Natural and synthetic analogues of actinomycin D as Grb2-SH2 domain blockers

Authors
Kim, HK Nam, JY Han, MY Son, KH Choi, JD Kwon, BM Takusagawa, HL Huang, YF Takusagawa, F
Citation
Hk. Kim et al., Natural and synthetic analogues of actinomycin D as Grb2-SH2 domain blockers, BIOORG MED, 10(13), 2000, pp. 1455-1457
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
13
Year of publication
2000
Pages
1455 - 1457
Database
ISI
SICI code
0960-894X(20000703)10:13<1455:NASAOA>2.0.ZU;2-B
Abstract
Natural analogues (D, C2, and VII) of actinomycin inhibit Grb2 SH2 domain b inding with phosphopeptide-derived from Shc in vitro and in intracellular s ystem. To study structure-activity relationships, 13 actinomycin analogues were synthesized and we found that the inhibition activity depended on the substituents of cyclic peptide groups in actinomycin and two analogues with Tyr residue are the most potent inhibitors with IC50 value of 0.5 and 0.8 mu M, respectively. (C) 2000 Elsevier Science Ltd. All rights reserved.