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RECEPTOR TYROSINKINASE (RTK) INHIBITORS AND WAYS OF THEIR APPLICATION
专利权人:
ЙЕЙЛ ЮНИВЕРСИТИ (US)
发明人:
БАЕ Дзае Хиун (US),ЛЭКС Айрит (US),ШЛЕССИНГЕР Джозеф (US)
申请号:
RU2012134637/10
公开号:
RU2012134637A
申请日:
2011.01.13
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. A molecule that binds to an asymmetric contact region of receptor tyrosine kinase (RTK), where the molecule inhibits ligand-induced trans-autophosphorylation of RTK. 2. The molecule according to claim 1, wherein the molecule does not bind to the nucleotide binding site of the RTK catalytic domain. The molecule of claim 1, wherein the molecule binds to an asymmetric contact region on the N-portion of one RTK monomer. The molecule of claim 1, wherein the molecule binds to an asymmetric contact region on the C-lobe of one RTK monomer. The molecule of claim 1, wherein the molecule does not cause a loss of intrinsic kinase activity. The molecule of claim 1, wherein the molecule increases steric restrictions between the RTK monomers. The molecule of claim 1, wherein the molecule does not prevent RTK dimerization. The molecule of claim 1, wherein the molecule prevents dimerization of the RTK cytoplasmic domains. The molecule of claim 1, wherein the RTK is a fibroblast growth factor receptor (FGFR). The molecule of claim 9, wherein the fibroblast growth factor receptor is a fibroblast growth factor receptor 1 (FGFR1). The molecule of claim 9, wherein the fibroblast growth factor receptor is a fibroblast growth factor receptor 2 (FGFR2). The molecule of claim 9, wherein the fibroblast growth factor receptor is a fibroblast growth factor receptor 3 (FGFR3). The molecule of claim 9, wherein the fibroblast growth factor receptor is a fibroblast growth factor receptor 4 (FGFR4). The molecule of claim 1, wherein the molecule binds to the amino acid residue Arg577 from FGFR1, Arg579 from FGFR2, or Arg580 from FGFR2.15. The molecule of claim 1, wherein the molecule binds to the amino acid residue Asp519 of FGFR1.16. The molecule of claim 1, wherein the molecule binds to an amino acid residue, select1. Молекула, которая связывается с асимметричной областью контакта рецепторной тирозинкиназы (RTK), где молекула ингибирует индуцируемое лигандом транс-аутофосфорилирование RTK.2. Мол
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