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

Journal Article


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.

Authors


  •   Xie, Yiyue (external author)
  •   Dahlin, Jayme L. (external author)
  •   Oakley, Aaron J.
  •   Casarotto, Marco G. (external author)
  •   Board, Philip G. (external author)
  •   Baell, Jonathan (external author)

Publication Date


  • 2018

Citation


  • 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.

Scopus Eid


  • 2-s2.0-85046440114

Number Of Pages


  • 22

Start Page


  • 7448

End Page


  • 7470

Volume


  • 61

Issue


  • 17

Place Of Publication


  • United States

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.

Authors


  •   Xie, Yiyue (external author)
  •   Dahlin, Jayme L. (external author)
  •   Oakley, Aaron J.
  •   Casarotto, Marco G. (external author)
  •   Board, Philip G. (external author)
  •   Baell, Jonathan (external author)

Publication Date


  • 2018

Citation


  • 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.

Scopus Eid


  • 2-s2.0-85046440114

Number Of Pages


  • 22

Start Page


  • 7448

End Page


  • 7470

Volume


  • 61

Issue


  • 17

Place Of Publication


  • United States