Cargando…

The future of EPAC-targeted therapies: agonism versus antagonism

Pharmaceutical manipulation of cAMP levels exerts beneficial effects through the regulation of the exchange protein activated by cAMP (EPAC) and protein kinase A (PKA) signalling routes. Recent attention has turned to the specific regulation of EPAC isoforms (EPAC1 and EPAC2) as a more targeted appr...

Descripción completa

Detalles Bibliográficos
Autores principales:	Parnell, Euan, Palmer, Timothy M., Yarwood, Stephen J.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Published By Elsevier In Association With The International Union Of Pharmacology 2015
Materias:	Review
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4392396/ https://www.ncbi.nlm.nih.gov/pubmed/25744542 http://dx.doi.org/10.1016/j.tips.2015.02.003

Ejemplares similares

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)

Targeting the GIPR for obesity: To agonize or antagonize? Potential mechanisms
por: Campbell, Jonathan E.
Publicado: (2020)

Selective small-molecule EPAC activators
por: Luchowska-Stańska, Urszula, et al.
Publicado: (2019)

Agonism and Antagonism at the Insulin Receptor
por: Knudsen, Louise, et al.
Publicado: (2012)

Identification of a Novel, Small Molecule Partial Agonist for the Cyclic AMP Sensor, EPAC1
por: Parnell, Euan, et al.
Publicado: (2017)

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)

Recent Advances in EPAC-Targeted Therapies: A Biophysical Perspective
por: Ahmed, Alveena, et al.
Publicado: (2019)

The role of c-Jun in controlling the EPAC1-dependent induction of the SOCS3 gene in HUVECs
por: Wiejak, Jolanta, et al.
Publicado: (2014)

Identification of A Novel Class of Benzofuran Oxoacetic Acid-Derived Ligands that Selectively Activate Cellular EPAC1
por: M. Beck, Elizabeth, et al.
Publicado: (2019)

Genomic agonism and phenotypic antagonism between estrogen and progesterone receptors in breast cancer
por: Singhal, Hari, et al.
Publicado: (2016)

Rapid-kinetics degron benchmarking reveals off-target activities and mixed agonism-antagonism of MYB inhibitors
por: Harada, Taku, et al.
Publicado: (2023)

Glucagon receptor antagonism impairs and glucagon receptor agonism enhances triglycerides metabolism in mice
por: Galsgaard, Katrine D., et al.
Publicado: (2022)

Epac and nociceptor sensitization
por: Huang, Li-Yen M, et al.
Publicado: (2017)

Protein interaction, cytotoxic, transcriptomic and proteomic responses to structurally distinct EPAC1 activators in HUVECs
por: Wiejak, Jolanta, et al.
Publicado: (2022)

Investigating the ligand agonism and antagonism at the D(2long) receptor by dynamic mass redistribution
por: Forster, Lisa, et al.
Publicado: (2022)

Multifunctional Enkephalin Analogs with a New Biological Profile: MOR/DOR Agonism and KOR Antagonism
por: Lee, Yeon Sun, et al.
Publicado: (2021)

Biased agonism
por: Kenakin, Terry
Publicado: (2009)

Isotype Switching Converts Anti-CD40 Antagonism to Agonism to Elicit Potent Antitumor Activity
por: Yu, Xiaojie, et al.
Publicado: (2020)

The Role of Epac in Cancer Progression
por: Wehbe, Nadine, et al.
Publicado: (2020)

Biased versus Partial Agonism in the Search for Safer Opioid Analgesics
por: Azevedo Neto, Joaquim, et al.
Publicado: (2020)

Optimized GIP analogs promote body weight lowering in mice through GIPR agonism not antagonism
por: Mroz, Piotr A., et al.
Publicado: (2018)

Design and Pharmacological Characterization of α(4)β(1) Integrin Cyclopeptide Agonists: Computational Investigation of Ligand Determinants for Agonism versus Antagonism
por: Anselmi, Michele, et al.
Publicado: (2023)

EPAC in Nice
Publicado: (1990)

EPAC impact
Publicado: (1994)

EPAC 2004
Publicado: (2004)

EPAC 2004
Publicado: (2004)

EPAC 2004
Publicado: (2004)

EPAC 2004
Publicado: (2004)

EPAC 2004
Publicado: (2004)

Predictive Modeling of Estrogen Receptor Agonism, Antagonism, and Binding Activities Using Machine and Deep Learning Approaches
por: Ciallella, Heather L., et al.
Publicado: (2020)

Identification and Characterization of an Affimer Affinity Reagent for the Detection of the cAMP Sensor, EPAC1
por: Buist, Hanna K., et al.
Publicado: (2021)

Structure-Guided Design of Selective Epac1 and Epac2 Agonists
por: Schwede, Frank, et al.
Publicado: (2015)

EPAC in Vascular Smooth Muscle Cells
por: Wehbe, Nadine, et al.
Publicado: (2020)

Opposing effects of chronic glucagon receptor agonism and antagonism on amino acids, hepatic gene expression, and alpha cells
por: Elmelund, Emilie, et al.
Publicado: (2022)

EPAC2: A new and promising protein for glioma pathogenesis and therapy
por: Richard, Seidu A.
Publicado: (2020)

Histamine 2 Receptor Agonism and Histamine 4 Receptor Antagonism Ameliorate Inflammation in a Model of Psoriasis
por: ROSSBACH, Kristine, et al.
Publicado: (2020)

Collective and Coordinated Conformational Changes Determine Agonism or Antagonism at the Human Trace Amine-Associated Receptor 1
por: Robles, Agustín I., et al.
Publicado: (2023)

Characterization of RNA driven structural changes in full length RIG-I leading to its agonism or antagonism
por: Sikorska, Justyna, et al.
Publicado: (2023)

Epac1 links prostaglandin E(2) to β-catenin-dependent transcription during epithelial-to-mesenchymal transition
por: Jansen, Sepp R., et al.
Publicado: (2016)

Cannot write session to /tmp/vufind_sessions/sess_51pvdogmg66taj3qbpg1e9ht17