Literature DB >> 24418775

A biochemical screen for GroEL/GroES inhibitors.

Steven M Johnson1, Orzala Sharif2, Puiying Annie Mak2, Hsiao-Ting Wang2, Ingo H Engels2, Achim Brinker2, Peter G Schultz3, Arthur L Horwich4, Eli Chapman5.   

Abstract

High-throughput screening of 700,000 small molecules has identified 235 inhibitors of the GroEL/GroES-mediated refolding cycle. Dose-response analysis of a subset of these hits revealed that 21 compounds are potent inhibitors of GroEL/GroES-mediated refolding (IC50 <10 μM). The screening results presented herein represent the first steps in a broader aim of developing molecular probes to study chaperonin biochemistry and physiology.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Chaperonin; GroEL; GroES; High-throughput screening; Small molecule inhibitors

Mesh：

Substances：

Year:  2014        PMID： 24418775     DOI： 10.1016/j.bmcl.2013.12.100

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


  19 in total

1.  Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.

Authors:  Trent Kunkle; Sanofar Abdeen; Nilshad Salim; Anne-Marie Ray; Mckayla Stevens; Andrew J Ambrose; José Victorino; Yangshin Park; Quyen Q Hoang; Eli Chapman; Steven M Johnson
Journal:  J Med Chem       Date:  2018-11-15       Impact factor: 7.446

Review 2.  The Chemical Biology of Molecular Chaperones--Implications for Modulation of Proteostasis.

Authors:  Kristoffer R Brandvold; Richard I Morimoto
Journal:  J Mol Biol       Date:  2015-05-21       Impact factor: 5.469

3.  Withaferin A Analogs That Target the AAA+ Chaperone p97.

Authors:  Shasha Tao; Joseph Tillotson; E M Kithsiri Wijeratne; Ya-Ming Xu; MinJin Kang; Tongde Wu; Eric C Lau; Celestina Mesa; Damian J Mason; Robert V Brown; James J La Clair; A A Leslie Gunatilaka; Donna D Zhang; Eli Chapman
Journal:  ACS Chem Biol       Date:  2015-06-03       Impact factor: 5.100

4.  Sulfonamido-2-arylbenzoxazole GroEL/ES Inhibitors as Potent Antibacterials against Methicillin-Resistant Staphylococcus aureus (MRSA).

Authors:  Sanofar Abdeen; Trent Kunkle; Nilshad Salim; Anne-Marie Ray; Najiba Mammadova; Corey Summers; Mckayla Stevens; Andrew J Ambrose; Yangshin Park; Peter G Schultz; Arthur L Horwich; Quyen Q Hoang; Eli Chapman; Steven M Johnson
Journal:  J Med Chem       Date:  2018-08-14       Impact factor: 7.446

Review 5.  Mitigating risk in academic preclinical drug discovery.

Authors:  Jayme L Dahlin; James Inglese; Michael A Walters
Journal:  Nat Rev Drug Discov       Date:  2015-04       Impact factor: 84.694

6.  HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules.

Authors:  Mckayla Stevens; Sanofar Abdeen; Nilshad Salim; Anne-Marie Ray; Alex Washburn; Siddhi Chitre; Jared Sivinski; Yangshin Park; Quyen Q Hoang; Eli Chapman; Steven M Johnson
Journal:  Bioorg Med Chem Lett       Date:  2019-02-28       Impact factor: 2.823

7.  Leishmania donovani chaperonin 10 regulates parasite internalization and intracellular survival in human macrophages.

Authors:  Lucie Colineau; Joachim Clos; Kyung-Mee Moon; Leonard J Foster; Neil E Reiner
Journal:  Med Microbiol Immunol       Date:  2017-03-11       Impact factor: 3.402

8.  Dual-targeting GroEL/ES chaperonin and protein tyrosine phosphatase B (PtpB) inhibitors: A polypharmacology strategy for treating Mycobacterium tuberculosis infections.

Authors:  Alex Washburn; Sanofar Abdeen; Yulia Ovechkina; Anne-Marie Ray; Mckayla Stevens; Siddhi Chitre; Jared Sivinski; Yangshin Park; James Johnson; Quyen Q Hoang; Eli Chapman; Tanya Parish; Steven M Johnson
Journal:  Bioorg Med Chem Lett       Date:  2019-04-24       Impact factor: 2.823

9.  Analogs of nitrofuran antibiotics are potent GroEL/ES inhibitor pro-drugs.

Authors:  Mckayla Stevens; Chris Howe; Anne-Marie Ray; Alex Washburn; Siddhi Chitre; Jared Sivinski; Yangshin Park; Quyen Q Hoang; Eli Chapman; Steven M Johnson
Journal:  Bioorg Med Chem       Date:  2020-08-30       Impact factor: 3.641

10.  Characterization and function analysis of Hsp60 and Hsp10 under different acute stresses in black tiger shrimp, Penaeus monodon.

Authors:  Jinxuan Shi; Mingjun Fu; Chao Zhao; Falin Zhou; Qibin Yang; Lihua Qiu
Journal:  Cell Stress Chaperones       Date:  2015-12-04       Impact factor: 3.667
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