Title

Isoform Selective Inhibition Of Stat1 Or Stat3 Homo-Dimerization Via Peptidomimetic Probes: Structural Recognition Of Stat Sh2 Domains

Keywords

Anti-cancer; Inhibitors; Peptidomimetics; SH2 domain recognition; STAT1; STAT3

Abstract

The identification of constitutively activated STAT (Signal Transducers and Activators of Transcription) proteins in aberrant cell signaling pathways has led to investigations targeting the selective disruption of specific STAT isoforms directly associated with oncogenisis. We have identified, through the design of a library of peptidomimetic inhibitors, agents that selectively disrupt STAT1 or STAT3 homo-dimerization at low micromolar concentrations. ISS840 has 20-fold higher inhibition of STAT1 homo-dimerization (IC50 value of 31 μM) relative to STAT3 (IC50 value of 560 μM). © 2007.

Publication Date

4-1-2007

Publication Title

Bioorganic and Medicinal Chemistry Letters

Volume

17

Issue

7

Number of Pages

1875-1878

Document Type

Article

Personal Identifier

scopus

DOI Link

https://doi.org/10.1016/j.bmcl.2007.01.077

Socpus ID

33847682326 (Scopus)

Source API URL

https://api.elsevier.com/content/abstract/scopus_id/33847682326

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