INHIBITION OF THE HER2 TYROSINE KINASE AND CHARACTERIZATION OF A HYDROPHOBIC SITE NEAR THE NUCLEOTIDE-BINDING DOMAIN

Authors
MADDRY JA KUSSNER C TRUSS JW NIWAS S WHITE EL KWONG CD
Citation
Ja. Maddry et al., INHIBITION OF THE HER2 TYROSINE KINASE AND CHARACTERIZATION OF A HYDROPHOBIC SITE NEAR THE NUCLEOTIDE-BINDING DOMAIN, Bioorganic & medicinal chemistry letters, 7(16), 1997, pp. 2109-2114
Citations number
49
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
16
Year of publication
1997
Pages
2109 - 2114
Database
ISI
SICI code
0960-894X(1997)7:16<2109:IOTHTK>2.0.ZU;2-Y
Abstract
A series of compounds was prepared to investigate the hydrophobic char acter of the HER2 receptor tyrosine kinase active site. These bisubstr ate analogs contained hydrophobic moieties in place of the polar triph osphate and nucleoside fragments of the natural ATP ligand. Despite th ese modifications, good affinity was observed as measured by inhibitio n of receptor autophosphorylation. (C) 1997 Elsevier Science Ltd.