1eax
From Proteopedia
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| - | [[Image:1eax.gif|left|200px]] | + | [[Image:1eax.gif|left|200px]] |
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| - | '''CRYSTAL STRUCTURE OF MTSP1 (MATRIPTASE)''' | + | {{Structure |
| + | |PDB= 1eax |SIZE=350|CAPTION= <scene name='initialview01'>1eax</scene>, resolution 1.30Å | ||
| + | |SITE= <scene name='pdbsite=SO4:Ben+Binding+Site+For+Chain+A'>SO4</scene> | ||
| + | |LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> and <scene name='pdbligand=BEN:BENZAMIDINE'>BEN</scene> | ||
| + | |ACTIVITY= | ||
| + | |GENE= | ||
| + | }} | ||
| + | |||
| + | '''CRYSTAL STRUCTURE OF MTSP1 (MATRIPTASE)''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1EAX is a [ | + | 1EAX is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1EAX OCA]. |
==Reference== | ==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:[http:// | + | 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:[http://www.ncbi.nlm.nih.gov/pubmed/11696548 11696548] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
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[[Category: serine proteinase]] | [[Category: serine proteinase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 10:52:54 2008'' |
Revision as of 08:52, 20 March 2008
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| , resolution 1.30Å | |||||||
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| Sites: | |||||||
| Ligands: | and | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
CRYSTAL STRUCTURE OF MTSP1 (MATRIPTASE)
Contents |
Overview
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.
Disease
Known disease associated with this structure: Ichthyosis with hypotrichosis OMIM:[606797]
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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