Fibroblast Growth Factor Receptor 1 Tyrosine Kinase (FGFR1K)
Fibroblast Growth Factor Receptor 1 Tyrosine Kinase (FGFR1K)
 Ligand in FGFR1K active site
 Ligand in FGFR1K active site.
Docking example from OTAVAchemicals Fgfr 1 tyrosine kinase focused library.
The detection of H-bonding between ligand and key FGFR1K residues (Ala564) was used for the library preparation.

Fibroblast growth factor receptors (FGFR) are members of a family of polypeptides synthesized by a variety of cell types during the processes of embryonic development and in adult tissues. FGFR have been detected in normal and malignant cells and are involved in biological events that include mitogenic and angiogenic activity with a consequent crucial role in cell differentiation and development. To activate signal transduction pathways, FGFR are coupled to fibroblast growth factors (FGF) and heparan sulfate (HS) proteoglycans to form a biologically fundamental ternary complex. Based on these considerations, a variety of inhibitors able to block the signaling cascade through a direct interaction with FGFR have been designed and investigated for their biological properties related to antiangiogenesis and antitumor activity.

The focused libraries, including docking scores and drug-like properties, are available on request.

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Manetti F, Botta M. Small-molecule inhibitors of fibroblast growth factor receptor (FGFR) tyrosine kinases (TK) Curr Pharm Des. 2003;9(7):567-81.