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1eax

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{{STRUCTURE_1eax| PDB=1eax | SCENE= }}
{{STRUCTURE_1eax| PDB=1eax | SCENE= }}
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'''CRYSTAL STRUCTURE OF MTSP1 (MATRIPTASE)'''
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===CRYSTAL STRUCTURE OF MTSP1 (MATRIPTASE)===
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==Overview==
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The type II transmembrane multidomain serine proteinase MT-SP1/matriptase is highly expressed in many human cancer-derived cell lines and has been implicated in extracellular matrix re-modeling, tumor growth, and metastasis. We have expressed the catalytic domain of MT-SP1 and solved the crystal structures of complexes with benzamidine at 1.3 A and bovine pancreatic trypsin inhibitor at 2.9 A. MT-SP1 exhibits a trypsin-like serine proteinase fold, featuring a unique nine-residue 60-insertion loop that influences interactions with protein substrates. The structure discloses a trypsin-like S1 pocket, a small hydrophobic S2 subsite, and an open negatively charged S4 cavity that favors the binding of basic P3/P4 residues. A complementary charge pattern on the surface opposite the active site cleft suggests a distinct docking of the preceding low density lipoprotein receptor class A domain. The benzamidine crystals possess a freely accessible active site and are hence well suited for soaking small molecules, facilitating the improvement of inhibitors. The crystal structure of the MT-SP1 complex with bovine pancreatic trypsin inhibitor serves as a model for hepatocyte growth factor activator inhibitor 1, the physiological inhibitor of MT-SP1, and suggests determinants for the substrate specificity.
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(as it appears on PubMed at http://www.pubmed.gov), where 11696548 is the PubMed ID number.
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{{ABSTRACT_PUBMED_11696548}}
==About this Structure==
==About this Structure==
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[[Category: Matrix degradation]]
[[Category: Matrix degradation]]
[[Category: Serine proteinase]]
[[Category: Serine proteinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 14:53:07 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 00:25:46 2008''

Revision as of 21:25, 30 June 2008

Image:1eax.png

Template:STRUCTURE 1eax

CRYSTAL STRUCTURE OF MTSP1 (MATRIPTASE)

Template:ABSTRACT PUBMED 11696548

About this Structure

1EAX is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Catalytic domain structures of MT-SP1/matriptase, a matrix-degrading transmembrane serine proteinase., Friedrich R, Fuentes-Prior P, Ong E, Coombs G, Hunter M, Oehler R, Pierson D, Gonzalez R, Huber R, Bode W, Madison EL, J Biol Chem. 2002 Jan 18;277(3):2160-8. Epub 2001 Nov 5. PMID:11696548

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