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PDBsum entry 6lvm
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References listed in PDB file
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Key reference
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Title
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Structure-Based drug design of 1,3,5-Triazine and pyrimidine derivatives as novel fgfr3 inhibitors with high selectivity over vegfr2.
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Authors
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I.Kuriwaki,
M.Kameda,
H.Hisamichi,
S.Kikuchi,
K.Iikubo,
Y.Kawamoto,
H.Moritomo,
Y.Kondoh,
Y.Amano,
Y.Tateishi,
Y.Echizen,
Y.Iwai,
A.Noda,
H.Tomiyama,
T.Suzuki,
M.Hirano.
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Ref.
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Bioorg Med Chem, 2020,
28,
115453.
[DOI no: ]
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PubMed id
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Abstract
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Fibroblast growth factor receptor 3 (FGFR3) is an attractive therapeutic target
for the treatment of bladder cancer. We identified 1,3,5-triazine derivative 18b
and pyrimidine derivative 40a as novel structures with potent and highly
selective FGFR3 inhibitory activity over vascular endothelial growth factor
receptor 2 (VEGFR2) using a structure-based drug design (SBDD) approach. X-ray
crystal structure analysis suggests that interactions between 18b and amino acid
residues located in the solvent region (Lys476 and Met488), and between 40a and
Met529 located in the back pocket of FGFR3 may underlie the potent FGFR3
inhibitory activity and high kinase selectivity over VEGFR2.
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