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

journal contribution
posted on 2024-11-16, 03:25 authored by Yiyue Xie, Jayme L Dahlin, Aaron OakleyAaron Oakley, Marco G Casarotto, Philip G Board, Jonathan Baell
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.

Funding

Glutathione transferase Omega 1 as a novel target for sepsis and other inflammatory disorders.

National Health and Medical Research Council

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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.

Journal title

Journal of Medicinal Chemistry

Volume

61

Issue

17

Pagination

7448-7470

Language

English

RIS ID

130492

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