DRUMMOND, ALAN HASTINGS,DAVIDSON, ALAN HORNSBY,MOFFAT, DAVID FESTUS CHARLES,DONALD, ALISTAIR DAVID GRAHAM,DAVIES, STEPHEN JOHN
申请号：
NZ58734109
公开号：
NZ587341A
申请日:
2009.02.27
申请国别(地区):
NZ
年份:
2012
代理人:
摘要：
Disclosed is a covalent conjugate of an alpha, alpha-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme, wherein: the ester group of the conjugate is hydrolysable by cells containing the intracellular carboxylesterase enzyme hCE-1 to the corresponding alpha amino acid and not by cells containing hCE-2 or hCE-3 the alpha, alpha-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme and the said alpha, alpha-disubstituted glycine ester being conjugated to the modulator via its alpha amino group such that the nitrogen of the said amino is not directly linked to a carbonyl moiety whereby the amino acid conjugate which is the hydrolysis product of the alpha, alpha-disubstituted glycine ester conjugate retains the intracellular binding activity of the parent modulator with the target enzyme.
