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Structure-Based Design of Conformationally Constrained, Cell-Permeable STAT3 Inhibitors.

ABSTRACT: We report herein the structure-based design of a class of conformationally constrained, potent, cell-permeable small-molecule inhibitors to target the SH2 domain in STAT3. Compound 11 (CJ-1383) binds to STAT3 with a K(i) value of 0.95 µM, dose-dependently inhibits cellular STAT3 signaling and cancer cell growth, and induces apoptosis in the MDA-MB-468 cancer cell line with constitutively activated STAT3.

SUBMITTER: Chen J

PROVIDER: S-EPMC2892918 | biostudies-literature | 2010 May

REPOSITORIES: biostudies-literature

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Structure-Based Design of Conformationally Constrained, Cell-Permeable STAT3 Inhibitors.

Chen Jianyong J Bai Longchuan L Bernard Denzil D Nikolovska-Coleska Zaneta Z Gomez Cindy C Zhang Jian J Yi Han H Wang Shaomeng S

ACS medicinal chemistry letters 20100501 2

We report herein the structure-based design of a class of conformationally constrained, potent, cell-permeable small-molecule inhibitors to target the SH2 domain in STAT3. Compound 11 (CJ-1383) binds to STAT3 with a K(i) value of 0.95 µM, dose-dependently inhibits cellular STAT3 signaling and cancer cell growth, and induces apoptosis in the MDA-MB-468 cancer cell line with constitutively activated STAT3. ...[more]

PMID: 20596242

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