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

*Corresponding author for this work

    Research output: Contribution to journalReview articlepeer-review

    12 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 Sept 2018

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