Matches in SemOpenAlex for { <https://semopenalex.org/work/W2111915171> ?p ?o ?g. }
- W2111915171 endingPage "18595" @default.
- W2111915171 startingPage "18590" @default.
- W2111915171 abstract "Levamisole-sensitive acetylcholine receptors (L-AChRs) are ligand-gated ion channels that mediate excitatory neurotransmission at the neuromuscular junctions of nematodes. They constitute a major drug target for anthelminthic treatments because they can be activated by nematode-specific cholinergic agonists such as levamisole. Genetic screens conducted in Caenorhabditis elegans for resistance to levamisole toxicity identified genes that are indispensable for the biosynthesis of L-AChRs. These include 5 genes encoding distinct AChR subunits and 3 genes coding for ancillary proteins involved in assembly and trafficking of the receptors. Despite extensive analysis of L-AChRs in vivo, pharmacological and biophysical characterization of these receptors has been greatly hampered by the absence of a heterologous expression system. Using Xenopus laevis oocytes, we were able to reconstitute functional L-AChRs by coexpressing the 5 distinct receptor subunits and the 3 ancillary proteins. Strikingly, this system recapitulates the genetic requirements for receptor expression in vivo because omission of any of these 8 genes dramatically impairs L-AChR expression. We demonstrate that 3 alpha- and 2 non-alpha-subunits assemble into the same receptor. Pharmacological analysis reveals that the prototypical cholinergic agonist nicotine is unable to activate L-AChRs but rather acts as a potent allosteric inhibitor. These results emphasize the role of ancillary proteins for efficient expression of recombinant neurotransmitter receptors and open the way for in vitro screening of novel anthelminthic agents." @default.
- W2111915171 created "2016-06-24" @default.
- W2111915171 creator A5024892015 @default.
- W2111915171 creator A5032755408 @default.
- W2111915171 creator A5043259469 @default.
- W2111915171 creator A5067251751 @default.
- W2111915171 creator A5077631330 @default.
- W2111915171 creator A5090649044 @default.
- W2111915171 date "2008-11-25" @default.
- W2111915171 modified "2023-10-14" @default.
- W2111915171 title "Eight genes are required for functional reconstitution of the <i>Caenorhabditis elegans</i> levamisole-sensitive acetylcholine receptor" @default.
- W2111915171 cites W1510221241 @default.
- W2111915171 cites W1605667399 @default.
- W2111915171 cites W1840564118 @default.
- W2111915171 cites W1900806927 @default.
- W2111915171 cites W1944127002 @default.
- W2111915171 cites W1954391111 @default.
- W2111915171 cites W1964737820 @default.
- W2111915171 cites W1965278459 @default.
- W2111915171 cites W1971083012 @default.
- W2111915171 cites W1972833869 @default.
- W2111915171 cites W1975624561 @default.
- W2111915171 cites W1975676315 @default.
- W2111915171 cites W1998279724 @default.
- W2111915171 cites W2000197813 @default.
- W2111915171 cites W2003804798 @default.
- W2111915171 cites W2004412059 @default.
- W2111915171 cites W2009245253 @default.
- W2111915171 cites W2010199408 @default.
- W2111915171 cites W2014629704 @default.
- W2111915171 cites W2023925525 @default.
- W2111915171 cites W2043236058 @default.
- W2111915171 cites W2044163971 @default.
- W2111915171 cites W2044849212 @default.
- W2111915171 cites W2051003806 @default.
- W2111915171 cites W2056174828 @default.
- W2111915171 cites W2059234084 @default.
- W2111915171 cites W2061407938 @default.
- W2111915171 cites W2070649188 @default.
- W2111915171 cites W2070706872 @default.
- W2111915171 cites W2074454109 @default.
- W2111915171 cites W2090690189 @default.
- W2111915171 cites W2098005352 @default.
- W2111915171 cites W2099542365 @default.
- W2111915171 cites W2102201378 @default.
- W2111915171 cites W2111622691 @default.
- W2111915171 cites W2116394768 @default.
- W2111915171 cites W2130233455 @default.
- W2111915171 cites W2136019568 @default.
- W2111915171 cites W2165797782 @default.
- W2111915171 cites W2166792915 @default.
- W2111915171 doi "https://doi.org/10.1073/pnas.0806933105" @default.
- W2111915171 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2587545" @default.
- W2111915171 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19020092" @default.
- W2111915171 hasPublicationYear "2008" @default.
- W2111915171 type Work @default.
- W2111915171 sameAs 2111915171 @default.
- W2111915171 citedByCount "168" @default.
- W2111915171 countsByYear W21119151712012 @default.
- W2111915171 countsByYear W21119151712013 @default.
- W2111915171 countsByYear W21119151712014 @default.
- W2111915171 countsByYear W21119151712015 @default.
- W2111915171 countsByYear W21119151712016 @default.
- W2111915171 countsByYear W21119151712017 @default.
- W2111915171 countsByYear W21119151712018 @default.
- W2111915171 countsByYear W21119151712019 @default.
- W2111915171 countsByYear W21119151712020 @default.
- W2111915171 countsByYear W21119151712021 @default.
- W2111915171 countsByYear W21119151712022 @default.
- W2111915171 countsByYear W21119151712023 @default.
- W2111915171 crossrefType "journal-article" @default.
- W2111915171 hasAuthorship W2111915171A5024892015 @default.
- W2111915171 hasAuthorship W2111915171A5032755408 @default.
- W2111915171 hasAuthorship W2111915171A5043259469 @default.
- W2111915171 hasAuthorship W2111915171A5067251751 @default.
- W2111915171 hasAuthorship W2111915171A5077631330 @default.
- W2111915171 hasAuthorship W2111915171A5090649044 @default.
- W2111915171 hasBestOaLocation W21119151712 @default.
- W2111915171 hasConcept C104317684 @default.
- W2111915171 hasConcept C108305142 @default.
- W2111915171 hasConcept C169760540 @default.
- W2111915171 hasConcept C170493617 @default.
- W2111915171 hasConcept C22885893 @default.
- W2111915171 hasConcept C2775910092 @default.
- W2111915171 hasConcept C2778944004 @default.
- W2111915171 hasConcept C40767141 @default.
- W2111915171 hasConcept C55493867 @default.
- W2111915171 hasConcept C80161118 @default.
- W2111915171 hasConcept C86803240 @default.
- W2111915171 hasConcept C95444343 @default.
- W2111915171 hasConcept C98274493 @default.
- W2111915171 hasConceptScore W2111915171C104317684 @default.
- W2111915171 hasConceptScore W2111915171C108305142 @default.
- W2111915171 hasConceptScore W2111915171C169760540 @default.
- W2111915171 hasConceptScore W2111915171C170493617 @default.
- W2111915171 hasConceptScore W2111915171C22885893 @default.
- W2111915171 hasConceptScore W2111915171C2775910092 @default.
- W2111915171 hasConceptScore W2111915171C2778944004 @default.