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Discovery of novel STAT3 small molecule inhibitors via in silico site-directed fragment-based drug design.

Abstract：

:Constitutive activation of signal transducer and activator of transcription 3 (STAT3) has been validated as an attractive therapeutic target for cancer therapy. To stop both STAT3 activation and dimerization, a viable strategy is to design inhibitors blocking its SH2 domain phosphotyrosine binding site that is responsible for both actions. A new fragment-based drug design (FBDD) strategy, in silico site-directed FBDD, was applied in this study. A designed novel compound, 5,8-dioxo-6-(pyridin-3-ylamino)-5,8-dihydronaphthalene-1-sulfonamide (LY5), was confirmed to bind to STAT3 SH2 by fluorescence polarization assay. In addition, four out of the five chosen compounds have IC50 values lower than 5 μM for the U2OS cancer cells. 8 (LY5) has an IC50 range in 0.5-1.4 μM in various cancer cell lines. 8 also suppresses tumor growth in an in vivo mouse model. This study has demonstrated the utility of this approach and could be used to other drug targets in general.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Yu W,Xiao H,Lin J,Li C

doi

10.1021/jm400080c

subject

Has Abstract

pub_date

2013-06-13 00:00:00

pages

4402-12

issue

11

eissn

0022-2623

issn

1520-4804

journal_volume

56

pub_type

杂志文章

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