8YKI

FGFR-1 in complex with ligand tasurgratinib

This is a non-PDB format compatible entry.

Summary for 8YKI

• Entry DOI: 10.2210/pdb8yki/pdb
• Descriptor: Fibroblast growth factor receptor 1, Tasurgratinib, CHLORIDE ION, ... (4 entities in total)
• Functional Keywords: fgf receptor kinase, proteros biostructures gmbh, transferase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 2
• Total formula weight: 73479.18

Authors

Ikemori-Kawada, M.,Watanabe Miyano, S. (deposition date: 2024-03-05, release date: 2024-06-12)

Primary citation

Kawano, S.,Kawada, M.I.,Fukushima, S.,Arai, Y.,Shibata, T.,Miyano, S.W.
Antitumor Activity of Tasurgratinib as an Orally Available FGFR1-3 Inhibitor in Cholangiocarcinoma Models With FGFR2-fusion.
Anticancer Res., 44:2393-2406, 2024

PubMed Abstract: Cholangiocarcinoma (CCA) is an aggressive tumor with limited treatment options especially in 2nd line or later treatments. Targeting fibroblast growth factor receptor (FGFR) 2 has recently emerged as a promising treatment option for patients with CCA harboring FGFR2-fusion. This study investigated the antitumor activities of tasurgratinib as an orally available FGFR1-3 inhibitor, in preclinical FGFR2-driven CCA models.

PubMed: 38821585
DOI: 10.21873/anticanres.17046

Experimental method

X-RAY DIFFRACTION (2.79 Å)