8GC8
Bruton's tyrosine kinase L528W mutant in complex with 5-(piperidin-1-yl)-3-{[4-(piperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide
Summary for 8GC8
Entry DOI | 10.2210/pdb8gc8/pdb |
Descriptor | Tyrosine-protein kinase BTK, 5-(piperidin-1-yl)-3-[4-(piperidin-4-yl)anilino]pyrazine-2-carboxamide, 1,2-ETHANEDIOL, ... (4 entities in total) |
Functional Keywords | degrader, complex, signaling protein |
Biological source | Homo sapiens (human) |
Total number of polymer chains | 1 |
Total formula weight | 32275.09 |
Authors | Gajewski, S. (deposition date: 2023-03-01, release date: 2024-01-31, Last modification date: 2024-02-21) |
Primary citation | Montoya, S.,Bourcier, J.,Noviski, M.,Lu, H.,Thompson, M.C.,Chirino, A.,Jahn, J.,Sondhi, A.K.,Gajewski, S.,Tan, Y.S.M.,Yung, S.,Urban, A.,Wang, E.,Han, C.,Mi, X.,Kim, W.J.,Sievers, Q.,Auger, P.,Bousquet, H.,Brathaban, N.,Bravo, B.,Gessner, M.,Guiducci, C.,Iuliano, J.N.,Kane, T.,Mukerji, R.,Reddy, P.J.,Powers, J.,Sanchez Garcia de Los Rios, M.,Ye, J.,Barrientos Risso, C.,Tsai, D.,Pardo, G.,Notti, R.Q.,Pardo, A.,Affer, M.,Nawaratne, V.,Totiger, T.M.,Pena-Velasquez, C.,Rhodes, J.M.,Zelenetz, A.D.,Alencar, A.,Roeker, L.E.,Mehta, S.,Garippa, R.,Linley, A.,Soni, R.K.,Skanland, S.S.,Brown, R.J.,Mato, A.R.,Hansen, G.M.,Abdel-Wahab, O.,Taylor, J. Kinase-impaired BTK mutations are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127. Science, 383:eadi5798-eadi5798, 2024 Cited by PubMed: 38301010DOI: 10.1126/science.adi5798 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.75 Å) |
Structure validation
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