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| | ==Substance P in DMPC/CHAPS isotropic q=0.25 bicelles as a ligand for NK1R== | | ==Substance P in DMPC/CHAPS isotropic q=0.25 bicelles as a ligand for NK1R== |
| - | <StructureSection load='2ksa' size='340' side='right' caption='[[2ksa]], [[NMR_Ensembles_of_Models | 5 NMR models]]' scene=''> | + | <StructureSection load='2ksa' size='340' side='right'caption='[[2ksa]]' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[2ksa]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2KSA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2KSA FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[2ksa]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2KSA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2KSA FirstGlance]. <br> |
| - | </td></tr><tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2ks9|2ks9]], [[2ksb|2ksb]]</td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 5 models</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=2ksa FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ksa OCA], [http://pdbe.org/2ksa PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2ksa RCSB], [http://www.ebi.ac.uk/pdbsum/2ksa PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2ksa 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=2ksa FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ksa OCA], [https://pdbe.org/2ksa PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2ksa RCSB], [https://www.ebi.ac.uk/pdbsum/2ksa PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2ksa ProSAT]</span></td></tr> |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[http://www.uniprot.org/uniprot/NK1R_HUMAN NK1R_HUMAN]] This is a receptor for the tachykinin neuropeptide substance P. It is probably associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: substance P > substance K > neuromedin-K. [[http://www.uniprot.org/uniprot/TKN1_HUMAN TKN1_HUMAN]] Tachykinins are active peptides which excite neurons, evoke behavioral responses, are potent vasodilators and secretagogues, and contract (directly or indirectly) many smooth muscles. | + | [https://www.uniprot.org/uniprot/TKN1_HUMAN TKN1_HUMAN] Tachykinins are active peptides which excite neurons, evoke behavioral responses, are potent vasodilators and secretagogues, and contract (directly or indirectly) many smooth muscles. |
| | <div style="background-color:#fffaf0;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
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| | </StructureSection> | | </StructureSection> |
| | [[Category: Homo sapiens]] | | [[Category: Homo sapiens]] |
| - | [[Category: Gayen, A]] | + | [[Category: Large Structures]] |
| - | [[Category: Mukhopadhyay, C]] | + | [[Category: Gayen A]] |
| - | [[Category: Autodock]] | + | [[Category: Mukhopadhyay C]] |
| - | [[Category: Dmpc/chaps bicelle]]
| + | |
| - | [[Category: Neuropeptide receptor-neuropeptide complex]]
| + | |
| - | [[Category: Nk1r]]
| + | |
| - | [[Category: Substance p]]
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| Structural highlights
Function
TKN1_HUMAN Tachykinins are active peptides which excite neurons, evoke behavioral responses, are potent vasodilators and secretagogues, and contract (directly or indirectly) many smooth muscles.
Publication Abstract from PubMed
Substance P (SP) is one of the target neurotransmitters associated with diseases related to chronic inflammation, pain and depression. The selective receptor for SP, NK(1)R is located in the heterogeneous microdomains or caveolae in membrane. Gangliosides, specifically GM1, are markers of these heterogeneous sites. Also, gangliosides are considered as important regulatory elements in cell-cell recognition and cell signaling. In the present work, we describe the conformations of Substance P in the presence of ternary membrane systems containing GM1 at the physiological concentration. SP is mostly unstructured in water, but appears as extended 3(10) helical or turn III in isotropic bicelles, more pronounced in the presence of GM1. NMR results suggest that, in the GM1 containing bicelles, the peptide is more inserted into the membrane with its C-terminus, while N-terminus lies close to the membrane-water interface. The NMR-derived conformation of SP in GM1 bicelles is docked on homology modeled NK(1)R and resulting interactions satisfy reported mutagenesis, fluorescence, photo-affinity labeling and modeling data. The results highlight efficacy of GM1 in membrane in providing structure in an otherwise flexible neurotransmitter Substance P; thus providing indication that it may be useful also for other neurotransmitter peptides/proteins associated with membrane.
NMR evidence of GM1-induced conformational change of Substance P using isotropic bicelles.,Gayen A, Goswami SK, Mukhopadhyay C Biochim Biophys Acta. 2010 Oct 16. PMID:20937248[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Gayen A, Goswami SK, Mukhopadhyay C. NMR evidence of GM1-induced conformational change of Substance P using isotropic bicelles. Biochim Biophys Acta. 2010 Oct 16. PMID:20937248 doi:10.1016/j.bbamem.2010.09.023
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