9U4S

Crystal Structure of PI5P4K-gamma in complex with n40

This is a non-PDB format compatible entry.

Summary for 9U4S

• Entry DOI: 10.2210/pdb9u4s/pdb
• Descriptor: Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, ~{N}-[5-(4-oxidanylidene-3-propyl-quinazolin-6-yl)pyridin-2-yl]pentanamide (3 entities in total)
• Functional Keywords: kinase, transferase, lipid metabolism, lipid binding protein
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 2
• Total formula weight: 81140.78

Authors

Zhao, W.F.,Xu, Y.C. (deposition date: 2025-03-20, release date: 2025-11-12)

Primary citation

Xiong, L.,Tang, L.,Zhao, W.,Wang, R.,Cheng, C.,Wang, D.,Xu, Y.,Tang, L.,Fan, Y.
Orthosteric-allosteric dual inhibitors of PI5P4K gamma with potent antitumor activity in non-small cell lung cancer.
J Adv Res, 2025

PubMed Abstract: Phosphatidylinositol 5-phosphate 4-kinase type II gamma (PI5P4Kγ) has emerged as a promising therapeutic target in oncology due to its key role in cancer progression. However, currently available inhibitors targeting either the orthosteric or allosteric sites of PI5P4Kγ suffer from limited in vitro activity and in vivo validation.

PubMed: 40992727
DOI: 10.1016/j.jare.2025.09.024

Experimental method

X-RAY DIFFRACTION (2.25 Å)