Compound containing farnesyl diphosphate for modulating TRPV3 function and use thereof
View Patent ↗The present invention relates to a method for activating TRPV3 (transient receptor potential vanilloid 3) using FPP (farnesyl diphosphate) and a method for screening a TRPV3 activity inhibitor. FPP of the present invention has TRPV3 specific activity and therefore it can be effectively used for the study on TRPV3 mechanism and functions and for the development of a TRPV3 based pain reliever.
1. A method for activating TRPV3 (transient receptor potential vanilloid 3) containing the step of contacting FPP (farnesyl diphosphate) with a transformant prepared by transfecting a host cell with a plasmid comprising a polynucleotide encoding TRPV3.
2. The method for activating TRPV3 according to claim 1 , wherein the FPP activates TRPV3 specifically.
3. A method for screening one or more TRPV3 activity inhibitor candidates comprising the following steps:
1) constructing a transformant by transfecting a host cell with a plasmid comprising a polynucleotide encoding TRPV3;
2) treating the transformant with FPP alone (positive control), and treating the transformant with FPP and TRPV3 activity inhibitor candidates (experimental group);
3) measuring TRPV3 ion channel activities in the experimental group and in the control group of step 2); and
4) selecting TRPV3 activity inhibitor candidates that demonstrate an inhibitory effect compared with the positive control.
4. The method for screening one or more TRPV3 activity inhibitor candidates according to claim 3 , wherein the FPP is administered at a concentration of 10-1000 μM.
5. The method for screening one or more TRPV3 activity inhibitor candidates according to claim 3 , wherein the one or more candidates are selected from the group consisting of natural compounds, synthetic compounds, RNA, DNA, polypeptides, enzymes, proteins, ligands, antibodies, antigens, bacterial or fungal metabolites and biological molecules.
6. The method for screening one or more TRPV3 activity inhibitor candidates according to claim 3 , wherein the measurement of TRPV3 activity in step 3) is performed by whole cell voltage clamp technique or calcium imaging.