3o9l

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 3: Line 3:
<StructureSection load='3o9l' size='340' side='right'caption='[[3o9l]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
<StructureSection load='3o9l' size='340' side='right'caption='[[3o9l]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
-
<table><tr><td colspan='2'>[[3o9l]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3O9L OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3O9L FirstGlance]. <br>
+
<table><tr><td colspan='2'>[[3o9l]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3O9L OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3O9L FirstGlance]. <br>
-
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=LPN:(3R,4S)-N-[2-CHLORO-5-(3-METHOXYPROPYL)BENZYL]-N-CYCLOPROPYL-4-{4-[2-(2,6-DICHLORO-4-METHYLPHENOXY)ETHOXY]PHENYL}PIPERIDINE-3-CARBOXAMIDE'>LPN</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</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]] 2.4&#8491;</td></tr>
-
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3g6z|3g6z]], [[3oag|3oag]], [[3oad|3oad]]</div></td></tr>
+
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=LPN:(3R,4S)-N-[2-CHLORO-5-(3-METHOXYPROPYL)BENZYL]-N-CYCLOPROPYL-4-{4-[2-(2,6-DICHLORO-4-METHYLPHENOXY)ETHOXY]PHENYL}PIPERIDINE-3-CARBOXAMIDE'>LPN</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr>
-
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">REN ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
+
-
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Renin Renin], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.15 3.4.23.15] </span></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=3o9l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3o9l OCA], [https://pdbe.org/3o9l PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3o9l RCSB], [https://www.ebi.ac.uk/pdbsum/3o9l PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3o9l ProSAT]</span></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=3o9l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3o9l OCA], [https://pdbe.org/3o9l PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3o9l RCSB], [https://www.ebi.ac.uk/pdbsum/3o9l PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3o9l ProSAT]</span></td></tr>
</table>
</table>
== Disease ==
== Disease ==
-
[[https://www.uniprot.org/uniprot/RENI_HUMAN RENI_HUMAN]] Defects in REN are a cause of renal tubular dysgenesis (RTD) [MIM:[https://omim.org/entry/267430 267430]]. RTD is an autosomal recessive severe disorder of renal tubular development characterized by persistent fetal anuria and perinatal death, probably due to pulmonary hypoplasia from early-onset oligohydramnios (the Potter phenotype).<ref>PMID:16116425</ref> Defects in REN are the cause of familial juvenile hyperuricemic nephropathy type 2 (HNFJ2) [MIM:[https://omim.org/entry/613092 613092]]. It is a renal disease characterized by juvenile onset of hyperuricemia, slowly progressive renal failure and anemia.<ref>PMID:19664745</ref>
+
[https://www.uniprot.org/uniprot/RENI_HUMAN RENI_HUMAN] Defects in REN are a cause of renal tubular dysgenesis (RTD) [MIM:[https://omim.org/entry/267430 267430]. RTD is an autosomal recessive severe disorder of renal tubular development characterized by persistent fetal anuria and perinatal death, probably due to pulmonary hypoplasia from early-onset oligohydramnios (the Potter phenotype).<ref>PMID:16116425</ref> Defects in REN are the cause of familial juvenile hyperuricemic nephropathy type 2 (HNFJ2) [MIM:[https://omim.org/entry/613092 613092]. It is a renal disease characterized by juvenile onset of hyperuricemia, slowly progressive renal failure and anemia.<ref>PMID:19664745</ref>
== Function ==
== Function ==
-
[[https://www.uniprot.org/uniprot/RENI_HUMAN RENI_HUMAN]] Renin is a highly specific endopeptidase, whose only known function is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of blood pressure and increased sodium retention by the kidney.
+
[https://www.uniprot.org/uniprot/RENI_HUMAN RENI_HUMAN] Renin is a highly specific endopeptidase, whose only known function is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of blood pressure and increased sodium retention by the kidney.
-
<div style="background-color:#fffaf0;">
+
-
== Publication Abstract from PubMed ==
+
-
The discovery of a new series of piperidine-based renin inhibitors is described herein. SAR optimization upon the P3 renin sub-pocket is described, leading to the discovery of 9 and 41, two bioavailable renin inhibitors orally active at low doses in a transgenic rat model of hypertension.
+
-
 
+
-
Design and optimization of new piperidines as renin inhibitors.,Corminboeuf O, Bezencon O, Grisostomi C, Remen L, Richard-Bildstein S, Bur D, Prade L, Hess P, Strickner P, Fischli W, Steiner B, Treiber A Bioorg Med Chem Lett. 2010 Nov 1;20(21):6286-90. Epub 2010 Aug 22. PMID:20843686<ref>PMID:20843686</ref>
+
-
 
+
-
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+
-
</div>
+
-
<div class="pdbe-citations 3o9l" style="background-color:#fffaf0;"></div>
+
==See Also==
==See Also==
Line 30: Line 19:
__TOC__
__TOC__
</StructureSection>
</StructureSection>
-
[[Category: Human]]
+
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
-
[[Category: Renin]]
+
[[Category: Bezencon O]]
-
[[Category: Bezencon, O]]
+
[[Category: Bur D]]
-
[[Category: Bur, D]]
+
[[Category: Corminboeuf O]]
-
[[Category: Corminboeuf, O]]
+
[[Category: Grisostomi C]]
-
[[Category: Grisostomi, C]]
+
[[Category: Hess P]]
-
[[Category: Hess, P]]
+
[[Category: Prade L]]
-
[[Category: Prade, L]]
+
[[Category: Remen L]]
-
[[Category: Remen, L]]
+
[[Category: Richard-Bildstein S]]
-
[[Category: Richard-Bildstein, S]]
+
[[Category: Strickner P]]
-
[[Category: Strickner, P]]
+
[[Category: Treiber A]]
-
[[Category: Treiber, A]]
+
-
[[Category: Blood]]
+
-
[[Category: Glycosilation]]
+
-
[[Category: Hydrolase]]
+
-
[[Category: Hydrolase-hydrolase inhibitor complex]]
+
-
[[Category: Protease]]
+

Revision as of 10:04, 14 February 2024

Design and optimisation of new piperidines as renin inhibitors

PDB ID 3o9l

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/3o9l"
Personal tools