Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay

Cyclic GMP-AMP synthase (cGAS) initiates the innate immune system in response to cytosolic dsDNA. After binding and activation from dsDNA, cGAS uses ATP and GTP to synthesize 2′, 3′ -cGAMP (cGAMP), a cyclic dinucleotide second messenger with mixed 2′-5′ and 3′-5′ phosphodiester bonds. Inappropriate...

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Publicado en:PLoS One
Main Authors: Hall, Justin, Brault, Amy, Vincent, Fabien, Weng, Shawn, Wang, Hong, Dumlao, Darren, Aulabaugh, Ann, Aivazian, Dikran, Castro, Dana, Chen, Ming, Culp, Jeffrey, Dower, Ken, Gardner, Joseph, Hawrylik, Steven, Golenbock, Douglas, Hepworth, David, Horn, Mark, Jones, Lyn, Jones, Peter, Latz, Eicke, Li, Jing, Lin, Lih-Ling, Lin, Wen, Lin, David, Lovering, Frank, Niljanskul, Nootaree, Nistler, Ryan, Pierce, Betsy, Plotnikova, Olga, Schmitt, Daniel, Shanker, Suman, Smith, James, Snyder, William, Subashi, Timothy, Trujillo, John, Tyminski, Edyta, Wang, Guoxing, Wong, Jimson, Lefker, Bruce, Dakin, Leslie, Leach, Karen
Formato: Artigo
Idioma:Inglês
Publicado: Public Library of Science 2017
Assuntos:
Research Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC5608272/
https://ncbi.nlm.nih.gov/pubmed/28934246
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1371/journal.pone.0184843
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