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Curr Opin Drug Discov Devel. 2005 Nov;8(6):684-700.

Developments in the design and synthesis of calpain inhibitors.

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University of Canterbury, Department of Chemistry, Christchurch 8020, New Zealand.


Calpains are Ca(2+)-dependent cysteine proteases that play an important role in cell differentiation and in apoptosis/necrosis. The overactivation of calpain is connected with a number of diseases, including cataracts and traumatic brain injury, making calpain an attractive drug target. The development of selective inhibitors of calpain has, however, proved difficult, due to a lack of detailed structural information on the protein. This difficulty has been somewhat alleviated with recent reports on the X-ray crystal structures of engineered calpains and improved biochemical characterization of the protein. This review describes properties and X-ray crystal structures of calpain, and the synthesis and binding affinities of novel calpain inhibitors.

[Indexed for MEDLINE]

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