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Literature DB >> 24964402

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

Peng Teng¹, Xiaolei Zhang, Haifan Wu, Qiao Qiao, Said M Sebti, Jianfeng Cai.

Abstract

From a γ-AApeptide-based one-bead-one-compound (OBOC) combinatorial library, we identified γ-AApeptides that can selectively inhibit STAT3-DNA interaction and suppress the expression levels of STAT3 target genes in intact cells. Our results demonstrate that in addition to the SH2 domain, the DNA binding domain of STAT3 is targetable for the development of a new generation of anti-cancer therapeutics.

Entities: CellLine Chemical Disease Gene Species

Mesh：

Substances：

Year: 2014 PMID： 24964402 PMCID： PMC4128407 DOI： 10.1039/c4cc03909b

Source DB: PubMed Journal: Chem Commun (Camb) ISSN： 1359-7345 Impact factor: 6.222

24 in total

1. Identification of a high-affinity phosphopeptide inhibitor of Stat3.

Authors: Zhiyong Ren; Larry A Cabell; Timothy S Schaefer; John S McMurray
Journal: Bioorg Med Chem Lett Date: 2003-02-24 Impact factor: 2.823

2. Alkylation of cysteine 468 in Stat3 defines a novel site for therapeutic development.

Authors: Ralf Buettner; Renzo Corzano; Rumana Rashid; Jianping Lin; Maheswari Senthil; Michael Hedvat; Anne Schroeder; Allen Mao; Andreas Herrmann; John Yim; Hongzhi Li; Yate-Ching Yuan; Kenichi Yakushijin; Fumiko Yakushijin; Nagarajan Vaidehi; Roger Moore; Gabriel Gugiu; Terry D Lee; Richard Yip; Yuan Chen; Richard Jove; David Horne; John C Williams
Journal: ACS Chem Biol Date: 2011-02-16 Impact factor: 5.100

3. Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts.

Authors: Xiaolei Zhang; Peibin Yue; Brent D G Page; Tianshu Li; Wei Zhao; Andrew T Namanja; David Paladino; Jihe Zhao; Yuan Chen; Patrick T Gunning; James Turkson
Journal: Proc Natl Acad Sci U S A Date: 2012-05-23 Impact factor: 11.205

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

Authors: Steven Fletcher; Brent D G Page; Xialoei Zhang; Peibin Yue; Zhi Hua Li; Sumaiya Sharmeen; Jagdeep Singh; Wei Zhao; Aaron D Schimmer; Suzanne Trudel; James Turkson; Patrick T Gunning
Journal: ChemMedChem Date: 2011-05-25 Impact factor: 3.466

5. Radiolabeled γ-AApeptides: a new class of tracers for positron emission tomography.

Authors: Yunan Yang; Youhong Niu; Hao Hong; Haifan Wu; Yin Zhang; Jonathan W Engle; Todd E Barnhart; Jianfeng Cai; Weibo Cai
Journal: Chem Commun (Camb) Date: 2012-07-02 Impact factor: 6.222

6. Synthesis of phosphatase-stable, cell-permeable peptidomimetic prodrugs that target the SH2 domain of Stat3.

Authors: Pijus K Mandal; Warren S-L Liao; John S McMurray
Journal: Org Lett Date: 2009-08-06 Impact factor: 6.005

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

Authors: Xiaolei Zhang; Ying Sun; Roberta Pireddu; Hua Yang; Murali K Urlam; Harshani R Lawrence; Wayne C Guida; Nicholas J Lawrence; Saïd M Sebti
Journal: Cancer Res Date: 2013-01-15 Impact factor: 12.701

8. An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects.

Authors: Khandaker A Z Siddiquee; Patrick T Gunning; Matthew Glenn; William P Katt; Shumin Zhang; Christopher Schrock; Christopher Schroeck; Said M Sebti; Richard Jove; Andrew D Hamilton; James Turkson
Journal: ACS Chem Biol Date: 2007-12-21 Impact factor: 5.100

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

1. Identification of a high-affinity phosphopeptide inhibitor of Stat3.

2. Alkylation of cysteine 468 in Stat3 defines a novel site for therapeutic development.

3. Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts.

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

5. Radiolabeled γ-AApeptides: a new class of tracers for positron emission tomography.

6. Synthesis of phosphatase-stable, cell-permeable peptidomimetic prodrugs that target the SH2 domain of Stat3.

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

8. An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects.

9. Lipidated cyclic γ-AApeptides display both antimicrobial and anti-inflammatory activity.

10. A biomimetic polyketide-inspired approach to small-molecule ligand discovery.

1. γ-AApeptides: Design, Structure, and Applications.

2. Aggregation-Induced Emissive and Circularly Polarized Homogeneous Sulfono-γ-AApeptide Foldamers.

Review 3. Structure and Function of AApeptides.

4. One-Bead-Two-Compound Thioether Bridged Macrocyclic γ-AApeptide Screening Library against EphA2.

5. γ-AApeptides as a New Class of Peptidomimetics.

Review 6. Tumor-targeting peptides from combinatorial libraries.