7zjh

From Proteopedia

(Difference between revisions)

Current revision

TRPV2-C16+Pro-2

Structural highlights

7zjh is a 4 chain structure with sequence from Rattus norvegicus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	Electron Microscopy, Resolution 3.39Å
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

TRPV2_RAT Calcium-permeable, non-selective cation channel with an outward rectification. Seems to be regulated, at least in part, by growth factors, like IGF1, PDGF and morphogenetic neuropeptide/head activator. May transduce physical stimuli in mast cells. Activated by temperatures higher than 52 degrees Celsius; is not activated by vanilloids and acidic pH (By similarity).^[1] ^[2]

Publication Abstract from PubMed

TRPV2 is a ligand-operated temperature sensor with poorly defined pharmacology. Here, we combine calcium imaging and patch-clamp electrophysiology with cryo-electron microscopy (cryo-EM) to explore how TRPV2 activity is modulated by the phytocannabinoid Delta(9)-tetrahydrocannabiorcol (C16) and by probenecid. C16 and probenecid act in concert to stimulate TRPV2 responses including histamine release from rat and human mast cells. Each ligand causes distinct conformational changes in TRPV2 as revealed by cryo-EM. Although the binding for probenecid remains elusive, C16 associates within the vanilloid pocket. As such, the C16 binding location is distinct from that of cannabidiol, partially overlapping with the binding site of the TRPV2 inhibitor piperlongumine. Taken together, we discover a new cannabinoid binding site in TRPV2 that is under the influence of allosteric control by probenecid. This molecular insight into ligand modulation enhances our understanding of TRPV2 in normal and pathophysiology.

Cannabinoid non-cannabidiol site modulation of TRPV2 structure and function.,Zhang L, Simonsen C, Zimova L, Wang K, Moparthi L, Gaudet R, Ekoff M, Nilsson G, Hellmich UA, Vlachova V, Gourdon P, Zygmunt PM Nat Commun. 2022 Dec 5;13(1):7483. doi: 10.1038/s41467-022-35163-y. PMID:36470868^[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Caterina MJ, Rosen TA, Tominaga M, Brake AJ, Julius D. A capsaicin-receptor homologue with a high threshold for noxious heat. Nature. 1999 Apr 1;398(6726):436-41. PMID:10201375 doi:http://dx.doi.org/10.1038/18906
↑ Stokes AJ, Shimoda LM, Koblan-Huberson M, Adra CN, Turner H. A TRPV2-PKA signaling module for transduction of physical stimuli in mast cells. J Exp Med. 2004 Jul 19;200(2):137-47. Epub 2004 Jul 12. PMID:15249591 doi:http://dx.doi.org/10.1084/jem.20032082
↑ Zhang L, Simonsen C, Zimova L, Wang K, Moparthi L, Gaudet R, Ekoff M, Nilsson G, Hellmich UA, Vlachova V, Gourdon P, Zygmunt PM. Cannabinoid non-cannabidiol site modulation of TRPV2 structure and function. Nat Commun. 2022 Dec 5;13(1):7483. doi: 10.1038/s41467-022-35163-y. PMID:36470868 doi:http://dx.doi.org/10.1038/s41467-022-35163-y

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 See Also
5 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/7zjh"

Categories: Large Structures | Rattus norvegicus | Gourdon P | Zhang L | Zygmunt PM

@@ Line 4: / Line 4: @@
 == Structural highlights ==
 <table><tr><td colspan='2'>[[7zjh]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7ZJH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7ZJH FirstGlance]. <br>
-</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=7zjh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7zjh OCA], [https://pdbe.org/7zjh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7zjh RCSB], [https://www.ebi.ac.uk/pdbsum/7zjh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7zjh ProSAT]</span></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3.39&#8491;</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=7zjh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7zjh OCA], [https://pdbe.org/7zjh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7zjh RCSB], [https://www.ebi.ac.uk/pdbsum/7zjh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7zjh ProSAT]</span></td></tr>
 </table>
 == Function ==
-[https://www.uniprot.org/uniprot/A0A0G2JSH6_RAT A0A0G2JSH6_RAT]
+[https://www.uniprot.org/uniprot/TRPV2_RAT TRPV2_RAT] Calcium-permeable, non-selective cation channel with an outward rectification. Seems to be regulated, at least in part, by growth factors, like IGF1, PDGF and morphogenetic neuropeptide/head activator. May transduce physical stimuli in mast cells. Activated by temperatures higher than 52 degrees Celsius; is not activated by vanilloids and acidic pH (By similarity).<ref>PMID:10201375</ref> <ref>PMID:15249591</ref>
 <div style="background-color:#fffaf0;">
 == Publication Abstract from PubMed ==
@@ Line 17: / Line 18: @@
 </div>
 <div class="pdbe-citations 7zjh" style="background-color:#fffaf0;"></div>
+==See Also==
+*[[Ion channels 3D structures|Ion channels 3D structures]]
 == References ==
 <references/>

7zjh

From Proteopedia

Current revision

TRPV2-C16+Pro-2

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

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