7L5E

Crystal Structure of KPT-330 bound to CRM1 (537-DLTVK-541 to GLCEQ)

7L5E の概要

• エントリーDOI: 10.2210/pdb7l5e/pdb
• 分子名称: GTP-binding nuclear protein Ran, Ran-specific GTPase-activating protein 1, Exportin-1, ... (8 entities in total)
• 機能のキーワード: crm1, xpo1, kpt, selinexor, kpt-330, protein transport
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 159303.52

構造登録者

Baumhardt, J.M.,Chook, Y.M. (登録日: 2020-12-21, 公開日: 2021-01-27, 最終更新日: 2023-10-18)

主引用文献

Walker, J.S.,Hing, Z.A.,Harrington, B.,Baumhardt, J.,Ozer, H.G.,Lehman, A.,Giacopelli, B.,Beaver, L.,Williams, K.,Skinner, J.N.,Cempre, C.B.,Sun, Q.,Shacham, S.,Stromberg, B.R.,Summers, M.K.,Abruzzo, L.V.,Rassenti, L.,Kipps, T.J.,Parikh, S.,Kay, N.E.,Rogers, K.A.,Woyach, J.A.,Coppola, V.,Chook, Y.M.,Oakes, C.,Byrd, J.C.,Lapalombella, R.
Recurrent XPO1 mutations alter pathogenesis of chronic lymphocytic leukemia.
J Hematol Oncol, 14:17-17, 2021

PubMed Abstract: Exportin 1 (XPO1/CRM1) is a key mediator of nuclear export with relevance to multiple cancers, including chronic lymphocytic leukemia (CLL). Whole exome sequencing has identified hot-spot somatic XPO1 point mutations which we found to disrupt highly conserved biophysical interactions in the NES-binding groove, conferring novel cargo-binding abilities and forcing cellular mis-localization of critical regulators. However, the pathogenic role played by change-in-function XPO1 mutations in CLL is not fully understood.

PubMed: 33451349
DOI: 10.1186/s13045-021-01032-2

実験手法

X-RAY DIFFRACTION (1.944 Å)