Structure, function and drug discovery of GPCR signaling
L Cheng, F Xia, Z Li, C Shen, Z Yang, H Hou… - Molecular …, 2023 - Springer
G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide
array of physiological processes and responses, such as sensory perception (eg, vision …
array of physiological processes and responses, such as sensory perception (eg, vision …
[HTML][HTML] Key aspects of modern GPCR drug discovery
P Addis, U Bali, F Baron, A Campbell, S Harborne… - SLAS Discovery, 2024 - Elsevier
G-protein-coupled receptors (GPCRs) are the largest and most versatile cell surface
receptor family with a broad repertoire of ligands and functions. We've learned an enormous …
receptor family with a broad repertoire of ligands and functions. We've learned an enormous …
Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation
C Zhao, H Wang, Y Liu, L Cheng, B Wang, X Tian, H Fu… - Molecular Cell, 2023 - cell.com
Summary Hydroxycarboxylic acid receptor 2 (HCAR2), modulated by endogenous ketone
body β-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for …
body β-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for …
Orthosteric and allosteric modulation of human HCAR2 signaling complex
C Mao, M Gao, SK Zang, Y Zhu, DD Shen… - Nature …, 2023 - nature.com
Hydroxycarboxylic acids are crucial metabolic intermediates involved in various
physiological and pathological processes, some of which are recognized by specific …
physiological and pathological processes, some of which are recognized by specific …
Integrative residue-intuitive machine learning and MD Approach to Unveil Allosteric Site and Mechanism for β2AR
X Chen, K Wang, J Chen, C Wu, J Mao, Y Song… - Nature …, 2024 - nature.com
Allosteric drugs offer a new avenue for modern drug design. However, the identification of
cryptic allosteric sites presents a formidable challenge. Following the allostery nature of …
cryptic allosteric sites presents a formidable challenge. Following the allostery nature of …
Structure-based identification of a G protein–biased allosteric modulator of cannabinoid receptor CB1
S Shen, C Wu, G Lin, X Yang, Y Zhou… - Proceedings of the …, 2024 - National Acad Sciences
Cannabis sativa is known for its therapeutic benefit in various diseases including pain relief
by targeting cannabinoid receptors. The primary component of cannabis, Δ9 …
by targeting cannabinoid receptors. The primary component of cannabis, Δ9 …
Orthosteric ligand selectivity and allosteric probe dependence at Hydroxycarboxylic acid receptor HCAR2
L Cheng, S Sun, H Wang, C Zhao, X Tian… - … and Targeted Therapy, 2023 - nature.com
Abstract Hydroxycarboxylic acid receptor 2 (HCAR2), a member of Class A G-protein-
coupled receptor (GPCR) family, plays a pivotal role in anti-lipolytic and anti-inflammatory …
coupled receptor (GPCR) family, plays a pivotal role in anti-lipolytic and anti-inflammatory …
[HTML][HTML] Allosteric crosstalk in modular proteins: Function fine-tuning and drug design
S Abhishek, W Deeksha, KR Nethravathi… - Computational and …, 2023 - Elsevier
Modular proteins are regulatory proteins that carry out more than one function. These
proteins upregulate or downregulate a biochemical cascade to establish homeostasis in …
proteins upregulate or downregulate a biochemical cascade to establish homeostasis in …
Know your molecule: pharmacological characterization of drug candidates to enhance efficacy and reduce late-stage attrition
T Kenakin - Nature Reviews Drug Discovery, 2024 - nature.com
Despite advances in chemical, computational and biological sciences, the rate of attrition of
drug candidates in clinical development is still high. A key point in the small-molecule …
drug candidates in clinical development is still high. A key point in the small-molecule …
[HTML][HTML] G protein-coupled receptors driven intestinal glucagon-like peptide-1 reprogramming for obesity: Hope or hype?
Abstract 'Globesity'is a foremost challenge to the healthcare system. The limited efficacy and
adverse effects of available oral pharmacotherapies pose a significant obstacle in the fight …
adverse effects of available oral pharmacotherapies pose a significant obstacle in the fight …