Literature DB >> 20158203

Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1.

Paul H Bernardo1, Thirunavukkarasu Sivaraman, Kah-Fei Wan, Jin Xu, Janarthanan Krishnamoorthy, Chun Meng Song, Liming Tian, Jasmine S F Chin, Diane S W Lim, Henry Y K Mok, Victor C Yu, Joo Chuan Tong, Christina L L Chai.   

Abstract

The screening of a small focused library of rhodanine derivatives as inhibitors of Bcl-2 proteins led to the discovery of two structurally related compounds with different binding profiles against the Bcl-XL and the Mcl-1 proteins. Subsequent NMR studies with mutant proteins and in silico docking studies provide a possible rationale for the observed specificity.

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Year:  2010        PMID： 20158203     DOI： 10.1021/jm901469p

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


  17 in total

1.  Design, synthesis and evaluation of marinopyrrole derivatives as selective inhibitors of Mcl-1 binding to pro-apoptotic Bim and dual Mcl-1/Bcl-xL inhibitors.

Authors:  Chunwei Cheng; Maria E Balasis; Yan Liu; Thomas P Garner; Rongshi Li; Kenyon G Daniel; Jerry Li; Yong Qin; Evripidis Gavathiotis; Said M Sebti
Journal:  Eur J Med Chem       Date:  2014-11-20       Impact factor: 6.514

2.  Three-component, one-flask synthesis of rhodanines (thiazolidinones).

Authors:  Alexander M Jacobine; Gary H Posner
Journal:  J Org Chem       Date:  2011-08-31       Impact factor: 4.354

Review 3.  Anticancer Profile of Rhodanines: Structure-Activity Relationship (SAR) and Molecular Targets-A Review.

Authors:  Jacek Szczepański; Helena Tuszewska; Nazar Trotsko
Journal:  Molecules       Date:  2022-06-10       Impact factor: 4.927

Review 4.  Small molecule Mcl-1 inhibitors for the treatment of cancer.

Authors:  Johannes Belmar; Stephen W Fesik
Journal:  Pharmacol Ther       Date:  2014-08-27       Impact factor: 12.310

Review 5.  Targeting MCL-1 in hematologic malignancies: Rationale and progress.

Authors:  Andrew H Wei; Andrew W Roberts; Andrew Spencer; Aaron Seth Rosenberg; David Siegel; Roland B Walter; Sean Caenepeel; Paul Hughes; Zach McIver; Khalid Mezzi; Phuong Khanh Morrow; Anthony Stein
Journal:  Blood Rev       Date:  2020-02-21       Impact factor: 8.250

6.  Evaluation and critical assessment of putative MCL-1 inhibitors.

Authors:  S Varadarajan; M Vogler; M Butterworth; D Dinsdale; L D Walensky; G M Cohen
Journal:  Cell Death Differ       Date:  2013-07-05       Impact factor: 15.828

7.  Selectivity by small-molecule inhibitors of protein interactions can be driven by protein surface fluctuations.

Authors:  David K Johnson; John Karanicolas
Journal:  PLoS Comput Biol       Date:  2015-02-23       Impact factor: 4.475

8.  Stapled BH3 peptides against MCL-1: mechanism and design using atomistic simulations.

Authors:  Thomas L Joseph; David P Lane; Chandra S Verma
Journal:  PLoS One       Date:  2012-08-31       Impact factor: 3.240

9.  Molecular interactions of prodiginines with the BH3 domain of anti-apoptotic Bcl-2 family members.

Authors:  Ali Hosseini; Margarita Espona-Fiedler; Vanessa Soto-Cerrato; Roberto Quesada; Ricardo Pérez-Tomás; Victor Guallar
Journal:  PLoS One       Date:  2013-02-27       Impact factor: 3.240

10.  3-Substituted-N-(4-hydroxynaphthalen-1-yl)arylsulfonamides as a novel class of selective Mcl-1 inhibitors: structure-based design, synthesis, SAR, and biological evaluation.

Authors:  Fardokht A Abulwerdi; Chenzhong Liao; Ahmed S Mady; Jordan Gavin; Chenxi Shen; Tomasz Cierpicki; Jeanne A Stuckey; H D Hollis Showalter; Zaneta Nikolovska-Coleska
Journal:  J Med Chem       Date:  2014-05-07       Impact factor: 7.446
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