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January 1, 2022Chemical ScienceOpen Access

Salicylate metal-binding isosteres as fragments for metalloenzyme inhibition

Moritz K. Jackl Hyeonglim Seo Johannes Karges Mark Kalaj Seth M. Cohen

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Abstract

). It was observed that salicylate MBIs could maintain or improve enzyme inhibition and selectivity. To probe salicylate MBIs as fragments for fragment-based drug discovery (FBDD), an MBI that showed good inhibitory activity against GLO1 was derivatized and a rudimentary structure-activity relationship was developed. The resulting elaborated fragments showed GLO1 inhibition with low micromolar activity.

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Jackl et al. (2022) studied this question.

synapsesocial.com/papers/69f41c50ce7a9e1da9d4005b https://doi.org/10.1039/d1sc06011b

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