8EJB
Bruton's tyrosine kinase in complex with 3-{[4-(1-acetylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide
Summary for 8EJB
Entry DOI | 10.2210/pdb8ejb/pdb |
Descriptor | Tyrosine-protein kinase BTK, 5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]-3-[4-(piperidin-4-yl)anilino]pyrazine-2-carboxamide, 1,2-ETHANEDIOL, ... (6 entities in total) |
Functional Keywords | protein degradation, leukemia, transferase |
Biological source | Homo sapiens (human) |
Total number of polymer chains | 1 |
Total formula weight | 32255.81 |
Authors | Gajewski, S.,Clifton, M.C. (deposition date: 2022-09-16, release date: 2023-02-15, Last modification date: 2024-05-22) |
Primary citation | Zhang, D.,Harris, H.M.,Chen, J.,Judy, J.,James, G.,Kelly, A.,McIntosh, J.,Tenn-McClellan, A.,Ambing, E.,Tan, Y.S.,Lu, H.,Gajewski, S.,Clifton, M.C.,Yung, S.,Robbins, D.W.,Pirooznia, M.,Skanland, S.S.,Gaglione, E.,Mhibik, M.,Underbayev, C.,Ahn, I.E.,Sun, C.,Herman, S.E.M.,Noviski, M.,Wiestner, A. NRX-0492 degrades wild-type and C481 mutant BTK and demonstrates in vivo activity in CLL patient-derived xenografts. Blood, 141:1584-1596, 2023 Cited by PubMed: 36375120DOI: 10.1182/blood.2022016934 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.58 Å) |
Structure validation
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