6JWE

structure of RET G-quadruplex in complex with colchicine

Summary for 6JWE

• Entry DOI: 10.2210/pdb6jwe/pdb
• Related: 2L88
• Descriptor: DNA (5'-D(*GP*GP*GP*GP*CP*GP*GP*GP*GP*CP*GP*GP*GP*GP*CP*GP*GP*GP*GP*T)-3'), N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5H-benzo[d]heptalen-7-yl]ethanamide (2 entities in total)
• Functional Keywords: ret, g-quadruplex, colchicine, dna
• Biological source: Homo sapiens
• Total number of polymer chains: 1
• Total formula weight: 6793.51

Authors

Wang, F.,Wang, C.,Liu, Y.,Lan, W.X.,Li, Y.M.,Wang, R.X.,Cao, C. (deposition date: 2019-04-20, release date: 2020-02-26, Last modification date: 2024-05-15)

Primary citation

Wang, F.,Wang, C.,Liu, Y.,Lan, W.,Han, H.,Wang, R.,Huang, S.,Cao, C.
Colchicine selective interaction with oncogene RET G-quadruplex revealed by NMR.
Chem.Commun.(Camb.), 56:2099-2102, 2020

PubMed Abstract: G-quadruplexes (G4s) are frequently formed in the promoter regions of oncogenes, considered as promising drug targets for anticancer therapy. Due to high structure similarity of G4s, discovering ligands selectively interacting with only one G4 is extremely difficult. Here, mainly by NMR, we report that colchicine selectively binds to oncogene RET G4-DNA.

PubMed: 32025680
DOI: 10.1039/d0cc00221f

Experimental method

SOLUTION NMR