2n08: Difference between revisions
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==NMR structure of a short hydrophobic 11mer peptide in 25 mM SDS solution== | |||
<StructureSection load='2n08' size='340' side='right'caption='[[2n08]]' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[2n08]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2N08 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2N08 FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 20 models</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NH2:AMINO+GROUP'>NH2</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=2n08 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2n08 OCA], [https://pdbe.org/2n08 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2n08 RCSB], [https://www.ebi.ac.uk/pdbsum/2n08 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2n08 ProSAT]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Cyclic constraints are incorporated here into an 11-residue analogue of the N-terminus of glucagon-like peptide-1 (GLP-1) to investigate effects of structure on agonist activity. Cyclization through linking side chains of residues 2 and 5 or 5 and 9 produced agonists at nM concentrations in a cAMP assay. 2D-NMR and CD spectra revealed an N-terminal beta-turn and a C-terminal helix that differentially influenced affinity and agonist potency. These structures can inform development of small molecule agonists of the GLP-1 receptor to treat type 2 diabetes. | |||
Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists.,Hoang HN, Song K, Hill TA, Derksen DR, Edmonds DJ, Kok WM, Limberakis C, Liras S, Loria PM, Mascitti V, Mathiowetz AM, Mitchell JM, Piotrowski DW, Price DA, Stanton RV, Suen JY, Withka JM, Griffith DA, Fairlie DP J Med Chem. 2015 Apr 3. PMID:25839426<ref>PMID:25839426</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: | <div class="pdbe-citations 2n08" style="background-color:#fffaf0;"></div> | ||
[[Category: | == References == | ||
[[Category: | <references/> | ||
[[Category: | __TOC__ | ||
[[Category: | </StructureSection> | ||
[[Category: | [[Category: Large Structures]] | ||
[[Category: | [[Category: Derksen DR]] | ||
[[Category: | [[Category: Edmonds DJ]] | ||
[[Category: | [[Category: Fairlie DP]] | ||
[[Category: | [[Category: Griffith DA]] | ||
[[Category: | [[Category: Hill TA]] | ||
[[Category: | [[Category: Hoang HN]] | ||
[[Category: | [[Category: Kok WM]] | ||
[[Category: | [[Category: Limberakis C]] | ||
[[Category: | [[Category: Liras S]] | ||
[[Category: | [[Category: Loria PM]] | ||
[[Category: | [[Category: Mascitti V]] | ||
[[Category: | [[Category: Mathiowetz AM]] | ||
[[Category: | [[Category: Mitchell JM]] | ||
[[Category: Piotrowski DW]] | |||
[[Category: Price DA]] | |||
[[Category: Song K]] | |||
[[Category: Stanton RV]] | |||
[[Category: Suen JY]] | |||
[[Category: Withka JM]] | |||
Latest revision as of 04:12, 21 November 2024
NMR structure of a short hydrophobic 11mer peptide in 25 mM SDS solutionNMR structure of a short hydrophobic 11mer peptide in 25 mM SDS solution
Structural highlights
Publication Abstract from PubMedCyclic constraints are incorporated here into an 11-residue analogue of the N-terminus of glucagon-like peptide-1 (GLP-1) to investigate effects of structure on agonist activity. Cyclization through linking side chains of residues 2 and 5 or 5 and 9 produced agonists at nM concentrations in a cAMP assay. 2D-NMR and CD spectra revealed an N-terminal beta-turn and a C-terminal helix that differentially influenced affinity and agonist potency. These structures can inform development of small molecule agonists of the GLP-1 receptor to treat type 2 diabetes. Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists.,Hoang HN, Song K, Hill TA, Derksen DR, Edmonds DJ, Kok WM, Limberakis C, Liras S, Loria PM, Mascitti V, Mathiowetz AM, Mitchell JM, Piotrowski DW, Price DA, Stanton RV, Suen JY, Withka JM, Griffith DA, Fairlie DP J Med Chem. 2015 Apr 3. PMID:25839426[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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