Matches in SemOpenAlex for { <https://semopenalex.org/work/W2890621053> ?p ?o ?g. }
- W2890621053 endingPage "8281" @default.
- W2890621053 startingPage "8255" @default.
- W2890621053 abstract "The transient receptor potential vanilloid type-2 (TRPV2) protein is a nonselective Ca2+ permeable channel member of the TRPV subfamily, still considered an orphan TRP channel due to the scarcity of available selective and potent pharmacological tools and endogenous modulators. Here we describe the discovery of novel synthetic long-chain capsaicin derivatives as potent TRPV2 antagonists in comparison to the totally inactive capsaicin, the role of their hydrophobic chain, and how the structure–activity relationships of such derivatives led, through a ligand-based approach, to the identification of endogenous long-chain fatty acid ethanolamides or primary amides acting as TRPV2 antagonists. Both synthetic and endogenous antagonists exhibited differential inhibition against known TRPV2 agonists characterized by distinct kinetic profiles. These findings represent the first example of both synthetic and naturally occurring TRPV2 modulators with efficacy in the submicromolar/low-micromolar range, which will be useful for clarifying the physiopathological roles of this receptor, its regulation, and its targeting in pathological conditions." @default.
- W2890621053 created "2018-09-27" @default.
- W2890621053 creator A5007484138 @default.
- W2890621053 creator A5007784336 @default.
- W2890621053 creator A5011475191 @default.
- W2890621053 creator A5027199589 @default.
- W2890621053 creator A5037793543 @default.
- W2890621053 creator A5043589092 @default.
- W2890621053 creator A5075031849 @default.
- W2890621053 creator A5076395210 @default.
- W2890621053 creator A5087596417 @default.
- W2890621053 date "2018-09-03" @default.
- W2890621053 modified "2023-10-16" @default.
- W2890621053 title "Elongation of the Hydrophobic Chain as a Molecular Switch: Discovery of Capsaicin Derivatives and Endogenous Lipids as Potent Transient Receptor Potential Vanilloid Channel 2 Antagonists" @default.
- W2890621053 cites W1495409864 @default.
- W2890621053 cites W1554059507 @default.
- W2890621053 cites W183810266 @default.
- W2890621053 cites W1943289153 @default.
- W2890621053 cites W1965654804 @default.
- W2890621053 cites W1965962126 @default.
- W2890621053 cites W1971379872 @default.
- W2890621053 cites W1973796039 @default.
- W2890621053 cites W1976441157 @default.
- W2890621053 cites W1983377357 @default.
- W2890621053 cites W1986500032 @default.
- W2890621053 cites W1987533819 @default.
- W2890621053 cites W1991972386 @default.
- W2890621053 cites W1992510938 @default.
- W2890621053 cites W1995655158 @default.
- W2890621053 cites W1999212252 @default.
- W2890621053 cites W1999522081 @default.
- W2890621053 cites W2001734687 @default.
- W2890621053 cites W2003403297 @default.
- W2890621053 cites W2007422532 @default.
- W2890621053 cites W2019879792 @default.
- W2890621053 cites W2040826892 @default.
- W2890621053 cites W2042968117 @default.
- W2890621053 cites W2043588922 @default.
- W2890621053 cites W2068839583 @default.
- W2890621053 cites W2069380892 @default.
- W2890621053 cites W2071947898 @default.
- W2890621053 cites W2077033210 @default.
- W2890621053 cites W2078120062 @default.
- W2890621053 cites W2080134430 @default.
- W2890621053 cites W2082632171 @default.
- W2890621053 cites W2085842962 @default.
- W2890621053 cites W2097824035 @default.
- W2890621053 cites W2119071913 @default.
- W2890621053 cites W2120806902 @default.
- W2890621053 cites W2129900856 @default.
- W2890621053 cites W2138376387 @default.
- W2890621053 cites W2138841389 @default.
- W2890621053 cites W2140122645 @default.
- W2890621053 cites W2150475011 @default.
- W2890621053 cites W2153704362 @default.
- W2890621053 cites W2156231244 @default.
- W2890621053 cites W2158518114 @default.
- W2890621053 cites W2167663419 @default.
- W2890621053 cites W2301186499 @default.
- W2890621053 cites W2303419544 @default.
- W2890621053 cites W2320219233 @default.
- W2890621053 cites W2323300135 @default.
- W2890621053 cites W2325338221 @default.
- W2890621053 cites W2408461971 @default.
- W2890621053 cites W2421422434 @default.
- W2890621053 cites W2474477322 @default.
- W2890621053 cites W2566870701 @default.
- W2890621053 cites W2618247170 @default.
- W2890621053 cites W2802330091 @default.
- W2890621053 cites W4248458349 @default.
- W2890621053 cites W4251203321 @default.
- W2890621053 doi "https://doi.org/10.1021/acs.jmedchem.8b00734" @default.
- W2890621053 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30176215" @default.
- W2890621053 hasPublicationYear "2018" @default.
- W2890621053 type Work @default.
- W2890621053 sameAs 2890621053 @default.
- W2890621053 citedByCount "11" @default.
- W2890621053 countsByYear W28906210532019 @default.
- W2890621053 countsByYear W28906210532020 @default.
- W2890621053 countsByYear W28906210532021 @default.
- W2890621053 countsByYear W28906210532022 @default.
- W2890621053 countsByYear W28906210532023 @default.
- W2890621053 crossrefType "journal-article" @default.
- W2890621053 hasAuthorship W2890621053A5007484138 @default.
- W2890621053 hasAuthorship W2890621053A5007784336 @default.
- W2890621053 hasAuthorship W2890621053A5011475191 @default.
- W2890621053 hasAuthorship W2890621053A5027199589 @default.
- W2890621053 hasAuthorship W2890621053A5037793543 @default.
- W2890621053 hasAuthorship W2890621053A5043589092 @default.
- W2890621053 hasAuthorship W2890621053A5075031849 @default.
- W2890621053 hasAuthorship W2890621053A5076395210 @default.
- W2890621053 hasAuthorship W2890621053A5087596417 @default.
- W2890621053 hasBestOaLocation W28906210532 @default.
- W2890621053 hasConcept C155164980 @default.
- W2890621053 hasConcept C160145004 @default.
- W2890621053 hasConcept C16613235 @default.
- W2890621053 hasConcept C170493617 @default.
- W2890621053 hasConcept C185592680 @default.