9IQX

Cryo-EM structure of the human TRPV4-RhoA in complex with AH001

Summary for 9IQX

• Entry DOI: 10.2210/pdb9iqx/pdb
• EMDB information: 60797
• Descriptor: Transient receptor potential cation channel subfamily V member 4, Transforming protein RhoA, O-[(R)-{[(2R)-2,3-bis(octadecanoyloxy)propyl]oxy}(hydroxy)phosphoryl]-L-serine, ... (6 entities in total)
• Functional Keywords: antagonist, complex, membrane protein, hydrolase
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 6
• Total formula weight: 338604.79

Authors

Yuan, Z.,Ruan, S.S.,Li, S.L. (deposition date: 2024-07-13, release date: 2025-05-28, Last modification date: 2025-07-02)

Primary citation

Wang, J.,Yuan, Z.,Yu, N.,Jiao, Q.,Zhou, H.,Liao, W.,Shan, J.,Ruan, S.,Zhao, Y.,Mo, Y.,Qi, L.,Li, T.,Fu, J.,Ke, B.,Xu, Y.,Qian, X.,Zhang, J.,Zhao, Z.,Li, S.,Wang, R.,Li, H.
Inactivation of RhoA for Hypertension Treatment Through the TRPV4-RhoA-RhoGDI1 Axis.
Circulation, 2025

PubMed Abstract: The RhoA (Ras homolog family member A) signaling pathway is pivotal in regulating vascular smooth muscle cells (VSMCs) function and blood pressure homeostasis. Current inhibitors of the RhoA signaling pathway are limited in hypertension treatment, suffering from poor efficacy, insufficient specificity, and developmental challenges.

PubMed: 40518994
DOI: 10.1161/CIRCULATIONAHA.124.071884

Experimental method

ELECTRON MICROSCOPY (3.37 Å)