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Structure paper

TitleStructural basis of TRPC4 regulation by calmodulin and pharmacological agents.
Journal, issue, pagesElife, Vol. 9, Year 2020
Publish dateNov 25, 2020
AuthorsDeivanayagabarathy Vinayagam / Dennis Quentin / Jing Yu-Strzelczyk / Oleg Sitsel / Felipe Merino / Markus Stabrin / Oliver Hofnagel / Maolin Yu / Mark W Ledeboer / Georg Nagel / Goran Malojcic / Stefan Raunser /
PubMed AbstractCanonical transient receptor potential channels (TRPC) are involved in receptor-operated and/or store-operated Ca signaling. Inhibition of TRPCs by small molecules was shown to be promising in ...Canonical transient receptor potential channels (TRPC) are involved in receptor-operated and/or store-operated Ca signaling. Inhibition of TRPCs by small molecules was shown to be promising in treating renal diseases. In cells, the channels are regulated by calmodulin (CaM). Molecular details of both CaM and drug binding have remained elusive so far. Here, we report structures of TRPC4 in complex with three pyridazinone-based inhibitors and CaM. The structures reveal that all the inhibitors bind to the same cavity of the voltage-sensing-like domain and allow us to describe how structural changes from the ligand-binding site can be transmitted to the central ion-conducting pore of TRPC4. CaM binds to the rib helix of TRPC4, which results in the ordering of a previously disordered region, fixing the channel in its closed conformation. This represents a novel CaM-induced regulatory mechanism of canonical TRP channels.
External linksElife / PubMed:33236980 / PubMed Central
MethodsEM (single particle)
Resolution2.85 - 3.8 Å
Structure data

11957

7b05

EMDB-11957, PDB-7b05:
TRPC4 in complex with inhibitor GFB-8749
Method: EM (single particle) / Resolution: 3.8 Å

11968

7b0j

EMDB-11968, PDB-7b0j:
TRPC4 in LMNG detergent
Method: EM (single particle) / Resolution: 2.85 Å

11970

7b0s

EMDB-11970, PDB-7b0s:
TRPC4 in complex with inhibitor GFB-8438
Method: EM (single particle) / Resolution: 3.6 Å

11979

7b16

EMDB-11979, PDB-7b16:
TRPC4 in complex with inhibitor GFB-9289
Method: EM (single particle) / Resolution: 3.15 Å

11985

7b1g

EMDB-11985, PDB-7b1g:
TRPC4 in complex with Calmodulin
Method: EM (single particle) / Resolution: 3.6 Å

Chemicals

ChemComp-SJQ:
4-[4-[[4,4-bis(fluoranyl)cyclohexyl]methyl]-3-oxidanylidene-piperazin-1-yl]-5-chloranyl-1~{H}-pyridazin-6-one

ChemComp-CA:
Unknown entry

ChemComp-44E:
(2R)-3-(phosphonooxy)propane-1,2-diyl dihexanoate / phospholipid*YM

ChemComp-LPP:
2-(HEXADECANOYLOXY)-1-[(PHOSPHONOOXY)METHYL]ETHYL HEXADECANOATE / phospholipid*YM

ChemComp-S9Q:
5-chloranyl-4-[3-oxidanylidene-4-[[2-(trifluoromethyl)phenyl]methyl]piperazin-1-yl]-1~{H}-pyridazin-6-one

ChemComp-SKQ:
5-chloranyl-4-(4-cyclohexyl-3-oxidanylidene-piperazin-1-yl)-1~{H}-pyridazin-6-one

Source
  • danio rerio (zebrafish)
  • mus musculus (house mouse)
KeywordsTRANSPORT PROTEIN / ION CHANNEL / TRPC4 / INHIBITOR / COMPLEX / MEMBRANE PROTEIN / LMNG / CALMODULIN

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