Literature DB >> 19215087

Discovery of novel Myc-Max heterodimer disruptors with a three-dimensional pharmacophore model.

Gabriela Mustata1, Ariele Viacava Follis, Dalia I Hammoudeh, Steven J Metallo, Huabo Wang, Edward V Prochownik, John S Lazo, Ivet Bahar.   

Abstract

A three-dimensional pharmacophore model was generated utilizing a set of known inhibitors of c-Myc-Max heterodimer formation. The model successfully identified a set of structurally diverse compounds with potential inhibitory activity against c-Myc. Nine compounds were tested in vitro, and four displayed affinities in the micromolar range and growth inhibitory activity against c-Myc-overexpressing cells. These studies demonstrate the applicability of pharmacophore modeling to the identification of novel and potentially more puissant inhibitors of the c-Myc oncoprotein.

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Year:  2009        PMID: 19215087      PMCID: PMC2765518          DOI: 10.1021/jm801278g

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  25 in total

Review 1.  The human CYP3A subfamily: practical considerations.

Authors:  S A Wrighton; E G Schuetz; K E Thummel; D D Shen; K R Korzekwa; P B Watkins
Journal:  Drug Metab Rev       Date:  2000 Aug-Nov       Impact factor: 4.518

Review 2.  Fragmental methods in the analysis of biological activities of diverse compound sets.

Authors:  P Japertas; R Didziapetris; A Petrauskas
Journal:  Mini Rev Med Chem       Date:  2003-12       Impact factor: 3.862

3.  Do structurally similar molecules have similar biological activity?

Authors:  Yvonne C Martin; James L Kofron; Linda M Traphagen
Journal:  J Med Chem       Date:  2002-09-12       Impact factor: 7.446

4.  Using a staged multi-objective optimization approach to find selective pharmacophore models.

Authors:  Robert D Clark; Edmond Abrahamian
Journal:  J Comput Aided Mol Des       Date:  2008-07-29       Impact factor: 3.686

5.  Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts.

Authors:  Thorsten Berg; Steven B Cohen; Joel Desharnais; Corinna Sonderegger; Daniel J Maslyar; Joel Goldberg; Dale L Boger; Peter K Vogt
Journal:  Proc Natl Acad Sci U S A       Date:  2002-03-12       Impact factor: 11.205

Review 6.  c-Myc as a therapeutic target in cancer.

Authors:  Edward V Prochownik
Journal:  Expert Rev Anticancer Ther       Date:  2004-04       Impact factor: 4.512

7.  Transcriptional activation by the human c-Myc oncoprotein in yeast requires interaction with Max.

Authors:  B Amati; S Dalton; M W Brooks; T D Littlewood; G I Evan; H Land
Journal:  Nature       Date:  1992-10-01       Impact factor: 49.962

8.  Low molecular weight inhibitors of Myc-Max interaction and function.

Authors:  Xiaoying Yin; Christine Giap; John S Lazo; Edward V Prochownik
Journal:  Oncogene       Date:  2003-09-18       Impact factor: 9.867

9.  Oncogenic activity of the c-Myc protein requires dimerization with Max.

Authors:  B Amati; M W Brooks; N Levy; T D Littlewood; G I Evan; H Land
Journal:  Cell       Date:  1993-01-29       Impact factor: 41.582

10.  The c-Myc protein induces cell cycle progression and apoptosis through dimerization with Max.

Authors:  B Amati; T D Littlewood; G I Evan; H Land
Journal:  EMBO J       Date:  1993-12-15       Impact factor: 11.598

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  38 in total

Review 1.  Understanding protein non-folding.

Authors:  Vladimir N Uversky; A Keith Dunker
Journal:  Biochim Biophys Acta       Date:  2010-02-01

Review 2.  Intrinsically disordered proteins are potential drug targets.

Authors:  Steven J Metallo
Journal:  Curr Opin Chem Biol       Date:  2010-07-02       Impact factor: 8.822

Review 3.  Oncogenic protein interfaces: small molecules, big challenges.

Authors:  Tracy L Nero; Craig J Morton; Jessica K Holien; Jerome Wielens; Michael W Parker
Journal:  Nat Rev Cancer       Date:  2014-03-13       Impact factor: 60.716

Review 4.  Pathological unfoldomics of uncontrolled chaos: intrinsically disordered proteins and human diseases.

Authors:  Vladimir N Uversky; Vrushank Davé; Lilia M Iakoucheva; Prerna Malaney; Steven J Metallo; Ravi Ramesh Pathak; Andreas C Joerger
Journal:  Chem Rev       Date:  2014-05-15       Impact factor: 60.622

5.  cMyc-p53 feedback mechanism regulates the dynamics of T lymphocytes in the immune response.

Authors:  Harsha S Madapura; Daniel Salamon; Klas G Wiman; Sonia Lain; Eva Klein; Noémi Nagy
Journal:  Cell Cycle       Date:  2016-05-02       Impact factor: 4.534

6.  Harnessing Human Microphysiology Systems as Key Experimental Models for Quantitative Systems Pharmacology.

Authors:  D Lansing Taylor; Albert Gough; Mark E Schurdak; Lawrence Vernetti; Chakra S Chennubhotla; Daniel Lefever; Fen Pei; James R Faeder; Timothy R Lezon; Andrew M Stern; Ivet Bahar
Journal:  Handb Exp Pharmacol       Date:  2019

Review 7.  A complex task? Direct modulation of transcription factors with small molecules.

Authors:  Angela N Koehler
Journal:  Curr Opin Chem Biol       Date:  2010-04-13       Impact factor: 8.822

Review 8.  Targeting intrinsically disordered proteins in neurodegenerative and protein dysfunction diseases: another illustration of the D(2) concept.

Authors:  Vladimir N Uversky
Journal:  Expert Rev Proteomics       Date:  2010-08       Impact factor: 3.940

9.  Therapeutic Targeting of Myc.

Authors:  Edward V Prochownik; Peter K Vogt
Journal:  Genes Cancer       Date:  2010-06

10.  A quantitative, surface plasmon resonance-based approach to evaluating DNA binding by the c-Myc oncoprotein and its disruption by small molecule inhibitors.

Authors:  Huabo Wang; Anand Ramakrishnan; Steven Fletcher; Edward V Prochownik
Journal:  J Biol Methods       Date:  2015
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