8GCC

T. cruzi topoisomerase II alpha bound to dsDNA and the covalent inhibitor CT1

Summary for 8GCC

• Entry DOI: 10.2210/pdb8gcc/pdb
• EMDB information: 29930
• Descriptor: DNA topoisomerase 2, DNA (28-MER), 2-{3-[(Z)-iminomethyl]-1H-1,2,4-triazol-1-yl}-1-{(3M)-3-[2-(trifluoromethyl)phenyl]-6H-pyrrolo[3,4-b]pyridin-6-yl}ethan-1-one (3 entities in total)
• Functional Keywords: topoisomerase, dna binding protein, topoisomerase inhibitor, isomerase
• Biological source: Trypanosoma cruzi strain CL Brener; More
• Total number of polymer chains: 4
• Total formula weight: 196650.69

Authors

Schenk, A.,Deniston, C.,Noeske, J. (deposition date: 2023-03-01, release date: 2023-07-12)

• Primary citation: Rao, S.P.S.,Gould, M.K.,Noeske, J.,Saldivia, M.,Jumani, R.S.,Ng, P.S.,Rene, O.,Chen, Y.L.,Kaiser, M.,Ritchie, R.,Francisco, A.F.,Johnson, N.,Patra, D.,Cheung, H.,Deniston, C.,Schenk, A.D.,Cortopassi, W.A.,Schmidt, R.S.,Wiedemar, N.,Thomas, B.,Palkar, R.,Ghafar, N.A.,Manoharan, V.,Luu, C.,Gable, J.E.,Wan, K.F.,Myburgh, E.,Mottram, J.C.,Barnes, W.,Walker, J.,Wartchow, C.,Aziz, N.,Osborne, C.,Wagner, J.,Sarko, C.,Kelly, J.M.,Manjunatha, U.H.,Maeser, P.,Jiricek, J.,Lakshminarayana, S.B.,Barrett, M.P.,Diagana, T.T.; Cyanotriazoles are selective topoisomerase II poisons that rapidly cure trypanosome infections.; Science, 380:1349-1356, 2023; PubMed: 37384702; DOI: 10.1126/science.adh0614

Experimental method

ELECTRON MICROSCOPY (2.94 Å)