TPX2 7-20 fused to Aurora-A residues 116-389, covalently modified on Cys290 by F104 (7-((perfluorophenyl)sulfonyl)-3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine)

TPX2 7-20 fused to Aurora-A residues 116-389, covalently modified on Cys290 by F104 (7-((perfluorophenyl)sulfonyl)-3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine) Descriptor: 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 7-[2,3,5,6-tetrakis(fluoranyl)phenyl]sulfonyl-3-(trifluoromethyl)-6,8-dihydro-5~{H}-[1,2,4]triazolo[4,3-a]pyrazine, ADENOSINE-5'-DIPHOSPHATE, ... Authors: Miles, J.A, Chesti, J, Nelson, A, Bayliss, R. Deposit date: 2025-09-30 Release date: 2026-03-18 Last modified: 2026-03-25 Method: X-RAY DIFFRACTION (2.27 Å) Cite: High-throughput discovery and characterisation of pentafluorobenzene sulfonamide modifiers of Aurora A kinase. Rsc Chem Biol, 2026

将TPX2 7-20片段融合至极光激酶A（Aurora-A）的116-389位残基，并通过F104（7-((全氟苯基)磺酰基)-3-(三氟甲基)-5,6,7,8-四氢-[1,2,4]三唑并[4,3-a]吡嗪）在Cys290位点实现共价修饰。描述符：2-(N-吗啉代)-乙磺酸、7-[2,3,5,6-四氟苯基]磺酰基-3-(三氟甲基)-6,8-二氢-5H-[1,2,4]三唑并[4,3-a]吡嗪、腺苷-5'-二磷酸（ADENOSINE-5'-DIPHOSPHATE）等。作者：Miles, J.A.、Chesti, J.、Nelson, A.、Bayliss, R. 提交日期：2025-09-30，发布日期：2026-03-18，最后修改日期：2026-03-25。实验方法：X射线衍射（X-RAY DIFFRACTION），分辨率2.27埃（Å）。引用文献：《极光A激酶五氟苯磺酰胺修饰剂的高通量发现与表征》，发表于Rsc Chem Biol，2026年。