‐1 及其潜在的分泌机制

L Tian, T Jin - Journal of diabetes, 2016 - Wiley Online Library
摘要胰高血糖素样肽‐1 (Glucagon‐like peptide‐1, GLP‐1) 是一种细胞类型特异性的胰高血糖
素原翻译后产物. 它是由胰高血糖素原基因所编码的, 在激素, 神经元以及营养的刺激下主要由肠 …

Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein

Y Zhang, B Sun, D Feng, H Hu, M Chu, Q Qu… - Nature, 2017 - nature.com
Abstract Glucagon-like peptide 1 (GLP-1) is a hormone with essential roles in regulating
insulin secretion, carbohydrate metabolism and appetite. GLP-1 effects are mediated …

Structural insights into differences in G protein activation by family A and family B GPCRs

D Hilger, KK Kumar, H Hu, MF Pedersen, ES O'Brien… - Science, 2020 - science.org
INTRODUCTION Transmembrane signaling of heterotrimeric guanine nucleotide–binding
protein (G protein)–coupled receptors (GPCRs) is mediated by ligand-dependent …

Diabetic cardiomyopathy: mechanisms and new treatment strategies targeting antioxidant signaling pathways

K Huynh, BC Bernardo, JR McMullen… - Pharmacology & …, 2014 - Elsevier
Cardiovascular disease is the primary cause of morbidity and mortality among the diabetic
population. Both experimental and clinical evidence suggest that diabetic subjects are …

Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators

G Song, D Yang, Y Wang, C De Graaf, Q Zhou, S Jiang… - Nature, 2017 - nature.com
The glucagon-like peptide-1 receptor (GLP-1R) and the glucagon receptor (GCGR) are
members of the secretin-like class B family of G-protein-coupled receptors (GPCRs) and …

Structure of the human glucagon class B G-protein-coupled receptor

FY Siu, M He, C De Graaf, GW Han, D Yang, Z Zhang… - Nature, 2013 - nature.com
Binding of the glucagon peptide to the glucagon receptor (GCGR) triggers the release of
glucose from the liver during fasting; thus GCGR plays an important role in glucose …

[HTML][HTML] GLP-1 and GLP-2 orchestrate intestine integrity, gut microbiota, and immune system crosstalk

N Abdalqadir, K Adeli - Microorganisms, 2022 - mdpi.com
The intestine represents the body's largest interface between internal organs and external
environments except for its nutrient and fluid absorption functions. It has the ability to sense …

Small molecule allosteric modulators of G-protein-coupled receptors: drug–target interactions

S Lu, J Zhang - Journal of medicinal chemistry, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) are the largest class of signaling receptors that are
most frequently targeted by therapeutic drugs. Allosteric modulators bound to GPCRs at …