3chp
From Proteopedia
OCA (Talk | contribs)
(New page: 200px <!-- The line below this paragraph, containing "STRUCTURE_3chp", creates the "Structure Box" on the page. You may change the PDB parameter (which sets the PD...)
Next diff →
Revision as of 06:54, 24 April 2008
Crystal structure of leukotriene a4 hydrolase in complex with (3S)-3-amino-4-oxo-4-[(4-phenylmethoxyphenyl)amino]butanoic acid
Overview
Leukotriene B(4) (LTB(4)) is a potent pro-inflammatory mediator that has been implicated in the pathogenesis of multiple diseases, including psoriasis, inflammatory bowel disease, multiple sclerosis and asthma. As a method to decrease the level of LTB(4) and possibly identify novel treatments, inhibitors of the LTB(4) biosynthetic enzyme, leukotriene A(4) hydrolase (LTA(4)-h), have been explored. Here we describe the discovery of a potent inhibitor of LTA(4)-h, arylamide of glutamic acid 4f, starting from the corresponding glycinamide 2. Analogs of 4f are then described, focusing on compounds that are both active and stable in whole blood. This effort culminated in the identification of amino alcohol 12a and amino ester 6b which meet these criteria.
About this Structure
3CHP is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Synthesis of glutamic acid analogs as potent inhibitors of leukotriene A(4) hydrolase., Kirkland TA, Adler M, Bauman JG, Chen M, Haeggstrom JZ, King B, Kochanny MJ, Liang AM, Mendoza L, Phillips GB, Thunnissen M, Trinh L, Whitlow M, Ye B, Ye H, Parkinson J, Guilford WJ, Bioorg Med Chem. 2008 Mar 20;. PMID:18394906 Page seeded by OCA on Thu Apr 24 09:54:16 2008
