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Alternative ways of modulating JAK-STAT pathway: Looking beyond phosphorylation.


ABSTRACT: Most attempts to develop inhibitors of STAT transcription factors target either activating phosphorylation of tyrosine residue or SH2 domains. However, all six domains of STATs are highly conserved between the species and play important roles in the function of this family of transcription factors. STATs are involved in numerous protein-protein interactions that are likely to regulate and fine tune transcriptional activity. Targeting these interactions can provide plentiful opportunities for the discovery of novel drug candidates and powerful chemical biology tools. Using N-terminal domains as an example we describe alternative rational approaches to the development of modulators of JAK-STAT signaling.

SUBMITTER: Timofeeva OA 

PROVIDER: S-EPMC3670285 | biostudies-literature | 2012 Oct

REPOSITORIES: biostudies-literature

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Alternative ways of modulating JAK-STAT pathway: Looking beyond phosphorylation.

Timofeeva Olga A OA   Tarasova Nadya I NI  

JAK-STAT 20121001 4


Most attempts to develop inhibitors of STAT transcription factors target either activating phosphorylation of tyrosine residue or SH2 domains. However, all six domains of STATs are highly conserved between the species and play important roles in the function of this family of transcription factors. STATs are involved in numerous protein-protein interactions that are likely to regulate and fine tune transcriptional activity. Targeting these interactions can provide plentiful opportunities for the  ...[more]

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