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Title 

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

Authors 

Hyae Kyeong KimJi Youn NamMi Young HanKwang Hee SonJung Do ChoiByoung-Mog KwonHana L TakusagawaYafei HuangFusao Takusagawa

Publisher 

Elsevier

Issue Date 

2000

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 10, no. 13, pp. 1455-1457

Keywords 

actinomycin derivativecactinomycindactinomycinphosphopeptidebinding affinitycomparative studydrug inhibitiondrug protein bindingdrug synthesisprotein domain

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

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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