3o9l: Difference between revisions

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'''Unreleased structure'''


The entry 3o9l is ON HOLD
==Design and optimisation of new piperidines as renin inhibitors==
<StructureSection load='3o9l' size='340' side='right'caption='[[3o9l]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
== Structural highlights ==
<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='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='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='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>
== 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>
== 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.
<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.


Authors: Corminboeuf, O., Bezencon, O., Grisostomi, C., Remen, L., Richard-Bildstein, S., Bur, D., Prade, L., Hess, P., Strickner, P., treiber, A.
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>


Description: Design and optimisation of new piperidines as renin inhibitors
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>


''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Dec  8 11:29:32 2010''
==See Also==
*[[Renin|Renin]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Bezencon O]]
[[Category: Bur D]]
[[Category: Corminboeuf O]]
[[Category: Grisostomi C]]
[[Category: Hess P]]
[[Category: Prade L]]
[[Category: Remen L]]
[[Category: Richard-Bildstein S]]
[[Category: Strickner P]]
[[Category: Treiber A]]
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