Matches in SemOpenAlex for { <https://semopenalex.org/work/W2065497251> ?p ?o ?g. }
Showing items 1 to 76 of
76
with 100 items per page.
- W2065497251 abstract "Sphingosine-1-phosphate (S1P) is a bioactive lipid with diverse functions, including cell proliferation, differentiation, angiogenesis, chemotaxis, and migration. Many of these activities are mediated through five closely related G-protein-coupled receptors (GPCR) of the S1P receptor (S1PR) family. Because of the technical challenges in crystallization of membrane-bound proteins, S1PR structures have not become publicly available. Instead, homology models were built based on a theoretical model of the retina pigment rhodopsin, which is a GPCR with a covalently bound ligand (Parrill, A. L. et al. J. Biol. Chem. 2000, 275, 39379). Recently, new techniques in crystallization have made more GPCR structures available, including those in complex with their agonist, antagonist, or inverse agonist. These structures provide more realistic basis for building S1PR structural models, and at the same time raise a new question about which structure to use in drug design and virtual screening. In this presentation, two structural models of S1PR subtype 5 (S1PR5, Kothapalli, R, Kusmartseva I, and Loughran Jr T. P. et al. Biochim. Biophys. Acta 2002, 1579, 117) are constructed based on crystal structures of β2-adrenergic receptor (β2AR), one of the most extensively studied GPCR. A nanobody-stabilized active state of β2AR (Soren, G. F. et al. Nature 2011, 469, 175) and an inactive state of β2AR in complex with its partial inverse agonist (Cherezov, V. et al. Science 2007, 318, 1258; Hanson, M. A. et al. Structure 2008, 16, 897) are used in building the two models, which are subsequently tested by in silico docking of their known ligands. The models based on active and inactive β2AR are used in virtual screening to find potential activators and inhibitors, respectively. Results from the two models are compared and their different applications are discussed. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2011 Nov 12-16; San Francisco, CA. Philadelphia (PA): AACR; Mol Cancer Ther 2011;10(11 Suppl):Abstract nr A132." @default.
- W2065497251 created "2016-06-24" @default.
- W2065497251 creator A5021096170 @default.
- W2065497251 date "2011-11-12" @default.
- W2065497251 modified "2023-09-27" @default.
- W2065497251 title "Abstract A132: S1PR5 structural model and its application in drug discovery." @default.
- W2065497251 doi "https://doi.org/10.1158/1535-7163.targ-11-a132" @default.
- W2065497251 hasPublicationYear "2011" @default.
- W2065497251 type Work @default.
- W2065497251 sameAs 2065497251 @default.
- W2065497251 citedByCount "0" @default.
- W2065497251 crossrefType "proceedings-article" @default.
- W2065497251 hasAuthorship W2065497251A5021096170 @default.
- W2065497251 hasConcept C104317684 @default.
- W2065497251 hasConcept C135285700 @default.
- W2065497251 hasConcept C159110408 @default.
- W2065497251 hasConcept C170493617 @default.
- W2065497251 hasConcept C185592680 @default.
- W2065497251 hasConcept C202033177 @default.
- W2065497251 hasConcept C2775905019 @default.
- W2065497251 hasConcept C2778938600 @default.
- W2065497251 hasConcept C2780827179 @default.
- W2065497251 hasConcept C41685203 @default.
- W2065497251 hasConcept C55493867 @default.
- W2065497251 hasConcept C70721500 @default.
- W2065497251 hasConcept C71240020 @default.
- W2065497251 hasConcept C71924100 @default.
- W2065497251 hasConcept C74187038 @default.
- W2065497251 hasConcept C86803240 @default.
- W2065497251 hasConcept C89951826 @default.
- W2065497251 hasConcept C95444343 @default.
- W2065497251 hasConceptScore W2065497251C104317684 @default.
- W2065497251 hasConceptScore W2065497251C135285700 @default.
- W2065497251 hasConceptScore W2065497251C159110408 @default.
- W2065497251 hasConceptScore W2065497251C170493617 @default.
- W2065497251 hasConceptScore W2065497251C185592680 @default.
- W2065497251 hasConceptScore W2065497251C202033177 @default.
- W2065497251 hasConceptScore W2065497251C2775905019 @default.
- W2065497251 hasConceptScore W2065497251C2778938600 @default.
- W2065497251 hasConceptScore W2065497251C2780827179 @default.
- W2065497251 hasConceptScore W2065497251C41685203 @default.
- W2065497251 hasConceptScore W2065497251C55493867 @default.
- W2065497251 hasConceptScore W2065497251C70721500 @default.
- W2065497251 hasConceptScore W2065497251C71240020 @default.
- W2065497251 hasConceptScore W2065497251C71924100 @default.
- W2065497251 hasConceptScore W2065497251C74187038 @default.
- W2065497251 hasConceptScore W2065497251C86803240 @default.
- W2065497251 hasConceptScore W2065497251C89951826 @default.
- W2065497251 hasConceptScore W2065497251C95444343 @default.
- W2065497251 hasLocation W20654972511 @default.
- W2065497251 hasOpenAccess W2065497251 @default.
- W2065497251 hasPrimaryLocation W20654972511 @default.
- W2065497251 hasRelatedWork W1989364758 @default.
- W2065497251 hasRelatedWork W1997313325 @default.
- W2065497251 hasRelatedWork W2020125455 @default.
- W2065497251 hasRelatedWork W2039010330 @default.
- W2065497251 hasRelatedWork W2060874643 @default.
- W2065497251 hasRelatedWork W2079353043 @default.
- W2065497251 hasRelatedWork W2082992054 @default.
- W2065497251 hasRelatedWork W2107998520 @default.
- W2065497251 hasRelatedWork W2130813862 @default.
- W2065497251 hasRelatedWork W2167086539 @default.
- W2065497251 hasRelatedWork W2332247803 @default.
- W2065497251 hasRelatedWork W2342650696 @default.
- W2065497251 hasRelatedWork W2395557655 @default.
- W2065497251 hasRelatedWork W2471992026 @default.
- W2065497251 hasRelatedWork W2769170787 @default.
- W2065497251 hasRelatedWork W2774484667 @default.
- W2065497251 hasRelatedWork W2793051699 @default.
- W2065497251 hasRelatedWork W2920994994 @default.
- W2065497251 hasRelatedWork W2945736625 @default.
- W2065497251 hasRelatedWork W3032456618 @default.
- W2065497251 isParatext "false" @default.
- W2065497251 isRetracted "false" @default.
- W2065497251 magId "2065497251" @default.
- W2065497251 workType "article" @default.