1orv

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{{STRUCTURE_1orv| PDB=1orv | SCENE= }}
{{STRUCTURE_1orv| PDB=1orv | SCENE= }}
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'''Crystal Structure of Porcine Dipeptidyl Peptidase IV (CD26)'''
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===Crystal Structure of Porcine Dipeptidyl Peptidase IV (CD26)===
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==Overview==
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The membrane-bound glycoprotein dipeptidyl peptidase IV (DP IV, CD26) is a unique multifunctional protein, acting as receptor, binding and proteolytic molecule. We have determined the sequence and 1.8 A crystal structure of native DP IV prepared from porcine kidney. The crystal structure reveals a 2-2-2 symmetric tetrameric assembly which depends on the natively glycosylated beta-propeller blade IV. The crystal structure indicates that tetramerization of DP IV is a key mechanism to regulate its interaction with other components. Each subunit comprises two structural domains, the N-terminal eight-bladed beta-propeller with open Velcro topology and the C-terminal alpha/beta-hydrolase domain. Analogy with the structurally related POP and tricorn protease suggests that substrates access the buried active site through the beta-propeller tunnel while products leave the active site through a separate side exit. A dipeptide mimicking inhibitor complexed to the active site discloses key determinants for substrate recognition, including a Glu-Glu motif that distinguishes DP IV as an aminopeptidase and an oxyanion trap that binds and activates the P(2)-carbonyl oxygen necessary for efficient postproline cleavage. We discuss active and nonactive site-directed inhibition strategies of this pharmaceutical target protein.
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(as it appears on PubMed at http://www.pubmed.gov), where 12690074 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12690074}}
==About this Structure==
==About this Structure==
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[[Category: Serine protease]]
[[Category: Serine protease]]
[[Category: Substrate channeling]]
[[Category: Substrate channeling]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:12:27 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 09:47:01 2008''

Revision as of 06:47, 29 July 2008

Image:1orv.png

Template:STRUCTURE 1orv

Crystal Structure of Porcine Dipeptidyl Peptidase IV (CD26)

Template:ABSTRACT PUBMED 12690074

About this Structure

1ORV is a Single protein structure of sequence from Sus scrofa. Full crystallographic information is available from OCA.

Reference

The crystal structure of dipeptidyl peptidase IV (CD26) reveals its functional regulation and enzymatic mechanism., Engel M, Hoffmann T, Wagner L, Wermann M, Heiser U, Kiefersauer R, Huber R, Bode W, Demuth HU, Brandstetter H, Proc Natl Acad Sci U S A. 2003 Apr 29;100(9):5063-8. Epub 2003 Apr 10. PMID:12690074

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