1r1j
From Proteopedia
(New page: 200px<br /> <applet load="1r1j" size="450" color="white" frame="true" align="right" spinBox="true" caption="1r1j, resolution 2.35Å" /> '''STRUCTURAL ANALYSIS...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:1r1j.gif|left|200px]]<br /> | + | [[Image:1r1j.gif|left|200px]]<br /><applet load="1r1j" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1r1j" size=" | + | |
caption="1r1j, resolution 2.35Å" /> | caption="1r1j, resolution 2.35Å" /> | ||
'''STRUCTURAL ANALYSIS OF NEPRILYSIN WITH VARIOUS SPECIFIC AND POTENT INHIBITORS'''<br /> | '''STRUCTURAL ANALYSIS OF NEPRILYSIN WITH VARIOUS SPECIFIC AND POTENT INHIBITORS'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Neutral endopeptidase (NEP) is the major enzyme involved in the metabolic | + | Neutral endopeptidase (NEP) is the major enzyme involved in the metabolic inactivation of a number of bioactive peptides including the enkephalins, substance P, endothelin, bradykinin and atrial natriuretic factor. Owing to the physiological importance of NEP in the modulation of nociceptive and pressor responses, there is considerable interest in inhibitors of this enzyme as novel analgesics and antihypertensive agents. Here, the crystal structures of the soluble extracellular domain of human NEP (residues 52-749) complexed with various potent and competitive inhibitors are described. The structures unambiguously reveal the binding mode of the different zinc-chelating groups and the subsite specificity of the enzyme. |
==Disease== | ==Disease== | ||
| Line 11: | Line 10: | ||
==About this Structure== | ==About this Structure== | ||
| - | 1R1J 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 NAG, ZN and OIR as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Neprilysin Neprilysin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.11 3.4.24.11] Full crystallographic information is available from [http:// | + | 1R1J 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=NAG:'>NAG</scene>, <scene name='pdbligand=ZN:'>ZN</scene> and <scene name='pdbligand=OIR:'>OIR</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Neprilysin Neprilysin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.11 3.4.24.11] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1R1J OCA]. |
==Reference== | ==Reference== | ||
| Line 18: | Line 17: | ||
[[Category: Neprilysin]] | [[Category: Neprilysin]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Dale, G | + | [[Category: Dale, G E.]] |
| - | [[Category: Fournie-Zaluski, M | + | [[Category: Fournie-Zaluski, M C.]] |
[[Category: Oefner, C.]] | [[Category: Oefner, C.]] | ||
| - | [[Category: Roques, B | + | [[Category: Roques, B P.]] |
[[Category: NAG]] | [[Category: NAG]] | ||
[[Category: OIR]] | [[Category: OIR]] | ||
| Line 29: | Line 28: | ||
[[Category: metalloprotease]] | [[Category: metalloprotease]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:46:00 2008'' |
Revision as of 12:46, 21 February 2008
|
STRUCTURAL ANALYSIS OF NEPRILYSIN WITH VARIOUS SPECIFIC AND POTENT INHIBITORS
Contents |
Overview
Neutral endopeptidase (NEP) is the major enzyme involved in the metabolic inactivation of a number of bioactive peptides including the enkephalins, substance P, endothelin, bradykinin and atrial natriuretic factor. Owing to the physiological importance of NEP in the modulation of nociceptive and pressor responses, there is considerable interest in inhibitors of this enzyme as novel analgesics and antihypertensive agents. Here, the crystal structures of the soluble extracellular domain of human NEP (residues 52-749) complexed with various potent and competitive inhibitors are described. The structures unambiguously reveal the binding mode of the different zinc-chelating groups and the subsite specificity of the enzyme.
Disease
Known diseases associated with this structure: Membranous glomerulonephritis, antenatal OMIM:[120520], Neutral endopeptidase deficiency OMIM:[120520], Schizophrenia, susceptibility to OMIM:[607265]
About this Structure
1R1J is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Neprilysin, with EC number 3.4.24.11 Full crystallographic information is available from OCA.
Reference
Structural analysis of neprilysin with various specific and potent inhibitors., Oefner C, Roques BP, Fournie-Zaluski MC, Dale GE, Acta Crystallogr D Biol Crystallogr. 2004 Feb;60(Pt 2):392-6. Epub 2004, Jan 23. PMID:14747736
Page seeded by OCA on Thu Feb 21 14:46:00 2008
Categories: Homo sapiens | Neprilysin | Single protein | Dale, G E. | Fournie-Zaluski, M C. | Oefner, C. | Roques, B P. | NAG | OIR | ZN | Enkephalinase | Glycoprotein | Metalloprotease
