1snk: Difference between revisions

From Proteopedia
Jump to navigationJump to search
OCA (talk | contribs)
New page: left|200px<br /> <applet load="1snk" size="450" color="white" frame="true" align="right" spinBox="true" caption="1snk, resolution 2.40Å" /> '''Cathepsin K complex...
 
OCA (talk | contribs)
No edit summary
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="450" color="white" frame="true" align="right" spinBox="true"  
caption="1snk, resolution 2.40&Aring;" />
caption="1snk, resolution 2.40&Aring;" />
'''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, 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.
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://ispc.weizmann.ac.il/oca-bin/ocashort?id=1SNK OCA].  
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.E.]]
[[Category: Boros, E E.]]
[[Category: Deaton, D.N.]]
[[Category: Deaton, D N.]]
[[Category: Hassell, A.M.]]
[[Category: Hassell, A M.]]
[[Category: Jr., D.H.Willard.]]
[[Category: Jr., D H.Willard.]]
[[Category: McFadyen, R.B.]]
[[Category: McFadyen, R B.]]
[[Category: Miller, A.B.]]
[[Category: Miller, A B.]]
[[Category: Miller, L.R.]]
[[Category: Miller, L R.]]
[[Category: Shewchuk, L.M.]]
[[Category: Shewchuk, L M.]]
[[Category: Thompson, J.B.]]
[[Category: Thompson, J B.]]
[[Category: Wright, L.L.]]
[[Category: Wright, L L.]]
[[Category: MYE]]
[[Category: MYE]]
[[Category: SO4]]
[[Category: SO4]]
[[Category: catk]]
[[Category: catk]]


''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 19:15:41 2007''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:03:22 2008''