Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Discovery and Optimization of Selective Inhibitors of Meprin α (Part II)

Version 1 : Received: 14 December 2020 / Approved: 15 December 2020 / Online: 15 December 2020 (12:56:31 CET)

A peer-reviewed article of this Preprint also exists.

Wang, C.; Diez, J.; Park, H.; Spicer, T.P.; Scampavia, L.D.; Becker-Pauly, C.; Fields, G.B.; Minond, D.; Bannister, T.D. Discovery and Optimization of Selective Inhibitors of Meprin α (Part II). Pharmaceuticals 2021, 14, 197. Wang, C.; Diez, J.; Park, H.; Spicer, T.P.; Scampavia, L.D.; Becker-Pauly, C.; Fields, G.B.; Minond, D.; Bannister, T.D. Discovery and Optimization of Selective Inhibitors of Meprin α (Part II). Pharmaceuticals 2021, 14, 197.

Journal reference: Pharmaceuticals 2021, 14, 197
DOI: 10.3390/ph14030197

Abstract

Meprin α is a zinc metalloproteinase (metzincin) that has been implicated in multiple diseases, including fibrosis and cancers. It has proven difficult to find small molecules that are capable of selectively inhibiting meprin α, or its close relative meprin β, over numerous other metzincins which, if inhibited, would elicit unwanted effects. We recently identified possible molecular starting points for meprin α-specific inhibition through an HTS effort (see part I, preceding paper). In part II we report the optimization of a potent and selective hydroxamic acid meprin α inhibitor probe which may help define the therapeutic potential for small molecule meprin α inhibition and spur further drug discovery efforts in the area of zinc metalloproteinase inhibition.

Keywords

meprin α; meprin β; zinc metalloproteinase; medicinal chemistry; probe development

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