2rgu: Difference between revisions

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[[Image:2rgu.~~gif~~|left|200px]]<br />

[[Image:2rgu.jpg|left|200px]]<br /><applet load="2rgu" size="350" color="white" frame="true" align="right" spinBox="true"

<applet load="2rgu" size="~~450~~" color="white" frame="true" align="right" spinBox="true"

caption="2rgu, resolution 2.600Å" />

'''Crystal structure of complex of human DPP4 and inhibitor'''<br />

==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 [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://~~ispc~~.weizmann.ac.il/oca-bin/ocashort?id=2RGU OCA].

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].

==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: Homo sapiens]]

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[[Category: transmembrane]]

''Page seeded by [http://~~ispc~~.weizmann.ac.il/oca OCA ] on ~~Mon Nov 12~~ 23:37:~~22 2007~~''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 11:13:29 2008''

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@@ Line 1: / Line 1: @@
-[[Image:2rgu.gif|left|200px]]<br />
+[[Image:2rgu.jpg|left|200px]]<br /><applet load="2rgu" size="350" color="white" frame="true" align="right" spinBox="true"
-<applet load="2rgu" size="450" color="white" frame="true" align="right" spinBox="true"
 caption="2rgu, resolution 2.600&Aring;" />
 '''Crystal structure of complex of human DPP4 and inhibitor'''<br />
+==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==
-RGU 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://ispc.weizmann.ac.il/oca-bin/ocashort?id=2RGU OCA].
+RGU 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].
+==Reference==
+-(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: Homo sapiens]]
@@ Line 26: / Line 31: @@
 [[Category: transmembrane]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 23:37:22 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 11:13:29 2008''