QIAO LIXIN,GHOSH SHOMIR,PETTER RUSSELL COLYN,NIU DEQIANG,SINGH JUSWINDER,ZHU ZHENDONG,KLUGE ARTHUR,LOBB ROY
申请号:
NZ62017410
公开号:
NZ620174A
申请日:
2010.09.15
申请国别(地区):
NZ
年份:
2016
代理人:
摘要:
Disclosed is a protein kinase conjugate that has the formula, X-M-S-CH2-Prot wherein, Prot is a protein kinase or portion thereof that contains a cysteine residue selected from the group consisting of CYS1, CYS5, CYS6, CYS7, CYS8, CYS9, CYS10, CYS11, CYS12 and CYS13 S-CH2 is the sulfur atom and methylene group from the side chain of said cysteine residue M is a modifier moiety that is formed by the covalent bonding of a warhead group with the side chain of said cysteine residue and X is a chemical moiety that binds in or near the ATP binding site of the protein kinase. Also disclosed in the use of the conjugates in the manufacture of a medicament for topical treatment of diseases and conditions, especially of the eye.