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TitleMolecular and Structural Basis of Pan-Resistance to BTK Degraders and Inhibitors.
Journal, issue, pagesCancer Discov, Year 2026
Publish dateOct 20, 2025 (structure data deposition date)
AuthorsSievers, Q. / Lu, H. / Cool, A. / Gajewski, S. / Kong, T. / Noviski, M.A. / Whelan, S. / Wang, Y. / Mendoza Navarrete, L. / Mi, X. ...Sievers, Q. / Lu, H. / Cool, A. / Gajewski, S. / Kong, T. / Noviski, M.A. / Whelan, S. / Wang, Y. / Mendoza Navarrete, L. / Mi, X. / Ficici, E. / Mukerji, R. / Iuliano, J.N. / Ye, J. / Sanchez Garcia De Los Rios, M. / Bousquet, H. / Tan, M. / Brathaban, N. / Narasappa, N. / Lu, Y.W. / Elechko, J. / Maron, M.I. / Phelps, C.B. / Rahman, J. / Notti, R.Q. / Sekeres, S. / Lamkin, E.N. / Bravo, E. / Alencar, A. / Ewalt, M.D. / Islam, P. / Mato, A.R. / Roeker, L. / Bhatt, S. / Taylor, J. / Thompson, M.C. / Hansen, G.M. / Abdel-Wahab, O.
External linksCancer Discov / PubMed:42484277
MethodsX-ray diffraction
Resolution1.5 - 1.8 Å
Structure data

PDB-9yt9:
A428D mutant of Bruton's tyrosine kinase
Method: X-RAY DIFFRACTION / Resolution: 1.8 Å

PDB-9zqv:
Crystal structure of wild-type Bruton's Tyrosine Kinase (BTK) in the apo form
Method: X-RAY DIFFRACTION / Resolution: 1.5 Å

Chemicals

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-HOH:
WATER

ChemComp-IOD:
IODIDE ION

ChemComp-CL:
Unknown entry

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / kinase dead mutant / clinical mutation / autoinhibited kinase / SIGNALING PROTEIN / nonreceptor protein tyrosine kinase / B-cell activation / BTK

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