2r6n
From Proteopedia
(New page: 200px<br /> <applet load="2r6n" size="450" color="white" frame="true" align="right" spinBox="true" caption="2r6n, resolution 1.950Å" /> '''Crystal structure ...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:2r6n. | + | [[Image:2r6n.jpg|left|200px]]<br /><applet load="2r6n" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2r6n" size=" | + | |
caption="2r6n, resolution 1.950Å" /> | caption="2r6n, resolution 1.950Å" /> | ||
'''Crystal structure of a pyrrolopyrimidine inhibitor in complex with human Cathepsin K'''<br /> | '''Crystal structure of a pyrrolopyrimidine inhibitor in complex with human Cathepsin K'''<br /> | ||
| Line 6: | Line 5: | ||
==Overview== | ==Overview== | ||
Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within, the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3, optimization and identified highly potent and selective cathepsin K, inhibitors 11-20. | Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within, the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3, optimization and identified highly potent and selective cathepsin K, inhibitors 11-20. | ||
| - | |||
| - | ==Disease== | ||
| - | Known disease associated with this structure: Pycnodysostosis OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601105 601105]] | ||
==About this Structure== | ==About this Structure== | ||
| - | 2R6N 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 CKE as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Cathepsin_K Cathepsin K], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.38 3.4.22.38] Full crystallographic information is available from [http:// | + | 2R6N 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=CKE:'>CKE</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Cathepsin_K Cathepsin K], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.38 3.4.22.38] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2R6N OCA]. |
==Reference== | ==Reference== | ||
| Line 32: | Line 28: | ||
[[Category: zymogen]] | [[Category: zymogen]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:24:21 2008'' |
Revision as of 10:24, 23 January 2008
|
Crystal structure of a pyrrolopyrimidine inhibitor in complex with human Cathepsin K
Overview
Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within, the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3, optimization and identified highly potent and selective cathepsin K, inhibitors 11-20.
About this Structure
2R6N is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Cathepsin K, with EC number 3.4.22.38 Full crystallographic information is available from OCA.
Reference
Novel scaffold for cathepsin K inhibitors., Teno N, Miyake T, Ehara T, Irie O, Sakaki J, Ohmori O, Gunji H, Matsuura N, Masuya K, Hitomi Y, Nonomura K, Horiuchi M, Gohda K, Iwasaki A, Umemura I, Tada S, Kometani M, Iwasaki G, Cowan-Jacob SW, Missbach M, Lattmann R, Betschart C, Bioorg Med Chem Lett. 2007 Nov 15;17(22):6096-100. Epub 2007 Sep 15. PMID:17911019
Page seeded by OCA on Wed Jan 23 12:24:21 2008
