5T31

Exploiting an Asp-Glu switch in Glycogen Synthase Kinase 3 to design paralog selective inhibitors for use in acute myeloid leukemia

Summary for 5T31

• Entry DOI: 10.2210/pdb5t31/pdb
• Descriptor: Glycogen synthase kinase-3 beta, (4~{S})-4-ethyl-7,7-dimethyl-4-phenyl-2,6,8,9-tetrahydropyrazolo[3,4-b]quinolin-5-one (2 entities in total)
• Functional Keywords: glycogen synthase 3 alpha beta mutant, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 2
• Total formula weight: 94433.27

Authors

Stein, A.J.,Holson, E.B.,Wagner, F.F.,Cambell, A.J. (deposition date: 2016-08-24, release date: 2018-02-21, Last modification date: 2023-11-15)

• Primary citation: Wagner, F.F.,Benajiba, L.,Campbell, A.J.,Weiwer, M.,Sacher, J.R.,Gale, J.P.,Ross, L.,Puissant, A.,Alexe, G.,Conway, A.,Back, M.,Pikman, Y.,Galinsky, I.,DeAngelo, D.J.,Stone, R.M.,Kaya, T.,Shi, X.,Robers, M.B.,Machleidt, T.,Wilkinson, J.,Hermine, O.,Kung, A.,Stein, A.J.,Lakshminarasimhan, D.,Hemann, M.T.,Scolnick, E.,Zhang, Y.L.,Pan, J.Q.,Stegmaier, K.,Holson, E.B.; Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia.; Sci Transl Med, 10:-, 2018; PubMed: 29515000; DOI: 10.1126/scitranslmed.aam8460

Experimental method

X-RAY DIFFRACTION (2.85 Å)