2rgu
From Proteopedia
(New page: 200px<br /> <applet load="2rgu" size="450" color="white" frame="true" align="right" spinBox="true" caption="2rgu, resolution 2.600Å" /> '''Crystal structure ...) |
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| - | [[Image:2rgu. | + | [[Image:2rgu.jpg|left|200px]]<br /><applet load="2rgu" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2rgu" size=" | + | |
caption="2rgu, resolution 2.600Å" /> | caption="2rgu, resolution 2.600Å" /> | ||
'''Crystal structure of complex of human DPP4 and inhibitor'''<br /> | '''Crystal structure of complex of human DPP4 and inhibitor'''<br /> | ||
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| + | ==Overview== | ||
| + | A new chemical class of potent DPP-4 inhibitors structurally derived from, the xanthine scaffold for the treatment of type 2 diabetes has been, discovered and evaluated. Systematic structural variations have led to 1, (BI 1356), a highly potent, selective, long-acting, and orally active, DPP-4 inhibitor that shows considerable blood glucose lowering in, different animal species. 1 is currently undergoing clinical phase IIb, trials and holds the potential for once-daily treatment of type 2, diabetics. | ||
==About this Structure== | ==About this Structure== | ||
| - | 2RGU 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 and 356 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] Full crystallographic information is available from [http:// | + | 2RGU 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 <scene name='pdbligand=NAG:'>NAG</scene> and <scene name='pdbligand=356:'>356</scene> 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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2RGU OCA]. |
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| + | ==Reference== | ||
| + | 8-(3-(R)-Aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin -2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a Highly Potent, Selective, Long-Acting, and Orally Bioavailable DPP-4 Inhibitor for the Treatment of Type 2 Diabetes., Eckhardt M, Langkopf E, Mark M, Tadayyon M, Thomas L, Nar H, Pfrengle W, Guth B, Lotz R, Sieger P, Fuchs H, Himmelsbach F, J Med Chem. 2007 Dec 27;50(26):6450-3. Epub 2007 Dec 1. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=18052023 18052023] | ||
[[Category: Dipeptidyl-peptidase IV]] | [[Category: Dipeptidyl-peptidase IV]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
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[[Category: transmembrane]] | [[Category: transmembrane]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 11:13:29 2008'' |
Revision as of 09:13, 23 January 2008
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Crystal structure of complex of human DPP4 and inhibitor
Overview
A new chemical class of potent DPP-4 inhibitors structurally derived from, the xanthine scaffold for the treatment of type 2 diabetes has been, discovered and evaluated. Systematic structural variations have led to 1, (BI 1356), a highly potent, selective, long-acting, and orally active, DPP-4 inhibitor that shows considerable blood glucose lowering in, different animal species. 1 is currently undergoing clinical phase IIb, trials and holds the potential for once-daily treatment of type 2, diabetics.
About this Structure
2RGU is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Full crystallographic information is available from OCA.
Reference
8-(3-(R)-Aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin -2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a Highly Potent, Selective, Long-Acting, and Orally Bioavailable DPP-4 Inhibitor for the Treatment of Type 2 Diabetes., Eckhardt M, Langkopf E, Mark M, Tadayyon M, Thomas L, Nar H, Pfrengle W, Guth B, Lotz R, Sieger P, Fuchs H, Himmelsbach F, J Med Chem. 2007 Dec 27;50(26):6450-3. Epub 2007 Dec 1. PMID:18052023
Page seeded by OCA on Wed Jan 23 11:13:29 2008
Categories: Dipeptidyl-peptidase IV | Homo sapiens | Single protein | Eckhardt, M. | Himmelsbach, F. | Nar, H. | 356 | NAG | Aminopeptidase | Glycoprotein | Hydrolase | Inhibitor | Membrane | Peptidase | Protease | Secreted | Serine protease | Signal-anchor | Transmembrane
