Matches in SemOpenAlex for { <https://semopenalex.org/work/W3209839330> ?p ?o ?g. }
Showing items 1 to 90 of
90
with 100 items per page.
- W3209839330 endingPage "64" @default.
- W3209839330 startingPage "55" @default.
- W3209839330 abstract "Transient Receptor Potential Melastatin 5 (TRPM5) is an intracellular calcium-activated cation-selective ion channel expressed in a variety of cell types. Dysfunction of this channel has recently been implied in a range of disease states including diabetes, enteric infections, inflammatory responses, parasitic infection and other pathologies. However, to date, agonists and positive modulators of this channel with sufficient selectivity to enable target validation studies have not been described, limiting the evaluation of TRPM5 biology and its potential as a drug target. We developed a high-throughput assay using a fluorescent membrane potential dye and a medium- and high-throughput electrophysiology assay using QPatch HTX and SyncroPatch 384PE. By employing these assays, we conducted a primary screening campaign and identified hit compounds as TRPM5 channel positive modulators. An initial selectivity profile confirmed hit selectivity to TRPM5 and is presented here. These small molecule TRPM5 compounds have a high potential both as early tool compounds to enable pharmacological studies of TRPM5 and as starting points for the development of potent, selective TRPM5 openers or positive modulators as novel drugs targeting several pathological states." @default.
- W3209839330 created "2021-11-08" @default.
- W3209839330 creator A5009945328 @default.
- W3209839330 creator A5012297677 @default.
- W3209839330 creator A5025838510 @default.
- W3209839330 creator A5027552825 @default.
- W3209839330 creator A5037329190 @default.
- W3209839330 creator A5059736948 @default.
- W3209839330 creator A5072058846 @default.
- W3209839330 creator A5079548097 @default.
- W3209839330 creator A5091411670 @default.
- W3209839330 date "2022-01-01" @default.
- W3209839330 modified "2023-10-14" @default.
- W3209839330 title "Identification of positive modulators of TRPM5 channel from a high-throughput screen using a fluorescent membrane potential assay" @default.
- W3209839330 cites W1604616389 @default.
- W3209839330 cites W1872370054 @default.
- W3209839330 cites W2013483087 @default.
- W3209839330 cites W2068323006 @default.
- W3209839330 cites W2086339199 @default.
- W3209839330 cites W2087355933 @default.
- W3209839330 cites W2121251468 @default.
- W3209839330 cites W2121570525 @default.
- W3209839330 cites W2131825325 @default.
- W3209839330 cites W2148761780 @default.
- W3209839330 cites W2157174760 @default.
- W3209839330 cites W2314754757 @default.
- W3209839330 cites W2528656882 @default.
- W3209839330 cites W2595550011 @default.
- W3209839330 cites W2611575983 @default.
- W3209839330 cites W2614925259 @default.
- W3209839330 cites W2801743977 @default.
- W3209839330 cites W3153248284 @default.
- W3209839330 cites W4211129675 @default.
- W3209839330 cites W4241897948 @default.
- W3209839330 cites W4294748274 @default.
- W3209839330 doi "https://doi.org/10.1016/j.slasd.2021.10.004" @default.
- W3209839330 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35058176" @default.
- W3209839330 hasPublicationYear "2022" @default.
- W3209839330 type Work @default.
- W3209839330 sameAs 3209839330 @default.
- W3209839330 citedByCount "4" @default.
- W3209839330 countsByYear W32098393302022 @default.
- W3209839330 countsByYear W32098393302023 @default.
- W3209839330 crossrefType "journal-article" @default.
- W3209839330 hasAuthorship W3209839330A5009945328 @default.
- W3209839330 hasAuthorship W3209839330A5012297677 @default.
- W3209839330 hasAuthorship W3209839330A5025838510 @default.
- W3209839330 hasAuthorship W3209839330A5027552825 @default.
- W3209839330 hasAuthorship W3209839330A5037329190 @default.
- W3209839330 hasAuthorship W3209839330A5059736948 @default.
- W3209839330 hasAuthorship W3209839330A5072058846 @default.
- W3209839330 hasAuthorship W3209839330A5079548097 @default.
- W3209839330 hasAuthorship W3209839330A5091411670 @default.
- W3209839330 hasBestOaLocation W32098393301 @default.
- W3209839330 hasConcept C12554922 @default.
- W3209839330 hasConcept C185592680 @default.
- W3209839330 hasConcept C51323132 @default.
- W3209839330 hasConcept C55493867 @default.
- W3209839330 hasConcept C74187038 @default.
- W3209839330 hasConcept C86803240 @default.
- W3209839330 hasConcept C98274493 @default.
- W3209839330 hasConceptScore W3209839330C12554922 @default.
- W3209839330 hasConceptScore W3209839330C185592680 @default.
- W3209839330 hasConceptScore W3209839330C51323132 @default.
- W3209839330 hasConceptScore W3209839330C55493867 @default.
- W3209839330 hasConceptScore W3209839330C74187038 @default.
- W3209839330 hasConceptScore W3209839330C86803240 @default.
- W3209839330 hasConceptScore W3209839330C98274493 @default.
- W3209839330 hasIssue "1" @default.
- W3209839330 hasLocation W32098393301 @default.
- W3209839330 hasLocation W32098393302 @default.
- W3209839330 hasOpenAccess W3209839330 @default.
- W3209839330 hasPrimaryLocation W32098393301 @default.
- W3209839330 hasRelatedWork W1466508163 @default.
- W3209839330 hasRelatedWork W1475153 @default.
- W3209839330 hasRelatedWork W1865162173 @default.
- W3209839330 hasRelatedWork W2086566345 @default.
- W3209839330 hasRelatedWork W2124910405 @default.
- W3209839330 hasRelatedWork W2134119452 @default.
- W3209839330 hasRelatedWork W2551232629 @default.
- W3209839330 hasRelatedWork W2614037532 @default.
- W3209839330 hasRelatedWork W2973785834 @default.
- W3209839330 hasRelatedWork W4313446302 @default.
- W3209839330 hasVolume "27" @default.
- W3209839330 isParatext "false" @default.
- W3209839330 isRetracted "false" @default.
- W3209839330 magId "3209839330" @default.
- W3209839330 workType "article" @default.