FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1982713585> ?p ?o ?g. }

• W1982713585 endingPage "1640" @default.
• W1982713585 startingPage "1628" @default.
• W1982713585 abstract "The transient receptor potential vanilloid 1 (TRPV1) channel is a thermosensory receptor implicated in diverse physiological and pathological processes. The TRP domain, a highly conserved region in the C terminus adjacent to the internal channel gate, is critical for subunit tetramerization and channel gating. Here, we show that cell-penetrating, membrane-anchored peptides patterned after this protein domain are moderate and selective TRPV1 antagonists both in vitro and in vivo, blocking receptor activity in intact rat primary sensory neurons and their peripheral axons with mean decline time of 30 min. The most potent lipopeptide, TRP-p5, blocked all modes of TRPV1 gating with micromolar efficacy (IC(50)<10 μM), without significantly affecting other thermoTRP channels. In contrast, its retrosequence or the corresponding sequences of other TRPV channels did not alter TRPV1 channel activity (IC(50)>100 μM). TRP-p5 did not affect the capsaicin sensitivity of the vanilloid receptor. Our data suggest that TRP-p5 interferes with protein-protein interactions at the level of the TRP domain that are essential for the conformational change that leads to gate opening. Therefore, these palmitoylated peptides, which we termed TRPducins, are noncompetitive, voltage-independent, sequence-specific TRPV1 blockers. Our findings indicate that TRPducin-like peptides may embody a novel molecular strategy that can be exploited to generate a selective pharmacological arsenal for the TRP superfamily of ion channels." @default.
• W1982713585 created "2016-06-24" @default.
• W1982713585 creator A5005736456 @default.
• W1982713585 creator A5007659587 @default.
• W1982713585 creator A5014885640 @default.
• W1982713585 creator A5024358687 @default.
• W1982713585 creator A5038934665 @default.
• W1982713585 creator A5058686844 @default.
• W1982713585 creator A5068542139 @default.
• W1982713585 creator A5069047258 @default.
• W1982713585 creator A5071387984 @default.
• W1982713585 creator A5081710490 @default.
• W1982713585 creator A5090824399 @default.
• W1982713585 date "2011-02-09" @default.
• W1982713585 modified "2023-10-13" @default.
• W1982713585 title "Membrane‐tethered peptides patterned after the TRP domain (TRPducins) selectively inhibit TRPV1 channel activity" @default.
• W1982713585 cites W1501520755 @default.
• W1982713585 cites W1972811533 @default.
• W1982713585 cites W1978275908 @default.
• W1982713585 cites W1985020794 @default.
• W1982713585 cites W1986696922 @default.
• W1982713585 cites W1990769918 @default.
• W1982713585 cites W1995705528 @default.
• W1982713585 cites W2001500190 @default.
• W1982713585 cites W2006187306 @default.
• W1982713585 cites W2007034094 @default.
• W1982713585 cites W2009294684 @default.
• W1982713585 cites W2009967312 @default.
• W1982713585 cites W2010739774 @default.
• W1982713585 cites W2028438640 @default.
• W1982713585 cites W2029263118 @default.
• W1982713585 cites W2032087136 @default.
• W1982713585 cites W2036189937 @default.
• W1982713585 cites W2039246411 @default.
• W1982713585 cites W2046856170 @default.
• W1982713585 cites W2047900214 @default.
• W1982713585 cites W2048180094 @default.
• W1982713585 cites W2050781058 @default.
• W1982713585 cites W2054558066 @default.
• W1982713585 cites W2057709157 @default.
• W1982713585 cites W2059452728 @default.
• W1982713585 cites W2063030604 @default.
• W1982713585 cites W2064374911 @default.
• W1982713585 cites W2071939666 @default.
• W1982713585 cites W2073606727 @default.
• W1982713585 cites W2075715972 @default.
• W1982713585 cites W2088450431 @default.
• W1982713585 cites W2089357523 @default.
• W1982713585 cites W2098203510 @default.
• W1982713585 cites W2129326126 @default.
• W1982713585 cites W2133738718 @default.
• W1982713585 cites W2155935601 @default.
• W1982713585 cites W2166917110 @default.
• W1982713585 cites W2168621999 @default.
• W1982713585 cites W2170873073 @default.
• W1982713585 cites W3023338839 @default.
• W1982713585 cites W4233595534 @default.
• W1982713585 doi "https://doi.org/10.1096/fj.10-174433" @default.
• W1982713585 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21307333" @default.
• W1982713585 hasPublicationYear "2011" @default.
• W1982713585 type Work @default.
• W1982713585 sameAs 1982713585 @default.
• W1982713585 citedByCount "37" @default.
• W1982713585 countsByYear W19827135852012 @default.
• W1982713585 countsByYear W19827135852014 @default.
• W1982713585 countsByYear W19827135852015 @default.
• W1982713585 countsByYear W19827135852016 @default.
• W1982713585 countsByYear W19827135852017 @default.
• W1982713585 countsByYear W19827135852018 @default.
• W1982713585 countsByYear W19827135852019 @default.
• W1982713585 countsByYear W19827135852020 @default.
• W1982713585 countsByYear W19827135852022 @default.
• W1982713585 countsByYear W19827135852023 @default.
• W1982713585 crossrefType "journal-article" @default.
• W1982713585 hasAuthorship W1982713585A5005736456 @default.
• W1982713585 hasAuthorship W1982713585A5007659587 @default.
• W1982713585 hasAuthorship W1982713585A5014885640 @default.
• W1982713585 hasAuthorship W1982713585A5024358687 @default.
• W1982713585 hasAuthorship W1982713585A5038934665 @default.
• W1982713585 hasAuthorship W1982713585A5058686844 @default.
• W1982713585 hasAuthorship W1982713585A5068542139 @default.
• W1982713585 hasAuthorship W1982713585A5069047258 @default.
• W1982713585 hasAuthorship W1982713585A5071387984 @default.
• W1982713585 hasAuthorship W1982713585A5081710490 @default.
• W1982713585 hasAuthorship W1982713585A5090824399 @default.
• W1982713585 hasBestOaLocation W19827135852 @default.
• W1982713585 hasConcept C12554922 @default.
• W1982713585 hasConcept C155164980 @default.
• W1982713585 hasConcept C160145004 @default.
• W1982713585 hasConcept C170493617 @default.
• W1982713585 hasConcept C185592680 @default.
• W1982713585 hasConcept C194544171 @default.
• W1982713585 hasConcept C2780051329 @default.
• W1982713585 hasConcept C50254741 @default.
• W1982713585 hasConcept C55493867 @default.
• W1982713585 hasConcept C86803240 @default.
• W1982713585 hasConcept C95444343 @default.
• W1982713585 hasConceptScore W1982713585C12554922 @default.

• next