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

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Title
Natural and synthetic analogues of actinomycin D as Grb2-SH2 domain blockers
Author(s)
Hyae Kyeong Kim; Ji Youn Nam; Mi Young Han; Kwang Hee Son; Jung Do Choi; Byoung-Mog Kwon; Hana L Takusagawa; Yafei Huang; Fusao Takusagawa
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 10, no. 13, pp. 1455-1457
Publication Year
2000
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.
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/S0960-894X(00)00258-4
Type
Article
Appears in Collections:
Division of Biomedical Research > Microbiome Convergence Research Center > 1. Journal Articles
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