Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor

Kavya Ramkumar; Soma Samanta; Anahita Kyani; Suhui Yang; Shuzo Tamura; Elizabeth Ziemke; Jeanne A. Stuckey; Si Li; Krishnapriya Chinnaswamy; Hiroyuki Otake; Bikash Debnath; Vladimir Yarovenko; Judith S. Sebolt-Leopold; Mats Ljungman; Nouri Neamati

doi:10.1038/ncomms13084

Nature Communications (Oct 2016)

Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor

Kavya Ramkumar,
Soma Samanta,
Anahita Kyani,
Suhui Yang,
Shuzo Tamura,
Elizabeth Ziemke,
Jeanne A. Stuckey,
Si Li,
Krishnapriya Chinnaswamy,
Hiroyuki Otake,
Bikash Debnath,
Vladimir Yarovenko,
Judith S. Sebolt-Leopold,
Mats Ljungman,
Nouri Neamati

Affiliations

Kavya Ramkumar: Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California
Soma Samanta: Department of Medicinal Chemistry, College of Pharmacy, University of Michigan
Anahita Kyani: Department of Medicinal Chemistry, College of Pharmacy, University of Michigan
Suhui Yang: Department of Medicinal Chemistry, College of Pharmacy, University of Michigan
Shuzo Tamura: Department of Medicinal Chemistry, College of Pharmacy, University of Michigan
Elizabeth Ziemke: Translational Oncology Program, University of Michigan
Jeanne A. Stuckey: Life Sciences Institute, University of Michigan
Si Li: Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California
Krishnapriya Chinnaswamy: Life Sciences Institute, University of Michigan
Hiroyuki Otake: Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California
Bikash Debnath: Department of Medicinal Chemistry, College of Pharmacy, University of Michigan
Vladimir Yarovenko: N.D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences
Judith S. Sebolt-Leopold: Translational Oncology Program, University of Michigan
Mats Ljungman: Translational Oncology Program, University of Michigan
Nouri Neamati: Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California

DOI: https://doi.org/10.1038/ncomms13084
Journal volume & issue: Vol. 7, no. 1
pp. 1 – 13

Abstract

Read online

Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform overexpressed in several cancers that has been implicated in drug resistance. Here the authors identify a small molecule inhibitor of GSTO1 that effectively inhibits tumor growth in colon cancer models, and establish its mechanism of action.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

About the journal