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Potent inhibition of Ca2+-dependent activation of calpain-1 by novel mercaptoacrylates

Adams, Sarah Elizabeth, Parr, Christian, Miller, David James, Allemann, Rudolf Konrad ORCID: and Hallett, Maurice Bartlett ORCID: 2012. Potent inhibition of Ca2+-dependent activation of calpain-1 by novel mercaptoacrylates. MedChemComm 3 (5) , pp. 566-570. 10.1039/c2md00280a

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Calpain-1 is a Ca2+-activated cytosolic cysteine protease. Its activation has been linked to extravasation into inflamed tissue of white blood cells, especially neutrophils. Calpain-1 may therefore be an anti-inflammatory target for therapeutic intervention. 24 novel monohalogenated phenyl and indole mercaptoacrylic acid derivatives were synthesised. The location and nature of the ring-coupled halides strongly influenced the potency of these compounds to inhibit calpain activation. Several of the calpain-1 inhibitors showed IC50 values in the low nanomolar range and prevented cell shape change of neutrophils, a necessary prelude to their migration from the blood in the body.

Item Type: Article
Status: Published
Schools: Chemistry
Cardiff Catalysis Institute (CCI)
Subjects: Q Science > QD Chemistry
Publisher: RSC Publishing
ISSN: 2040-2503
Funders: EPSRC, MRC
Last Modified: 20 Oct 2022 08:07

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