Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example

Yiyue Xie, Jayme L. Dahlin, Aaron J. Oakley, Marco G. Casarotto, Philip G. Board, Jonathan B. Baell

Research output: Contribution to journalReview ArticleResearchpeer-review

8 Citations (Scopus)

Abstract

Early stage drug discovery reporting on relatively new or difficult targets is often associated with insufficient hit triage. Literature reviews of such targets seldom delve into the detail required to critically analyze the associated screening hits reported. Here we take the enzyme glutathione transferase omega-1 (GSTO1-1) as an example of a relatively difficult target and review the associated literature involving small-molecule inhibitors. As part of this process we deliberately pay closer-than-usual attention to assay interference and hit quality aspects. We believe this Perspective will be a useful guide for future development of GSTO1-1 inhibitors, as well serving as a template for future review formats of new or difficult targets.

Original languageEnglish
Pages (from-to)7448-7470
Number of pages23
JournalJournal of Medicinal Chemistry
Volume61
Issue number17
DOIs
Publication statusPublished - 13 Sep 2018

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