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The response of PKD1L3 / PKD2L1 to acid stimuli is inhibited by capsaicin and its pungent analogs
Author(s) -
Ishii Sho,
Kurokawa Azusa,
Kishi Mikiya,
Yamagami Keigo,
Okada Shinji,
Ishimaru Yoshiro,
Misaka Takumi
Publication year - 2012
Publication title -
the febs journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.981
H-Index - 204
eISSN - 1742-4658
pISSN - 1742-464X
DOI - 10.1111/j.1742-4658.2012.08566.x
Subject(s) - transient receptor potential channel , trpv1 , capsaicin , hek 293 cells , chemistry , pharmacology , microbiology and biotechnology , biochemistry , receptor , biology
Polycystic kidney disease (PKD) 2L1 protein is a member of the transient receptor potential (TRP) ion channel family. In circumvallate and foliate papillae, PKD2L1 is coexpressed with PKD1L3. PKD2L1 and PKD1L3 interact through their transmembrane domain and the resulting heteromer PKD1L3/PKD2L1 owns a unique channel property called ‘off‐responses’ to acid stimulation, although PKD2L1 does not own this property by itself. To define the pharmacological properties of the PKD1L3/PKD2L1 channel, we developed a new method to effectively evaluate channel activity using human embryonic kidney 293T cells in which the channel was heterologously expressed. This method was applied to screen substances that potentially regulate it. We found that capsaicin and its analogs, which are TRPV1 agonists, inhibited the response to acid stimuli and that the capsaicin inhibition was reversible with an IC 50 of 32.5 μ m . Capsaicin and its analogs are thus useful tools for physiological analysis of PKD1L3/PKD2L1 function. Database
Nucleotide sequence data are available in the GenBank database under the accession numbers hTRPA1, BC148423 and hTRPV3, BC104866

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