1l2e

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1l2e, resolution 1.75Å

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Human Kallikrein 6 (hK6) Active Form with benzamidine inhibitor

Overview

The human kallikreins are a large multigene family of closely related, serine-type proteases. In this regard, they are similar to the multigene, kallikrein families characterized in mice and rats. There is a much more, extensive body of knowledge regarding the function of mouse and rat, kallikreins in comparison with the human kallikreins. Human kallikrein 6, has been proposed as the homologue to rat myelencephalon-specific, protease, an arginine-specific degradative-type protease abundantly, expressed in the central nervous system and implicated in demyelinating, disease. We present the x-ray crystal structure of mature, active, recombinant human kallikrein 6 at 1.75-A resolution. This high resolution, model provides the first three-dimensional view of one of the human, kallikreins and one of only a few structures of serine proteases, predominantly expressed in the central nervous system. Enzymatic data are, presented that support the identification of human kallikrein 6 as the, functional homologue of rat myelencephalon-specific protease and are, corroborated by a molecular phylogenetic analysis. Furthermore, the x-ray, data provide support for the characterization of human kallikrein 6 as a, degradative protease with structural features more similar to trypsin than, the regulatory kallikreins.

About this Structure

1L2E is a Single protein structure of sequence from Homo sapiens with MG and BEN as ligands. Full crystallographic information is available from OCA.

Reference

Crystal structure and biochemical characterization of human kallikrein 6 reveals that a trypsin-like kallikrein is expressed in the central nervous system., Bernett MJ, Blaber SI, Scarisbrick IA, Dhanarajan P, Thompson SM, Blaber M, J Biol Chem. 2002 Jul 5;277(27):24562-70. Epub 2002 Apr 30. PMID:11983703

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