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Achieving selectivity between highly homologous tyrosine kinases: a novel selective erbB2 inhibitor.

Abstract：

:The discovery of small molecule kinase inhibitors for use as drugs is a promising approach for the treatment of cancer and other diseases, but the discovery of highly specific agents is challenging because over 850 kinases are expressed in mammalian cells. Systematic modification of the 4-anilino functionality of a selective quinazoline inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase can invert selectivity to favor inhibition of the highly homologous erbB2 tyrosine kinase. The selectivity pattern was demonstrated in assays of recombinant kinases and recapitulated in measures of kinase activity in intact cells. The most potent and selective erbB2 inhibitor of the analog series has anti-proliferative activity against an erbB2-overexpressing cell line that was lacking in the original EGFR-selective compound. Subtle changes to the molecular structure of ATP-competitive small molecule inhibitors of tyrosine kinases can yield dramatic changes in potency and selectivity. These results suggest that the discovery of highly selective small molecule inhibitors of very homologous kinases is achievable.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Bhattacharya SK,Cox ED,Kath JC,Mathiowetz AM,Morris J,Moyer JD,Pustilnik LR,Rafidi K,Richter DT,Su C,Wessel MD

doi

10.1016/s0006-291x(03)01160-4

subject

Has Abstract

pub_date

2003-07-25 00:00:00

pages

267-73

issue

2

eissn

0006-291X

issn

1090-2104

pii

S0006291X03011604

journal_volume

307

pub_type

杂志文章

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