4UAL

MRCK beta in complex with BDP00005290

4UAL の概要

• エントリーDOI: 10.2210/pdb4ual/pdb
• 分子名称: Serine/threonine-protein kinase MRCK beta, 4-chloro-1-(piperidin-4-yl)-N-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]-1H-pyrazole-3-carboxamide, CHLORIDE ION, ... (5 entities in total)
• 機能のキーワード: myotonic dystrophy kinase-related cdc42-binding kinase, metastasis, cell invasion, transferase
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Cytoplasm : Q9Y5S2
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 48528.17

構造登録者

Schuettelkopf, A.W. (登録日: 2014-08-10, 公開日: 2014-10-22, 最終更新日: 2023-12-20)

主引用文献

Unbekandt, M.,Croft, D.R.,Crighton, D.,Mezna, M.,McArthur, D.,McConnell, P.,Schuttelkopf, A.W.,Belshaw, S.,Pannifer, A.,Sime, M.,Bower, J.,Drysdale, M.,Olson, M.F.
A novel small-molecule MRCK inhibitor blocks cancer cell invasion.
Cell Commun. Signal, 12:54-54, 2014

PubMed Abstract: The myotonic dystrophy kinase-related CDC42-binding kinases MRCKα and MRCKβ regulate actin-myosin contractility and have been implicated in cancer metastasis. Along with the related ROCK1 and ROCK2 kinases, the MRCK proteins initiate signalling events that lead to contractile force generation which powers cancer cell motility and invasion. A potential strategy for cancer therapy is to reduce metastasis by blocking MRCK activity, either alone or in combination with ROCK inhibition. However, to date no potent small molecule inhibitors have been developed with selectivity towards MRCK.

PubMed: 25288205
DOI: 10.1186/PREACCEPT-1467335606136283

実験手法

X-RAY DIFFRACTION (1.71 Å)