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Structure paper

TitleStructural basis of TRPV3 inhibition by an antagonist.
Journal, issue, pagesNat Chem Biol, Vol. 19, Issue 1, Page 81-90, Year 2023
Publish dateOct 27, 2022
AuthorsJunping Fan / Linghan Hu / Zongwei Yue / Daohong Liao / Fusheng Guo / Han Ke / Daohua Jiang / Yong Yang / Xiaoguang Lei /
PubMed AbstractThe TRPV3 channel plays vital roles in skin physiology. Dysfunction of TRPV3 causes skin diseases, including Olmsted syndrome. However, the lack of potent and selective inhibitors impedes the ...The TRPV3 channel plays vital roles in skin physiology. Dysfunction of TRPV3 causes skin diseases, including Olmsted syndrome. However, the lack of potent and selective inhibitors impedes the validation of TRPV3 as a therapeutic target. In this study, we identified Trpvicin as a potent and subtype-selective inhibitor of TRPV3. Trpvicin exhibits pharmacological potential in the inhibition of itch and hair loss in mouse models. Cryogenic electron microscopy structures of TRPV3 and the pathogenic G573S mutant complexed with Trpvicin reveal detailed ligand-binding sites, suggesting that Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state. Our G573S mutant structures demonstrate that the mutation causes a dilated pore, generating constitutive opening activity. Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel the channel symmetry and block the channel. Together, our results provide mechanistic insights into the inhibition of TRPV3 by Trpvicin and support TRPV3-related drug development.
External linksNat Chem Biol / PubMed:36302896
MethodsEM (single particle)
Resolution2.53 - 3.64 Å
Structure data

33214

7xj0

EMDB-33214, PDB-7xj0:
Structure of human TRPV3 in complex with Trpvicin
Method: EM (single particle) / Resolution: 2.53 Å

33216

7xj1

EMDB-33216, PDB-7xj1:
Structure of human TRPV3_G573S in complex with Trpvicin in C2 symmetry
Method: EM (single particle) / Resolution: 2.93 Å

33217

7xj2

EMDB-33217, PDB-7xj2:
Structure of human TRPV3_G573S in complex with Trpvicin in C4 symmetry
Method: EM (single particle) / Resolution: 3.64 Å

33218

7xj3

EMDB-33218, PDB-7xj3:
Structure of human TRPV3
Method: EM (single particle) / Resolution: 3.54 Å

Chemicals

ChemComp-6OU:
[(2~{R})-1-[2-azanylethoxy(oxidanyl)phosphoryl]oxy-3-hexadecanoyloxy-propan-2-yl] (~{Z})-octadec-9-enoate / phospholipid*YM

ChemComp-EQK:
N-[5-[2-(2-cyanopropan-2-yl)pyridin-4-yl]-4-(trifluoromethyl)-1,3-thiazol-2-yl]-4,6-dimethoxy-pyrimidine-5-carboxamide

Source
  • homo sapiens (human)
KeywordsMEMBRANE PROTEIN / channel

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