6obx: Difference between revisions
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New page: '''Unreleased structure''' The entry 6obx is ON HOLD Authors: Caner, S., Brayer, G.D. Description: Montbretin A analogue M10-MbA in complex with Human pancreatic alpha-amylase [[Catego... |
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==Montbretin A analogue M10-MbA in complex with Human pancreatic alpha-amylase== | |||
<StructureSection load='6obx' size='340' side='right'caption='[[6obx]], [[Resolution|resolution]] 1.30Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[6obx]] is a 1 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=6OBX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6OBX 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]] 1.3Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=MPD:(4S)-2-METHYL-2,4-PENTANEDIOL'>MPD</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=PCA:PYROGLUTAMIC+ACID'>PCA</scene>, <scene name='pdbligand=ZXU:(2~{S})-~{N}-[3-[2-[3,4-bis(oxidanyl)phenyl]-5,7-bis(oxidanyl)-4-oxidanylidene-chromen-3-yl]oxypropyl]-2-[[(~{E})-3-[3,4-bis(oxidanyl)phenyl]prop-2-enoyl]amino]-3-(4-hydroxyphenyl)propanamide'>ZXU</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=6obx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6obx OCA], [https://pdbe.org/6obx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6obx RCSB], [https://www.ebi.ac.uk/pdbsum/6obx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6obx ProSAT]</span></td></tr> | |||
</table> | |||
== Function == | |||
[https://www.uniprot.org/uniprot/AMYP_HUMAN AMYP_HUMAN] | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, K I = 60 and 70 nM, with improved specificity over medically relevant glycosidases, making them promising candidates for controlling blood glucose. Crystallographic analysis confirmed similar binding modes and identified new active site interactions. | |||
Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic alpha-amylase.,Tysoe CR, Caner S, Calvert MB, Win-Mason A, Brayer GD, Withers SG Chem Sci. 2019 Oct 18;10(48):11073-11077. doi: 10.1039/c9sc02610j. eCollection, 2019 Dec 28. PMID:32206255<ref>PMID:32206255</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: Brayer | <div class="pdbe-citations 6obx" style="background-color:#fffaf0;"></div> | ||
[[Category: Caner | |||
==See Also== | |||
*[[Amylase 3D structures|Amylase 3D structures]] | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Homo sapiens]] | |||
[[Category: Large Structures]] | |||
[[Category: Brayer GD]] | |||
[[Category: Caner S]] | |||
Latest revision as of 13:17, 23 October 2024
Montbretin A analogue M10-MbA in complex with Human pancreatic alpha-amylaseMontbretin A analogue M10-MbA in complex with Human pancreatic alpha-amylase
Structural highlights
FunctionPublication Abstract from PubMedSimplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, K I = 60 and 70 nM, with improved specificity over medically relevant glycosidases, making them promising candidates for controlling blood glucose. Crystallographic analysis confirmed similar binding modes and identified new active site interactions. Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic alpha-amylase.,Tysoe CR, Caner S, Calvert MB, Win-Mason A, Brayer GD, Withers SG Chem Sci. 2019 Oct 18;10(48):11073-11077. doi: 10.1039/c9sc02610j. eCollection, 2019 Dec 28. PMID:32206255[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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