Structure, function and drug discovery of GPCR signaling
L Cheng, F **a, 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 …
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 …
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 …
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
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 …
Biased signaling in drug discovery and precision medicine
Receptors are crucial for converting chemical and environmental signals into cellular
responses, making them prime targets in drug discovery, with about 70% of drugs targeting …
responses, making them prime targets in drug discovery, with about 70% of drugs targeting …
Structural basis of CXCR4 assembly and regulation
Summary CXC chemokine receptor 4 (CXCR4) is a well-established drug target and a key
representative of the chemokine receptor family. Chemokine receptors tend to assemble …
representative of the chemokine receptor family. Chemokine receptors tend to assemble …