Intracellular cAMP sensor EPAC: physiology, pathophysiology, and therapeutics development

WG Robichaux III, X Cheng - Physiological reviews, 2018 - journals.physiology.org
This review focuses on one family of the known cAMP receptors, the exchange proteins
directly activated by cAMP (EPACs), also known as the cAMP-regulated guanine nucleotide …

Paving the Rho in cancer metastasis: Rho GTPases and beyond

S Jansen, R Gosens, T Wieland, M Schmidt - Pharmacology & therapeutics, 2018 - Elsevier
Malignant carcinomas are often characterized by metastasis, the movement of carcinoma
cells from a primary site to colonize distant organs. For metastasis to occur, carcinoma cells …

Cyclic AMP sensor EPAC proteins and their role in cardiovascular function and disease

F Lezoualc'h, L Fazal, M Laudette, C Conte - Circulation research, 2016 - Am Heart Assoc
cAMP is a universal second messenger that plays central roles in cardiovascular regulation
influencing gene expression, cell morphology, and function. A crucial step toward a better …

Targeting the small GTPase superfamily through their regulatory proteins

JL Gray, F von Delft, PE Brennan - … Chemie International Edition, 2020 - Wiley Online Library
The Ras superfamily of small GTPases are guanine‐nucleotide‐dependent switches
essential for numerous cellular processes. Mutations or dysregulation of these proteins are …

Membranes prime the RapGEF EPAC1 to transduce cAMP signaling

C Sartre, F Peurois, M Ley, MH Kryszke… - Nature …, 2023 - nature.com
EPAC1, a cAMP-activated GEF for Rap GTPases, is a major transducer of cAMP signaling
and a therapeutic target in cardiac diseases. The recent discovery that cAMP is …

Multifunctional mitochondrial Epac1 controls myocardial cell death

L Fazal, M Laudette, S Paula-Gomes, S Pons… - Circulation …, 2017 - Am Heart Assoc
Rationale: Although the second messenger cyclic AMP (cAMP) is physiologically beneficial
in the heart, it largely contributes to cardiac disease progression when dysregulated. Current …

Epac-inhibitors: facts and artefacts

H Rehmann - Scientific reports, 2013 - nature.com
Abstract cAMP is a universal second messenger. Its signalling is mediated by protein kinase
A, Epac and certain types of ion channels in mammalians. cAMP signalling is involved in …

Advances in NMR methods to map allosteric sites: from models to translation

S Boulton, G Melacini - Chemical Reviews, 2016 - ACS Publications
The last five years have witnessed major developments in the understanding of the allosteric
phenomenon, broadly defined as coupling between remote molecular sites. Such advances …

The future of EPAC-targeted therapies: agonism versus antagonism

E Parnell, TM Palmer, SJ Yarwood - Trends in pharmacological sciences, 2015 - cell.com
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 …

Cyclic AMP sensor EPAC proteins and energy homeostasis

M Almahariq, FC Mei, X Cheng - Trends in Endocrinology & Metabolism, 2014 - cell.com
The pleiotropic second-messenger cAMP plays a crucial role in mediating the effects of
various hormones on metabolism. The major intracellular functions of cAMP are transduced …