2aux: Difference between revisions

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

Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.

2AUX 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=CT1:'>CT1</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=2AUX OCA].  

[[Category: Adkison, K K.]]

[[Category: Barrett, D G.]]

[[Category: Deaton, D N.]]

[[Category: Gampe, R T.]]

[[Category: Hassell, A M.]]

[[Category: Long, S T.]]

[[Category: McFadyen, R B.]]

[[Category: Miller, A B.]]

[[Category: Miller, L R.]]

[[Category: Shewchuk, L M.]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:31:20 2008''