Identification of a non-phosphorylated, cell permeable, small molecule ligand for the Stat3 SH2 domain
نویسندگان
چکیده
منابع مشابه
Identification of novel non-phosphorylated ligands, which bind selectively to the SH2 domain of Grb7.
Grb7 is an adapter-type signaling protein, which is recruited via its SH2 domain to a variety of receptor tyrosine kinases (RTKs), including ErbB2 and ErbB3. It is overexpressed in breast, esophageal, and gastric cancers, and may contribute to the invasive potential of cancer cells. Molecular interactions involving Grb7 therefore provide attractive targets for therapeutic intervention. We have ...
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A 396-member peptide-hybrid small molecule microarray was fabricated to profile small molecule ligands across 15 SH2 proteins, revealing hits against Lck and Grb2.
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Signal transducer and activator of transcription 3 (STAT3) plays important roles in multiple aspects of cancer aggressiveness including migration, invasion, survival, self-renewal, angiogenesis, and tumor cell immune evasion by regulating the expression of multiple downstream target genes. STAT3 is constitutively activated in many malignant tumors and its activation is associated with high hist...
متن کاملProbing the effect of conformational constraint on phosphorylated ligand binding to an SH2 domain using polarizable force field simulations.
Preorganizing a ligand in the conformation it adopts upon binding to a protein has long been considered to be an effective way to improve affinity by making the binding entropy more favorable. However, recent thermodynamic studies of a series of complexes of the Grb2 SH2 domain with peptide analogues having constrained and flexible replacements for a phosphotyrosine residue revealed that less f...
متن کاملCharacterizing protein domain associations by Small-molecule ligand binding.
BACKGROUND Protein domains are evolutionarily conserved building blocks for protein structure and function, which are conventionally identified based on protein sequence or structure similarity. Small molecule binding domains are of great importance for the recognition of small molecules in biological systems and drug development. Many small molecules, including drugs, have been increasingly id...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2011
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2011.06.056