Cargando…
Identification of a Novel, Small Molecule Partial Agonist for the Cyclic AMP Sensor, EPAC1
Screening of a carefully selected library of 5,195 small molecules identified 34 hit compounds that interact with the regulatory cyclic nucleotide-binding domain (CNB) of the cAMP sensor, EPAC1. Two of these hits (I942 and I178) were selected for their robust and reproducible inhibitory effects with...
Autores principales: | Parnell, Euan, McElroy, Stuart P., Wiejak, Jolanta, Baillie, Gemma L., Porter, Alison, Adams, David R., Rehmann, Holger, Smith, Brian O., Yarwood, Stephen J. |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group UK
2017
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5428521/ https://www.ncbi.nlm.nih.gov/pubmed/28331191 http://dx.doi.org/10.1038/s41598-017-00455-7 |
Ejemplares similares
-
Phosphorylation of ezrin on Thr567 is required for the synergistic activation of cell spreading by EPAC1 and protein kinase A in HEK293T cells
por: Parnell, Euan, et al.
Publicado: (2015) -
The novel exchange protein activated by cyclic AMP 1 (EPAC1) agonist, I942, regulates inflammatory gene expression in human umbilical vascular endothelial cells (HUVECs)
por: Wiejak, Jolanta, et al.
Publicado: (2019) -
Identification of A Novel Class of Benzofuran Oxoacetic Acid-Derived Ligands that Selectively Activate Cellular EPAC1
por: M. Beck, Elizabeth, et al.
Publicado: (2019) -
The cAMP sensors, EPAC1 and EPAC2, display distinct subcellular distributions despite sharing a common nuclear pore localisation signal
por: Parnell, Euan, et al.
Publicado: (2015) -
The Potential of a Novel Class of EPAC-Selective Agonists to Combat Cardiovascular Inflammation
por: Barker, Graeme, et al.
Publicado: (2017)