4UWB

Fibroblast growth factor receptor 1 kinase in complex with JK-P5

Summary for 4UWB

• Entry DOI: 10.2210/pdb4uwb/pdb
• Related: 4UWC
• Descriptor: FIBROBLAST GROWTH FACTOR RECEPTOR 1, 1,2-ETHANEDIOL, N-[4-(4-methylpiperazin-1-yl)phenyl]-1H-indazole-3-carboxamide, ... (5 entities in total)
• Functional Keywords: transferase
• Biological source: HOMO SAPIENS (HUMAN)
• Cellular location: Cell membrane; Single-pass type I membrane protein: P11362
• Total number of polymer chains: 2
• Total formula weight: 71443.95

Authors

Beeston, H.,Tucker, J.,Kankanala, J. (deposition date: 2014-08-11, release date: 2015-09-02, Last modification date: 2024-05-01)

Primary citation

Beeston, H.S.,Klein, T.,Norman, R.A.,Tucker, J.A.,Anderson, M.,Ashcroft, A.E.,Holdgate, G.A.
Validation of IMS-MS as a screening tool to identify type II kinase inhibitors of FGFR1 kinase.
Rapid Commun Mass Spectrom, :e9130-e9130, 2021

PubMed Abstract: The protein kinase FGFR1 regulates cellular processes in human development. As over-activity of FGFR1 is implicated with cancer, effective inhibitors are in demand. Type I inhibitors, which bind to the active form of FGFR1, are less effective than type II inhibitors, which bind to the inactive form. Screening to distinguish between type I and type II inhibitors is required.

PubMed: 34038603
DOI: 10.1002/rcm.9130

Experimental method

X-RAY DIFFRACTION (2.31 Å)