9O3B

PKM2 bound to MCTI-566

This is a non-PDB format compatible entry.

Summary for 9O3B

• Entry DOI: 10.2210/pdb9o3b/pdb
• Descriptor: Pyruvate kinase PKM, 1,6-di-O-phosphono-beta-D-fructofuranose, OXALATE ION, ... (8 entities in total)
• Functional Keywords: activator, pyruvate kinase, transferase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 8
• Total formula weight: 484577.81

Authors

Stuckey, J.A. (deposition date: 2025-04-07, release date: 2025-08-13)

Primary citation

Pan, W.W.,Weh, K.M.,Chaudhury, S.,Fernando, R.,Hager, H.,Wen, B.,Chinnaswamy, K.,Stuckey, J.A.,Rech, J.C.,Besirli, C.G.,Weh, E.,Wubben, T.J.
A Novel, Long-Acting, Small Molecule PKM2 Activator and Its Potential Broad Application Against Photoreceptor Degeneration.
Transl Vis Sci Technol, 14:26-26, 2025

PubMed Abstract: Activating pyruvate kinase M2 (PKM2) has been shown to be neuroprotective in preclinical models of photoreceptor degeneration. We recently developed novel, small molecule activators for ocular delivery. Here, we sought to characterize the ocular pharmacology, toxicity, and efficacy of MCTI-566, a novel PKM2 activator, to translate this therapeutic strategy to the clinic.

PubMed: 40742037
DOI: 10.1167/tvst.14.7.26

Experimental method

X-RAY DIFFRACTION (2.416 Å)