2bub
From Proteopedia
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==About this Structure== | ==About this Structure== | ||
| - | 2BUB is a | + | 2BUB is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with NAG, NDG and FPB as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Dipeptidyl-peptidase_IV Dipeptidyl-peptidase IV], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BUB OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transmembrane]] | [[Category: transmembrane]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 13:13:04 2007'' |
Revision as of 11:07, 5 November 2007
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CRYSTAL STRUCTURE OF HUMAN DIPEPTIDYL PEPTIDASE IV (CD26) IN COMPLEX WITH A REVERSED AMIDE INHIBITOR
Overview
The co-crystal structure of beta-phenethylamine fragment inhibitor 5 bound, to DPP-IV revealed that the phenyl ring occupied the proline pocket of the, enzyme. This finding provided the basis for a general hypothesis of a, reverse binding mode for beta-phenethylamine-based DPP-IV inhibitors., Novel inhibitor design concepts that obviate substrate-like, structure-activity relationships (SAR) were thereby enabled, and novel, potent inhibitors were discovered.
About this Structure
2BUB is a Single protein structure of sequence from Homo sapiens with NAG, NDG and FPB as ligands. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Structure known Active Site: AC1. Full crystallographic information is available from OCA.
Reference
The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors., Nordhoff S, Cerezo-Galvez S, Feurer A, Hill O, Matassa VG, Metz G, Rummey C, Thiemann M, Edwards PJ, Bioorg Med Chem Lett. 2006 Mar 15;16(6):1744-8. Epub 2006 Jan 11. PMID:16376544
Page seeded by OCA on Mon Nov 5 13:13:04 2007
Categories: Dipeptidyl-peptidase IV | Homo sapiens | Single protein | Cerezo-Galvez, S. | Edwards, P.J. | Feurer, A. | Hill, O. | Matassa, V.G. | Metz, G. | Nordhoff, S. | Rummey, C. | Thiemann, M. | FPB | NAG | NDG | Aminopeptidase | Complex | Diabetes mellitus | Dpp-iv | Drug design | Glycoprotein | Hydrolase | Protease | Serine protease | Signal-anchor | Transmembrane
