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; PubMed: 38301010; DOI: 10.1126/science.adi5798

Experimental method

X-RAY DIFFRACTION (1.75 Å)