Matches in SemOpenAlex for { <https://semopenalex.org/work/W4367366180> ?p ?o ?g. }
- W4367366180 abstract "Abstract The μ-opioid receptor (μOR) is an important target for pain management and the molecular understanding of drug action will facilitate the development of better therapeutics. Here we show, using double electron-electron resonance (DEER) and single-molecule fluorescence resonance energy transfer (smFRET), how ligand-specific conformational changes of the μOR translate into a broad range of intrinsic efficacies at the transducer level. We identify several cytoplasmic receptor conformations interconverting on different timescales, including a pre-activated receptor conformation which is capable of G protein binding, and a fully activated conformation which dramatically lowers GDP affinity within the ternary complex. Interaction of β-arrestin-1 with the μOR core binding site appears less specific and occurs with much lower affinity than binding of G protein G i . One-Sentence Summary Ligand-dependent conformational dynamics of the μ-opioid receptor determine downstream signaling efficacy." @default.
- W4367366180 created "2023-04-30" @default.
- W4367366180 creator A5000409712 @default.
- W4367366180 creator A5002248774 @default.
- W4367366180 creator A5032410588 @default.
- W4367366180 creator A5036133609 @default.
- W4367366180 creator A5050776292 @default.
- W4367366180 creator A5063926315 @default.
- W4367366180 creator A5066945113 @default.
- W4367366180 creator A5079682203 @default.
- W4367366180 creator A5079816239 @default.
- W4367366180 creator A5087186394 @default.
- W4367366180 creator A5091597046 @default.
- W4367366180 date "2023-04-29" @default.
- W4367366180 modified "2023-09-30" @default.
- W4367366180 title "Conformational dynamics of the μ-opioid receptor determine ligand intrinsic efficacy" @default.
- W4367366180 cites W1490029082 @default.
- W4367366180 cites W1560061125 @default.
- W4367366180 cites W1918796765 @default.
- W4367366180 cites W1975740938 @default.
- W4367366180 cites W1993343824 @default.
- W4367366180 cites W1995376165 @default.
- W4367366180 cites W2001302355 @default.
- W4367366180 cites W2015087988 @default.
- W4367366180 cites W2024847911 @default.
- W4367366180 cites W2030632688 @default.
- W4367366180 cites W2064562717 @default.
- W4367366180 cites W2083725367 @default.
- W4367366180 cites W2102459914 @default.
- W4367366180 cites W2103364571 @default.
- W4367366180 cites W2109083102 @default.
- W4367366180 cites W2132316084 @default.
- W4367366180 cites W2162435350 @default.
- W4367366180 cites W2164662577 @default.
- W4367366180 cites W2165671231 @default.
- W4367366180 cites W2211369331 @default.
- W4367366180 cites W2507665026 @default.
- W4367366180 cites W2512819857 @default.
- W4367366180 cites W2520075163 @default.
- W4367366180 cites W2624652951 @default.
- W4367366180 cites W2737272816 @default.
- W4367366180 cites W2770319189 @default.
- W4367366180 cites W2777807685 @default.
- W4367366180 cites W2794409435 @default.
- W4367366180 cites W2807850657 @default.
- W4367366180 cites W2809303314 @default.
- W4367366180 cites W2909204744 @default.
- W4367366180 cites W2910817182 @default.
- W4367366180 cites W2941121164 @default.
- W4367366180 cites W2944643389 @default.
- W4367366180 cites W2944677299 @default.
- W4367366180 cites W3000145087 @default.
- W4367366180 cites W3006232652 @default.
- W4367366180 cites W3015123576 @default.
- W4367366180 cites W3030533699 @default.
- W4367366180 cites W3090176044 @default.
- W4367366180 cites W3093130791 @default.
- W4367366180 cites W3110321636 @default.
- W4367366180 cites W3160957009 @default.
- W4367366180 cites W3164232678 @default.
- W4367366180 cites W4200388193 @default.
- W4367366180 cites W4220751234 @default.
- W4367366180 cites W4309660299 @default.
- W4367366180 doi "https://doi.org/10.1101/2023.04.28.538657" @default.
- W4367366180 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/37163120" @default.
- W4367366180 hasPublicationYear "2023" @default.
- W4367366180 type Work @default.
- W4367366180 citedByCount "3" @default.
- W4367366180 countsByYear W43673661802023 @default.
- W4367366180 crossrefType "posted-content" @default.
- W4367366180 hasAuthorship W4367366180A5000409712 @default.
- W4367366180 hasAuthorship W4367366180A5002248774 @default.
- W4367366180 hasAuthorship W4367366180A5032410588 @default.
- W4367366180 hasAuthorship W4367366180A5036133609 @default.
- W4367366180 hasAuthorship W4367366180A5050776292 @default.
- W4367366180 hasAuthorship W4367366180A5063926315 @default.
- W4367366180 hasAuthorship W4367366180A5066945113 @default.
- W4367366180 hasAuthorship W4367366180A5079682203 @default.
- W4367366180 hasAuthorship W4367366180A5079816239 @default.
- W4367366180 hasAuthorship W4367366180A5087186394 @default.
- W4367366180 hasAuthorship W4367366180A5091597046 @default.
- W4367366180 hasBestOaLocation W43673661801 @default.
- W4367366180 hasConcept C116569031 @default.
- W4367366180 hasConcept C121332964 @default.
- W4367366180 hasConcept C12554922 @default.
- W4367366180 hasConcept C135285700 @default.
- W4367366180 hasConcept C147597530 @default.
- W4367366180 hasConcept C170493617 @default.
- W4367366180 hasConcept C181199279 @default.
- W4367366180 hasConcept C185592680 @default.
- W4367366180 hasConcept C2777339483 @default.
- W4367366180 hasConcept C2778938600 @default.
- W4367366180 hasConcept C2779886867 @default.
- W4367366180 hasConcept C2781063702 @default.
- W4367366180 hasConcept C38533456 @default.
- W4367366180 hasConcept C55493867 @default.
- W4367366180 hasConcept C59593255 @default.
- W4367366180 hasConcept C62520636 @default.
- W4367366180 hasConcept C71240020 @default.
- W4367366180 hasConcept C86756495 @default.