1j1a: Difference between revisions

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[[Image:1j1a.gif|left|200px]]
{{Seed}}
[[Image:1j1a.png|left|200px]]


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{{STRUCTURE_1j1a|  PDB=1j1a  |  SCENE=  }}  
{{STRUCTURE_1j1a|  PDB=1j1a  |  SCENE=  }}  


'''PANCREATIC SECRETORY PHOSPHOLIPASE A2 (IIa) WITH ANTI-INFLAMMATORY ACTIVITY'''
===PANCREATIC SECRETORY PHOSPHOLIPASE A2 (IIa) WITH ANTI-INFLAMMATORY ACTIVITY===




==Overview==
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Few reported inhibitors of secretory phospholipase A(2) enzymes truly inhibit the IIa human isoform (hnpsPLA(2)-IIa) noncovalently at submicromolar concentrations. Herein, the simple chiral precursor D-tyrosine was derivatised to give a series of potent new inhibitors of hnpsPLA(2)-IIa. A 2.2-A crystal structure shows an inhibitor bound in the active site of the enzyme, chelated to a Ca(2+) ion through carboxylate and amide oxygen atoms, H-bonded through an amide NH group to His48, with multiple hydrophobic contacts and a T-shaped aromatic-group-His6 interaction. Antiinflammatory activity is also demonstrated for two compounds administered orally to rats.
The line below this paragraph, {{ABSTRACT_PUBMED_12616631}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 12616631 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12616631}}


==About this Structure==
==About this Structure==
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[[Category: Medicinal chemistry]]
[[Category: Medicinal chemistry]]
[[Category: Structure-activity relationship]]
[[Category: Structure-activity relationship]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 20:40:41 2008''
 
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