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

Authors

Yiyue Xie, Monash University
Jayme L. Dahlin, Brigham and Women's Hospital
Aaron J. Oakley, University of WollongongFollow
Marco G. Casarotto, Australian National University
Philip G. Board, Australian National University
Jonathan Baell, Nanjing Tech University, Monash UniversityFollow

RIS ID

130492

Publication Details

Xie, Y., Dahlin, J. L., Oakley, A. J., Casarotto, M. G., Board, P. G. & Baell, J. (2018). Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example. Journal Of Medicinal Chemistry, 61 (17), 7448-7470.

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.

Grant Number

NHMRC/1124673