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Literature DB >> 12639546

Identification of a high-affinity phosphopeptide inhibitor of Stat3.

Zhiyong Ren¹, Larry A Cabell, Timothy S Schaefer, John S McMurray.

Abstract

Stat3 is a latent transcription factor that exhibits elevated activity in a variety of human cancers. To find a lead peptide for peptidomimetic drug development we synthesized and tested phosphopeptides derived from known receptor docking sites and found Y(p)LPQTV as the optimal sequence. SAR studies showed that each residue from pY to pY+3 provided binding energy.

Entities: Disease Gene Species

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Year: 2003 PMID： 12639546 DOI： 10.1016/s0960-894x(02)01050-8

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

47 in total

1. Dietary compounds as potent inhibitors of the signal transducers and activators of transcription (STAT) 3 regulatory network.

Authors: Anne Trécul; Franck Morceau; Mario Dicato; Marc Diederich
Journal: Genes Nutr Date: 2012-01-25 Impact factor: 5.523

2. Solid-phase synthesis of Stat3 inhibitors incorporating O-carbamoylserine and O-carbamoylthreonine as glutamine mimics.

Authors: Pijus K Mandal; Patricia A Heard; Zhiyong Ren; Xiaomin Chen; John S McMurray
Journal: Bioorg Med Chem Lett Date: 2006-11-06 Impact factor: 2.823

Review 3. Targeting STAT3 in cancer: how successful are we?

Authors: Peibin Yue; James Turkson
Journal: Expert Opin Investig Drugs Date: 2009-01 Impact factor: 6.206

4. Conformationally constrained peptidomimetic inhibitors of signal transducer and activator of transcription. 3: Evaluation and molecular modeling.

Authors: Pijus K Mandal; Donald Limbrick; David R Coleman; Garrett A Dyer; Zhiyong Ren; J Sanderson Birtwistle; Chiyi Xiong; Xiaomin Chen; James M Briggs; John S McMurray
Journal: J Med Chem Date: 2009-04-23 Impact factor: 7.446

Identification of a high-affinity phosphopeptide inhibitor of Stat3.

1. Dietary compounds as potent inhibitors of the signal transducers and activators of transcription (STAT) 3 regulatory network.

2. Solid-phase synthesis of Stat3 inhibitors incorporating O-carbamoylserine and O-carbamoylthreonine as glutamine mimics.

Review 3. Targeting STAT3 in cancer: how successful are we?

4. Conformationally constrained peptidomimetic inhibitors of signal transducer and activator of transcription. 3: Evaluation and molecular modeling.

Review 5. Therapeutic modulators of STAT signalling for human diseases.

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

7. Antagonism of the Stat3-Stat3 protein dimer with salicylic acid based small molecules.

8. A novel inhibitor of STAT3 homodimerization selectively suppresses STAT3 activity and malignant transformation.

Review 9. Targeting SH2 domains in breast cancer.

10. Identification of novel inhibitors that disrupt STAT3-DNA interaction from a γ-AApeptide OBOC combinatorial library.