Literature DB >> 20596242

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

Jianyong Chen1, Longchuan Bai, Denzil Bernard, Zaneta Nikolovska-Coleska, Cindy Gomez, Jian Zhang, Han Yi, Shaomeng Wang.   

Abstract

We report herein the structure-based design of a class of conformationally constrained, potent, cell-permeable small-molecule inhibitors to target the SH2 domain in STAT3. Compound 11 (CJ-1383) binds to STAT3 with a K(i) value of 0.95 µM, dose-dependently inhibits cellular STAT3 signaling and cancer cell growth, and induces apoptosis in the MDA-MB-468 cancer cell line with constitutively activated STAT3.

Entities:  

Year:  2010        PMID： 20596242      PMCID： PMC2892918          DOI： 10.1021/ml100010j

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  25 in total

Review 1.  Transcription factors as targets for cancer therapy.

Authors:  James E Darnell
Journal:  Nat Rev Cancer       Date:  2002-10       Impact factor: 60.716

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

3.  Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.

Authors:  Patrick T Gunning; William P Katt; Matthew Glenn; Khandaker Siddiquee; Khandaker Siddique; Joon S Kim; Richard Jove; Saïd M Sebti; James Turkson; Andrew D Hamilton
Journal:  Bioorg Med Chem Lett       Date:  2007-01-27       Impact factor: 2.823

4.  Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors.

Authors:  Cindy Gomez; Longchuan Bai; Jian Zhang; Zaneta Nikolovska-Coleska; Jianyong Chen; Han Yi; Shaomeng Wang
Journal:  Bioorg Med Chem Lett       Date:  2009-01-31       Impact factor: 2.823

Review 5.  The role of STATs in transcriptional control and their impact on cellular function.

Authors:  J Bromberg; J E Darnell
Journal:  Oncogene       Date:  2000-05-15       Impact factor: 9.867

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.  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

8.  Structural requirements for signal transducer and activator of transcription 3 binding to phosphotyrosine ligands containing the YXXQ motif.

Authors:  Huang Shao; Xuejun Xu; Mary-Ann A Mastrangelo; Naijie Jing; Richard G Cook; Glen B Legge; David J Tweardy
Journal:  J Biol Chem       Date:  2004-02-13       Impact factor: 5.157

9.  Novel peptidomimetic inhibitors of signal transducer and activator of transcription 3 dimerization and biological activity.

Authors:  James Turkson; Joon S Kim; Shumin Zhang; Jing Yuan; Mei Huang; Matthew Glenn; Eric Haura; Said Sebti; Andrew D Hamilton; Richard Jove
Journal:  Mol Cancer Ther       Date:  2004-03       Impact factor: 6.261

10.  New syntheses of tetrazolylmethylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors.

Authors:  Jennifer Dourlat; Bruno Valentin; Wang-Qing Liu; Christiane Garbay
Journal:  Bioorg Med Chem Lett       Date:  2007-05-03       Impact factor: 2.823
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  35 in total

Review 1.  Therapeutic modulators of STAT signalling for human diseases.

Authors:  Gabriella Miklossy; Tyvette S Hilliard; James Turkson
Journal:  Nat Rev Drug Discov       Date:  2013-08       Impact factor: 84.694

2.  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

3.  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

4.  Potent and selective phosphopeptide mimetic prodrugs targeted to the Src homology 2 (SH2) domain of signal transducer and activator of transcription 3.

Authors:  Pijus K Mandal; Fengqin Gao; Zhen Lu; Zhiyong Ren; Rajagopal Ramesh; J Sanderson Birtwistle; Kumaralal K Kaluarachchi; Xiaomin Chen; Robert C Bast; Warren S Liao; John S McMurray
Journal:  J Med Chem       Date:  2011-04-26       Impact factor: 7.446

5.  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

6.  Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors.

Authors:  Francisco Lopez-Tapia; Christine Brotherton-Pleiss; Peibin Yue; Heide Murakami; Ana Carolina Costa Araujo; Bruna Reis Dos Santos; Erin Ichinotsubo; Anna Rabkin; Raj Shah; Megan Lantz; Suzie Chen; Marcus A Tius; James Turkson
Journal:  ACS Med Chem Lett       Date:  2018-02-16       Impact factor: 4.345

7.  Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents.

Authors:  Haijun Chen; Zhengduo Yang; Chunyong Ding; Lili Chu; Yusong Zhang; Kristin Terry; Huiling Liu; Qiang Shen; Jia Zhou
Journal:  ACS Med Chem Lett       Date:  2013-01-15       Impact factor: 4.345

Review 8.  Distinct roles of STAT3 and STAT5 in the pathogenesis and targeted therapy of breast cancer.

Authors:  Sarah R Walker; Michael Xiang; David A Frank
Journal:  Mol Cell Endocrinol       Date:  2013-03-24       Impact factor: 4.102

9.  A phosphopeptide mimetic prodrug targeting the SH2 domain of Stat3 inhibits tumor growth and angiogenesis.

Authors:  Edmond J Auzenne; Jim Klostergaard; Pijus K Mandal; Warren S Liao; Zhen Lu; Fengqin Gao; Robert C Bast; Fredika M Robertson; John S McMurray
Journal:  J Exp Ther Oncol       Date:  2012

10.  Hirsutinolide Series Inhibit Stat3 Activity, Alter GCN1, MAP1B, Hsp105, G6PD, Vimentin, TrxR1, and Importin α-2 Expression, and Induce Antitumor Effects against Human Glioma.

Authors:  Gabriella Miklossy; Ui Joung Youn; Peibin Yue; Mingming Zhang; Chih-Hong Chen; Tyvette S Hilliard; David Paladino; Yifei Li; Justin Choi; Jann N Sarkaria; Joel K Kawakami; Supakit Wongwiwatthananukit; Yuan Chen; Dianqing Sun; Leng Chee Chang; James Turkson
Journal:  J Med Chem       Date:  2015-09-17       Impact factor: 7.446
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