The corticotropin-releasing factor family: physiology of the stress response

JM Deussing, A Chen - Physiological reviews, 2018 - journals.physiology.org
The physiological stress response is responsible for the maintenance of homeostasis in the
presence of real or perceived challenges. In this function, the brain activates adaptive …

The emergence of the C–H functionalization strategy in medicinal chemistry and drug discovery

R Jana, HM Begam, E Dinda - Chemical Communications, 2021 - pubs.rsc.org
Owing to the market competitiveness and urgent societal need, an optimum speed of drug
discovery is an important criterion for successful implementation. Despite the rapid ascent of …

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 …

Phase-plate cryo-EM structure of a class B GPCR–G-protein complex

YL Liang, M Khoshouei, M Radjainia, Y Zhang… - Nature, 2017 - nature.com
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases,
such as osteoporosis, diabetes and obesity. Here we report the structure of a full-length …

Differential GLP-1R binding and activation by peptide and non-peptide agonists

X Zhang, MJ Belousoff, P Zhao, AJ Kooistra, TT Truong… - Molecular Cell, 2020 - cell.com
Peptide drugs targeting class B1 G-protein-coupled receptors (GPCRs) can treat multiple
diseases; however, there remains substantial interest in the development of orally delivered …

Structural basis of Gs and Gi recognition by the human glucagon receptor

A Qiao, S Han, X Li, Z Li, P Zhao, A Dai, R Chang, L Tai… - Science, 2020 - science.org
Class BG protein–coupled receptors, an important class of therapeutic targets, signal mainly
through the Gs class of heterotrimeric G proteins, although they do display some promiscuity …

Toward a structural understanding of class B GPCR peptide binding and activation

YL Liang, MJ Belousoff, P Zhao, C Koole, MM Fletcher… - Molecular cell, 2020 - cell.com
Class BG protein-coupled receptors (GPCRs) are important therapeutic targets for major
diseases. Here, we present structures of peptide and Gs-bound pituitary adenylate cyclase …

Extending the structural view of class B GPCRs

C de Graaf, G Song, C Cao, Q Zhao, MW Wang… - Trends in biochemical …, 2017 - cell.com
The secretin-like class B family of G protein-coupled receptors (GPCRs) are key players in
hormonal homeostasis. Recent structures of various receptors in complex with a variety of …

[HTML][HTML] Delineating the activation mechanism and conformational landscape of a class BG protein-coupled receptor glucagon receptor

Y Wang, M Li, W Liang, X Shi, J Fan, R Kong… - Computational and …, 2022 - Elsevier
Class BG protein-coupled receptors (GPCRs) are important targets in the treatment of
metabolic syndrome and diabetes. Although multiple structures of class B GPCRs–G protein …

Molecular basis for hormone recognition and activation of corticotropin-releasing factor receptors

S Ma, Q Shen, LH Zhao, C Mao, XE Zhou, DD Shen… - Molecular cell, 2020 - cell.com
Corticotropin-releasing factor (CRF) and the three related peptides urocortins 1–3 (UCN1–
UCN3) are endocrine hormones that control the stress responses by activating CRF1R and …