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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
- Full Text Link
- http://dx.doi.org/10.1016/S0960-894X(00)00258-4
- Type
- Article
- Appears in Collections:
- Division of A.I. & Biomedical Research > Microbiome Convergence Research Center > 1. Journal Articles
- Files in This Item:
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