dc.contributor.author |
Kwon, Y-J
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|
dc.contributor.author |
Lee, W
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|
dc.contributor.author |
Genovesio, A
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dc.contributor.author |
Emans, N
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dc.date.accessioned |
2013-01-30T08:52:32Z |
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dc.date.available |
2013-01-30T08:52:32Z |
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dc.date.issued |
2012-03 |
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dc.identifier.citation |
Kwon, Y-J, Lee, W, Genovesio, A and Emans, N. 2012. A high-content subtractive screen for selecting small molecules affecting internalization of GPCRs. Journal of Biomolecular Screening, vol. 17(3), pp 379-85 |
en_US |
dc.identifier.issn |
1087-0571 |
|
dc.identifier.uri |
http://jbx.sagepub.com/content/early/2011/11/15/1087057111427347
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|
dc.identifier.uri |
http://hdl.handle.net/10204/6498
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|
dc.description |
Copyright: 2012 SAGE Publications. This is an ABSTRACT ONLY. The definitive version is published in Journal of Biomolecular Screening, vol. 17(3), pp 379-85 |
en_US |
dc.description.abstract |
G-protein–coupled receptors (GPCRs) are pivotal in cellular responses to the environment and are common drug targets. Identification of selective small molecules acting on single GPCRs is complicated by the shared machinery coupling signal transduction to physiology. Here, the authors demonstrate a high-content screen using a panel of GPCR assays to identify receptor selective molecules acting within the kinase/phosphatase inhibitor family. A collection of 88 kinase and phosphatase inhibitors was screened against seven agonist-induced GPCR internalization cell models as well as transferrin uptake in human embryonic kidney cells. Molecules acting on a single receptor were identified through excluding pan-specific compounds affecting housekeeping endocytosis or disrupting internalization of multiple receptors. They identified compounds acting on a sole GPCR from activities in a broad range of chemical structures that could not be easily sorted by conventional means. Selective analysis can therefore rapidly select compounds selectively affecting GPCR activity with specificity to one receptor class through high-content screening. |
en_US |
dc.language.iso |
en |
en_US |
dc.publisher |
SAGE Publications |
en_US |
dc.relation.ispartofseries |
Workflow;8510 |
|
dc.subject |
High-content screening |
en_US |
dc.subject |
G-protein–coupled receptor |
en_US |
dc.subject |
Endocytosis |
en_US |
dc.subject |
Cell-based assay |
en_US |
dc.subject |
Image analysis |
en_US |
dc.subject |
Chemical biology |
en_US |
dc.title |
A high-content subtractive screen for selecting small molecules affecting internalization of GPCRs |
en_US |
dc.type |
Article |
en_US |
dc.identifier.apacitation |
Kwon, Y., Lee, W., Genovesio, A., & Emans, N. (2012). A high-content subtractive screen for selecting small molecules affecting internalization of GPCRs. http://hdl.handle.net/10204/6498 |
en_ZA |
dc.identifier.chicagocitation |
Kwon, Y-J, W Lee, A Genovesio, and N Emans "A high-content subtractive screen for selecting small molecules affecting internalization of GPCRs." (2012) http://hdl.handle.net/10204/6498 |
en_ZA |
dc.identifier.vancouvercitation |
Kwon Y, Lee W, Genovesio A, Emans N. A high-content subtractive screen for selecting small molecules affecting internalization of GPCRs. 2012; http://hdl.handle.net/10204/6498. |
en_ZA |
dc.identifier.ris |
TY - Article
AU - Kwon, Y-J
AU - Lee, W
AU - Genovesio, A
AU - Emans, N
AB - G-protein–coupled receptors (GPCRs) are pivotal in cellular responses to the environment and are common drug targets. Identification of selective small molecules acting on single GPCRs is complicated by the shared machinery coupling signal transduction to physiology. Here, the authors demonstrate a high-content screen using a panel of GPCR assays to identify receptor selective molecules acting within the kinase/phosphatase inhibitor family. A collection of 88 kinase and phosphatase inhibitors was screened against seven agonist-induced GPCR internalization cell models as well as transferrin uptake in human embryonic kidney cells. Molecules acting on a single receptor were identified through excluding pan-specific compounds affecting housekeeping endocytosis or disrupting internalization of multiple receptors. They identified compounds acting on a sole GPCR from activities in a broad range of chemical structures that could not be easily sorted by conventional means. Selective analysis can therefore rapidly select compounds selectively affecting GPCR activity with specificity to one receptor class through high-content screening.
DA - 2012-03
DB - ResearchSpace
DP - CSIR
KW - High-content screening
KW - G-protein–coupled receptor
KW - Endocytosis
KW - Cell-based assay
KW - Image analysis
KW - Chemical biology
LK - https://researchspace.csir.co.za
PY - 2012
SM - 1087-0571
T1 - A high-content subtractive screen for selecting small molecules affecting internalization of GPCRs
TI - A high-content subtractive screen for selecting small molecules affecting internalization of GPCRs
UR - http://hdl.handle.net/10204/6498
ER -
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en_ZA |