1snk
From Proteopedia
(New page: 200px<br /> <applet load="1snk" size="450" color="white" frame="true" align="right" spinBox="true" caption="1snk, resolution 2.40Å" /> '''Cathepsin K complex...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:1snk.gif|left|200px]]<br /> | + | [[Image:1snk.gif|left|200px]]<br /><applet load="1snk" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1snk" size=" | + | |
caption="1snk, resolution 2.40Å" /> | caption="1snk, resolution 2.40Å" /> | ||
'''Cathepsin K complexed with carbamate derivatized norleucine aldehyde'''<br /> | '''Cathepsin K complexed with carbamate derivatized norleucine aldehyde'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The synthesis and biological activity of a series of aldehyde inhibitors | + | The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S2 and S3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P2 and P3 positions afforded analogs with cathepsin K IC50s between 600 nM and 130 pM. |
==Disease== | ==Disease== | ||
| Line 11: | Line 10: | ||
==About this Structure== | ==About this Structure== | ||
| - | 1SNK 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 SO4 and MYE as [http://en.wikipedia.org/wiki/ligands ligands]. 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:// | + | 1SNK 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=SO4:'>SO4</scene> and <scene name='pdbligand=MYE:'>MYE</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. 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=1SNK OCA]. |
==Reference== | ==Reference== | ||
| Line 18: | Line 17: | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Boros, E | + | [[Category: Boros, E E.]] |
| - | [[Category: Deaton, D | + | [[Category: Deaton, D N.]] |
| - | [[Category: Hassell, A | + | [[Category: Hassell, A M.]] |
| - | [[Category: Jr., D | + | [[Category: Jr., D H.Willard.]] |
| - | [[Category: McFadyen, R | + | [[Category: McFadyen, R B.]] |
| - | [[Category: Miller, A | + | [[Category: Miller, A B.]] |
| - | [[Category: Miller, L | + | [[Category: Miller, L R.]] |
| - | [[Category: Shewchuk, L | + | [[Category: Shewchuk, L M.]] |
| - | [[Category: Thompson, J | + | [[Category: Thompson, J B.]] |
| - | [[Category: Wright, L | + | [[Category: Wright, L L.]] |
[[Category: MYE]] | [[Category: MYE]] | ||
[[Category: SO4]] | [[Category: SO4]] | ||
[[Category: catk]] | [[Category: catk]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:03:22 2008'' |
Revision as of 13:03, 21 February 2008
|
Cathepsin K complexed with carbamate derivatized norleucine aldehyde
Contents |
Overview
The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S2 and S3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P2 and P3 positions afforded analogs with cathepsin K IC50s between 600 nM and 130 pM.
Disease
Known disease associated with this structure: Pycnodysostosis OMIM:[601105]
About this Structure
1SNK is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Cathepsin K, with EC number 3.4.22.38 Full crystallographic information is available from OCA.
Reference
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors., Boros EE, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Paulick MG, Shewchuk LM, Thompson JB, Willard DH Jr, Wright LL, Bioorg Med Chem Lett. 2004 Jul 5;14(13):3425-9. PMID:15177446
Page seeded by OCA on Thu Feb 21 15:03:22 2008
Categories: Cathepsin K | Homo sapiens | Single protein | Boros, E E. | Deaton, D N. | Hassell, A M. | Jr., D H.Willard. | McFadyen, R B. | Miller, A B. | Miller, L R. | Shewchuk, L M. | Thompson, J B. | Wright, L L. | MYE | SO4 | Catk
