Title of article
Natural and synthetic analogues of actinomycin D as Grb2-SH2 domain blockers
Author/Authors
Hyae-Kyeong Kim، نويسنده , , Ji-Youn Nam، نويسنده , , Mi Young Han، نويسنده , , Kwang-Hee Son، نويسنده , , Jung-Do Choi، نويسنده , , Byoung-Mog Kwon، نويسنده , , Hana L. Takusagawa، نويسنده , , Yafei Huang، نويسنده , , Fusao Takusagawa، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
3
From page
1455
To page
1457
Abstract
Natural analogues (D, C2, and VII) of actinomycin inhibit Grb2 SH2 domain binding with phosphopeptide-derived from Shc in vitro and in intracellular system. 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 μM, respectively.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790895
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