FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2019691875> ?p ?o ?g. }

• W2019691875 endingPage "6719" @default.
• W2019691875 startingPage "6707" @default.
• W2019691875 abstract "Given the importance of G-protein-coupled receptors as pharmacological targets in medicine, efforts directed at understanding the molecular mechanism by which pharmacological compounds regulate their presence at the cell surface is of paramount importance. In this context, using confocal microscopy and bioluminescence resonance energy transfer, we have investigated internalization and intracellular trafficking of the cholecystokinin-2 receptor (CCK2R) in response to both natural and synthetic ligands with different pharmacological features. We found that CCK and gastrin, which are full agonists on CCK2R-induced inositol phosphate production, rapidly and abundantly stimulate internalization. Internalized CCK2R did not rapidly recycle to plasma membrane but instead was directed to late endosomes/lysosomes. CCK2R endocytosis involves clathrin-coated pits and dynamin and high affinity and prolonged binding of β-arrestin1 or -2. Partial agonists and antagonists on CCK2R-induced inositol phosphate formation and ERK1/2 phosphorylation did not stimulate CCK2R internalization or β-arrestin recruitment to the CCK2R but blocked full agonist-induced internalization and β-arrestin recruitment. The extreme C-terminal region of the CCK2R (and more precisely phosphorylatable residues Ser(437)-Xaa(438)-Thr(439)-Thr(440)-Xaa(441)-Ser(442)-Thr(443)) were critical for β-arrestin recruitment. However, this region and β-arrestins were dispensable for CCK2R internalization. In conclusion, this study allowed us to classify the human CCK2R as a member of class B G-protein-coupled receptors with regard to its endocytosis features and identified biased agonists of the CCK2R. These new important insights will allow us to investigate the role of internalized CCK2R·β-arrestin complexes in cancers expressing this receptor and to develop new diagnosis and therapeutic strategies targeting this receptor." @default.
• W2019691875 created "2016-06-24" @default.
• W2019691875 creator A5037683371 @default.
• W2019691875 creator A5044824466 @default.
• W2019691875 creator A5050135007 @default.
• W2019691875 creator A5081053692 @default.
• W2019691875 creator A5091866377 @default.
• W2019691875 creator A5054368831 @default.
• W2019691875 date "2011-02-01" @default.
• W2019691875 modified "2023-10-04" @default.
• W2019691875 title "Regulation of Membrane Cholecystokinin-2 Receptor by Agonists Enables Classification of Partial Agonists as Biased Agonists" @default.
• W2019691875 cites W1884991998 @default.
• W2019691875 cites W1970430112 @default.
• W2019691875 cites W1971057214 @default.
• W2019691875 cites W1971265845 @default.
• W2019691875 cites W1971463295 @default.
• W2019691875 cites W1972513389 @default.
• W2019691875 cites W1974710770 @default.
• W2019691875 cites W1980602971 @default.
• W2019691875 cites W1980987767 @default.
• W2019691875 cites W1983377532 @default.
• W2019691875 cites W1988646125 @default.
• W2019691875 cites W1991158050 @default.
• W2019691875 cites W1994668150 @default.
• W2019691875 cites W2010101046 @default.
• W2019691875 cites W2013134850 @default.
• W2019691875 cites W2015704490 @default.
• W2019691875 cites W2025022118 @default.
• W2019691875 cites W2027119507 @default.
• W2019691875 cites W2030655819 @default.
• W2019691875 cites W2034917348 @default.
• W2019691875 cites W2054009022 @default.
• W2019691875 cites W2059981611 @default.
• W2019691875 cites W2061254153 @default.
• W2019691875 cites W2067005574 @default.
• W2019691875 cites W2073037108 @default.
• W2019691875 cites W2082477622 @default.
• W2019691875 cites W2083334427 @default.
• W2019691875 cites W2089974427 @default.
• W2019691875 cites W2105012896 @default.
• W2019691875 cites W2112032807 @default.
• W2019691875 cites W2117754393 @default.
• W2019691875 cites W2118304925 @default.
• W2019691875 cites W2120539487 @default.
• W2019691875 cites W2123318057 @default.
• W2019691875 cites W2126132542 @default.
• W2019691875 cites W2132877656 @default.
• W2019691875 cites W2135037322 @default.
• W2019691875 cites W2138668301 @default.
• W2019691875 cites W2140452919 @default.
• W2019691875 cites W2142527866 @default.
• W2019691875 cites W2147196684 @default.
• W2019691875 cites W2151526347 @default.
• W2019691875 cites W2151946208 @default.
• W2019691875 cites W2156446121 @default.
• W2019691875 cites W2157426031 @default.
• W2019691875 cites W2166431785 @default.
• W2019691875 cites W2331000103 @default.
• W2019691875 cites W2468102957 @default.
• W2019691875 doi "https://doi.org/10.1074/jbc.m110.196048" @default.
• W2019691875 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3057855" @default.
• W2019691875 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21156802" @default.
• W2019691875 hasPublicationYear "2011" @default.
• W2019691875 type Work @default.
• W2019691875 sameAs 2019691875 @default.
• W2019691875 citedByCount "16" @default.
• W2019691875 countsByYear W20196918752012 @default.
• W2019691875 countsByYear W20196918752013 @default.
• W2019691875 countsByYear W20196918752014 @default.
• W2019691875 countsByYear W20196918752015 @default.
• W2019691875 countsByYear W20196918752017 @default.
• W2019691875 countsByYear W20196918752018 @default.
• W2019691875 countsByYear W20196918752020 @default.
• W2019691875 countsByYear W20196918752022 @default.
• W2019691875 countsByYear W20196918752023 @default.
• W2019691875 crossrefType "journal-article" @default.
• W2019691875 hasAuthorship W2019691875A5037683371 @default.
• W2019691875 hasAuthorship W2019691875A5044824466 @default.
• W2019691875 hasAuthorship W2019691875A5050135007 @default.
• W2019691875 hasAuthorship W2019691875A5054368831 @default.
• W2019691875 hasAuthorship W2019691875A5081053692 @default.
• W2019691875 hasAuthorship W2019691875A5091866377 @default.
• W2019691875 hasBestOaLocation W20196918751 @default.
• W2019691875 hasConcept C102747710 @default.
• W2019691875 hasConcept C135285700 @default.
• W2019691875 hasConcept C139770010 @default.
• W2019691875 hasConcept C156407911 @default.
• W2019691875 hasConcept C170493617 @default.
• W2019691875 hasConcept C185592680 @default.
• W2019691875 hasConcept C2777503648 @default.
• W2019691875 hasConcept C2778938600 @default.
• W2019691875 hasConcept C28005876 @default.
• W2019691875 hasConcept C55493867 @default.
• W2019691875 hasConcept C58732023 @default.
• W2019691875 hasConcept C86803240 @default.
• W2019691875 hasConcept C95444343 @default.
• W2019691875 hasConceptScore W2019691875C102747710 @default.
• W2019691875 hasConceptScore W2019691875C135285700 @default.

• next