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1wo9

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{{STRUCTURE_1wo9| PDB=1wo9 | SCENE= }}
{{STRUCTURE_1wo9| PDB=1wo9 | SCENE= }}
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'''Selective inhibition of trypsins by insect peptides: role of P6-P10 loop'''
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===Selective inhibition of trypsins by insect peptides: role of P6-P10 loop===
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==Overview==
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PMP-D2 and HI, two peptides from Locusta migratoria, were shown to belong to the family of tight-binding protease inhibitors. However, they interact weakly with bovine trypsin (K(i) around 100 nM) despite a trypsin-specific Arg at the primary specificity site P1. Here we demonstrate that they are potent inhibitors of midgut trypsins isolated from the same insect and of a fungal trypsin from Fusarium oxysporum (K(i) &lt;or= 0.02 nM). Therefore, they display a selectivity not existing for the parent chymotrypsin inhibitor PMP-C. By NMR, we demonstrate that HI possesses a highly rigid structure similar to the crystal structure of a variant of PMP-D2 in complex with bovine alpha-chymotrypsin. The main difference with PMP-C is located in the region from residues 20 to 24 (positions P6-P10) that interacts with the loop containing Gly173 in chymotrypsin. The corresponding residue in mammalian trypsins is always a proline that may generate a steric clash with the inhibitor. The residues thought to confer selectivity were mutated with PMP-C as a model. The resulting analogue PMP-D2(K10W,P21A,W25A) loses some activity toward insect and fungal trypsins but is a more potent inhibitor of mammalian trypsins, corresponding to a decrease of selectivity. This work represents a first attempt in tuning the selectivity of natural peptidic serine protease inhibitors by mutating residues out of the reactive loop (P3-P'3).
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{{ABSTRACT_PUBMED_14622007}}
==About this Structure==
==About this Structure==
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Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WO9 OCA].
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Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WO9 OCA].
==Reference==
==Reference==
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[[Category: Roussel, A.]]
[[Category: Roussel, A.]]
[[Category: Hydrolase inhibitor]]
[[Category: Hydrolase inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:19:32 2008''

Revision as of 13:19, 28 July 2008

Image:1wo9.png

Template:STRUCTURE 1wo9

Selective inhibition of trypsins by insect peptides: role of P6-P10 loop

Template:ABSTRACT PUBMED 14622007

About this Structure

Full experimental information is available from OCA.

Reference

Selective inhibition of trypsins by insect peptides: role of P6-P10 loop., Kellenberger C, Ferrat G, Leone P, Darbon H, Roussel A, Biochemistry. 2003 Nov 25;42(46):13605-12. PMID:14622007

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