This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


4fxy

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Current revision (15:36, 14 March 2024) (edit) (undo)
 
(4 intermediate revisions not shown.)
Line 1: Line 1:
 +
==Crystal structure of rat neurolysin with bound pyrazolidin inhibitor==
==Crystal structure of rat neurolysin with bound pyrazolidin inhibitor==
-
<StructureSection load='4fxy' size='340' side='right' caption='[[4fxy]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
+
<StructureSection load='4fxy' size='340' side='right'caption='[[4fxy]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
-
<table><tr><td colspan='2'>[[4fxy]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FXY OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FXY FirstGlance]. <br>
+
<table><tr><td colspan='2'>[[4fxy]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FXY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4FXY FirstGlance]. <br>
-
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0W2:1-{(2S)-1-[(3R)-3-(2-CHLOROPHENYL)-2-(2-FLUOROPHENYL)PYRAZOLIDIN-1-YL]-1-OXOPROPAN-2-YL}-3-[(1R,3S,5R,7R)-TRICYCLO[3.3.1.1~3,7~]DEC-2-YL]UREA'>0W2</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
+
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.8&#8491;</td></tr>
-
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1i1i|1i1i]], [[2o3e|2o3e]]</td></tr>
+
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0W2:1-{(2S)-1-[(3R)-3-(2-CHLOROPHENYL)-2-(2-FLUOROPHENYL)PYRAZOLIDIN-1-YL]-1-OXOPROPAN-2-YL}-3-[(1R,3S,5R,7R)-TRICYCLO[3.3.1.1~3,7~]DEC-2-YL]UREA'>0W2</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
-
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Nln ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])</td></tr>
+
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4fxy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fxy OCA], [https://pdbe.org/4fxy PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4fxy RCSB], [https://www.ebi.ac.uk/pdbsum/4fxy PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4fxy ProSAT]</span></td></tr>
-
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Neurolysin Neurolysin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.16 3.4.24.16] </span></td></tr>
+
-
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4fxy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fxy OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4fxy RCSB], [http://www.ebi.ac.uk/pdbsum/4fxy PDBsum]</span></td></tr>
+
</table>
</table>
-
<div style="background-color:#fffaf0;">
+
== Function ==
-
== Publication Abstract from PubMed ==
+
[https://www.uniprot.org/uniprot/NEUL_RAT NEUL_RAT] Hydrolyzes oligopeptides such as neurotensin, bradykinin and dynorphin A.
-
Neuropeptidases specialize in the hydrolysis of the small bioactive peptides that play a variety of signaling roles in the nervous and endocrine systems. One neuropeptidase, neurolysin, helps control the levels of the dopaminergic circuit modulator neurotensin and is a member of a fold group that includes the antihypertensive target angiotensin converting enzyme. We report the discovery of a potent inhibitor that, unexpectedly, binds away from the enzyme catalytic site. The location of the bound inhibitor suggests it disrupts activity by preventing a hinge-like motion associated with substrate binding and catalysis. In support of this model, the inhibition kinetics are mixed, with both noncompetitive and competitive components, and fluorescence polarization shows directly that the inhibitor reverses a substrate-associated conformational change. This new type of inhibition may have widespread utility in targeting neuropeptidases.
+
-
 
+
-
Allosteric Inhibition of the Neuropeptidase Neurolysin.,Hines CS, Ray K, Schmidt JJ, Xiong F, Feenstra RW, Pras-Raves M, de Moes JP, Lange JH, Melikishvili M, Fried MG, Mortenson P, Charlton M, Patel Y, Courtney SM, Kruse CG, Rodgers DW J Biol Chem. 2014 Nov 5. pii: jbc.M114.620930. PMID:25378390<ref>PMID:25378390</ref>
+
-
 
+
-
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+
-
</div>
+
-
== References ==
+
-
<references/>
+
__TOC__
__TOC__
</StructureSection>
</StructureSection>
-
[[Category: Buffalo rat]]
+
[[Category: Large Structures]]
-
[[Category: Neurolysin]]
+
[[Category: Rattus norvegicus]]
-
[[Category: Hines, C S]]
+
[[Category: Hines CS]]
-
[[Category: Rodgers, D W]]
+
[[Category: Rodgers DW]]
-
[[Category: Endopeptidase]]
+
-
[[Category: Hydrolase]]
+
-
[[Category: Hydrolase-hydrolase inhibitor complex]]
+
-
[[Category: Neuropeptidase]]
+
-
[[Category: Zinc metallopeptidase]]
+

Current revision

Crystal structure of rat neurolysin with bound pyrazolidin inhibitor

PDB ID 4fxy

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4fxy"
Personal tools