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 …

Multiple recent HCAR2 structures demonstrate a highly dynamic ligand binding and G protein activation mode

A Shenol, R Tenente, M Lückmann, TM Frimurer… - Nature …, 2024 - nature.com
A surprisingly clear picture of the allosteric mechanism connecting G protein-coupled
receptor agonists with G protein binding—and back–is revealed by a puzzle of thirty novel …

Our extended microbiome: The human-relevant metabolites and biology of fermented foods

EB Caffrey, JL Sonnenburg, S Devkota - Cell Metabolism, 2024 - cell.com
One of the key modes of microbial metabolism occurring in the gut microbiome is
fermentation. This energy-yielding process transforms common macromolecules like …

Structural basis for ligand recognition and signaling of hydroxy-carboxylic acid receptor 2

JH Park, K Kawakami, N Ishimoto, T Ikuta… - Nature …, 2023 - nature.com
Hydroxycarboxylic acid receptors (HCAR1, HCAR2, and HCAR3) transduce Gi/o signaling
upon biding to molecules such as lactic acid, butyric acid and 3-hydroxyoctanoic acid, which …

Structure-guided engineering of biased-agonism in the human niacin receptor via single amino acid substitution

MK Yadav, P Sarma, J Maharana, M Ganguly… - Nature …, 2024 - nature.com
The Hydroxycarboxylic acid receptor 2 (HCA2), also known as the niacin receptor or
GPR109A, is a prototypical GPCR that plays a central role in the inhibition of lipolytic and …

[HTML][HTML] Molecular recognition of niacin and lipid-lowering drugs by the human hydroxycarboxylic acid receptor 2

S Zhu, Q Yuan, X Li, X He, S Shen, D Wang, J Li… - Cell Reports, 2023 - cell.com
Niacin, an age-old lipid-lowering drug, acts through the hydroxycarboxylic acid receptor 2
(HCAR2), a G-protein-coupled receptor (GPCR). Yet, its use is hindered by side effects like …

Structural insights into ligand recognition and selectivity of the human hydroxycarboxylic acid receptor HCAR2

X Pan, F Ye, P Ning, Z Zhang, X Li, B Zhang, Q Wang… - Cell Discovery, 2023 - nature.com
Abstract Hydroxycarboxylic acid receptor 2 (HCAR2) belongs to the family of class AG
protein-coupled receptors with key roles in regulating lipolysis and free fatty acid formation …

Molecular activation and G protein coupling selectivity of human succinate receptor SUCR1

T Wang, W Tang, X Zhu, Z Lv, J Chen, Y Li, X Sun, H Lv… - Cell Research, 2024 - nature.com
Dear Editor, Succinate (SA) is a classic intermediate metabolite of the TCA cycle and is
produced in mitochondria under normal physiological conditions. 1 SA accumulates within …

Role of GPR109A in psoriasis

L Leko - 2023 - repozitorij.pbf.unizg.hr
Sažetak Psoriasis is a chronic, inflammatory skin disease characterized by keratinocyte
hyperproliferation and immune cell infiltration. In this study, bioinformatic analysis showed …