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8D4Z

Crystal structure of USP7 in complex with allosteric inhibitor FX1-3763

Summary for 8D4Z
Entry DOI10.2210/pdb8d4z/pdb
DescriptorUbiquitin carboxyl-terminal hydrolase 7, 1-({(7M)-7-[1-(azetidin-3-yl)-6-chloro-1,2,3,4-tetrahydroquinolin-8-yl]thieno[3,2-b]pyridin-2-yl}methyl)pyrrolidine-2,5-dione, GLYCEROL, ... (4 entities in total)
Functional Keywordsusp7, allosteric, inhibitor, hydrolase, hydrolase-inhibitor complex, hydrolase/inhibitor
Biological sourceHomo sapiens (human)
Total number of polymer chains2
Total formula weight85129.03
Authors
Bell, J.A. (deposition date: 2022-06-03, release date: 2023-09-20)
Primary citationFutran, A.S.,Lu, T.,Amberg-Johnson, K.,Xu, J.,Yang, X.,He, S.,Boyce, S.,Bell, J.,Pelletier, R.,Suzuki, T.,Huang, X.,Qian, H.,Fang, L.,Xing, L.,Xu, Z.,Kurtz, S.E.,Tyner, J.W.,Tang, W.,Guo, T.,Akinsanya, K.,Madge, D.,Jensen, K.
Novel USP7 inhibitors demonstrate potent anti-cancer activity in models of AML, synergy with BCL2 inhibition, and a differentiated mechanism of action
To Be Published,
Experimental method
X-RAY DIFFRACTION (2.26 Å)
Structure validation

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