2bub: Difference between revisions
New page: left|200px<br /> <applet load="2bub" size="450" color="white" frame="true" align="right" spinBox="true" caption="2bub, resolution 2.66Å" /> '''CRYSTAL STRUCTURE O... |
No edit summary |
||
| Line 8: | Line 8: | ||
==About this Structure== | ==About this Structure== | ||
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/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BUB OCA]]. | 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== | ||
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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16376544 16376544] | 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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16376544 16376544] | ||
[[Category: Dipeptidyl-peptidase IV]] | |||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| Line 38: | Line 39: | ||
[[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 Tue Oct 30 11:24:01 2007'' | ||
Revision as of 12:19, 30 October 2007
|
CRYSTAL STRUCTURE OF HUMAN DIPEPTIDYL PEPTIDASE IV (CD26) IN COMPLEX WITH A REVERSED AMIDE INHIBITOR
OverviewOverview
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 StructureAbout 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].
ReferenceReference
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 Tue Oct 30 11:24:01 2007
Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- 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