4UAK
MRCK beta in complex with ADP
Summary for 4UAK
| Entry DOI | 10.2210/pdb4uak/pdb |
| Descriptor | Serine/threonine-protein kinase MRCK beta, ADENOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... (6 entities in total) |
| Functional Keywords | myotonic dystrophy kinase-related cdc42-binding kinase, metastasis, cell invasion, transferase |
| Biological source | Homo sapiens (Human) |
| Cellular location | Cytoplasm : Q9Y5S2 |
| Total number of polymer chains | 1 |
| Total formula weight | 48632.15 |
| Authors | Schuettelkopf, A.W. (deposition date: 2014-08-10, release date: 2014-10-22, Last modification date: 2023-12-20) |
| Primary citation | 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 Cited by 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: 25288205DOI: 10.1186/PREACCEPT-1467335606136283 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.73 Å) |
Structure validation
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