AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors

X He, C You, H Jiang, Y Jiang, HE Xu… - Acta Pharmacologica …, 2023 - nature.com
As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide
range of physiological processes. Extensive efforts of structural biology have been made on …

New insights into the structure and function of class B1 GPCRs

BP Cary, X Zhang, J Cao, RM Johnson… - Endocrine …, 2023 - academic.oup.com
G protein–coupled receptors (GPCRs) are the largest family of cell surface receptors. Class
B1 GPCRs constitute a subfamily of 15 receptors that characteristically contain large …

Structural basis of odorant recognition by a human odorant receptor

CB Billesbølle, CA de March, WJC van der Velden… - Nature, 2023 - nature.com
Our sense of smell enables us to navigate a vast space of chemically diverse odour
molecules. This task is accomplished by the combinatorial activation of approximately 400 …

Structural insights into ligand recognition and activation of the medium-chain fatty acid-sensing receptor GPR84

H Liu, Q Zhang, X He, M Jiang, S Wang, X Yan… - nature …, 2023 - nature.com
GPR84 is an orphan class AG protein-coupled receptor (GPCR) that is predominantly
expressed in immune cells and plays important roles in inflammation, fibrosis, and …

Profiling of basal and ligand-dependent GPCR activities by means of a polyvalent cell-based high-throughput platform

M Zeghal, G Laroche, JD Freitas, R Wang… - Nature …, 2023 - nature.com
Representing the most attractive and successful druggable receptors of the proteome,
GPCRs regulate a myriad of physiological and pathophysiological functions. Although over …

Structural insights into the human niacin receptor HCA2-Gi signalling complex

Y Yang, HJ Kang, R Gao, J Wang, GW Han… - Nature …, 2023 - nature.com
The hydroxycarboxylic acid receptor 2 (HCA2) agonist niacin has been used as treatment for
dyslipidemia for several decades albeit with skin flushing as a common side-effect in treated …

Mechanism of activation and biased signaling in complement receptor C5aR1

Y Feng, C Zhao, Y Deng, H Wang, L Ma, S Liu, X Tian… - Cell Research, 2023 - nature.com
The complement system plays an important role in the innate immune response to invading
pathogens. The complement fragment C5a is one of its important effector components and …

Structural Insights into Molecular Recognition and Receptor Activation in Chemokine–Chemokine Receptor Complexes

L Urvas, E Kellenberger - Journal of Medicinal Chemistry, 2023 - ACS Publications
The chemokine system is a key player in the functioning of the immune system and a sought-
after target for drug candidates. The number of experimental structures of chemokines in …

Mechanism of hormone and allosteric agonist mediated activation of follicle stimulating hormone receptor

J Duan, P Xu, H Zhang, X Luan, J Yang, X He… - Nature …, 2023 - nature.com
Follicle stimulating hormone (FSH) is an essential glycoprotein hormone for human
reproduction, which functions are mediated by a G protein-coupled receptor, FSHR …

Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator

BE Krumm, JF DiBerto, RHJ Olsen, HJ Kang… - Biochemistry, 2023 - ACS Publications
The NTSR1 neurotensin receptor (NTSR1) is a G protein-coupled receptor (GPCR) found in
the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide …