The metabolic role of GRK2 in insulin resistance and associated conditions

D Sorriento, MR Rusciano, V Visco, A Fiordelisi… - Cells, 2021 - mdpi.com
Insulin resistance (IRES) is a pathophysiological condition characterized by the reduced
response to insulin of several tissues, including myocardial and skeletal muscle. IRES is …

G-protein-coupled receptor kinase 2 (GRK2) inhibitors: current trends and future perspectives

M Guccione, R Ettari, S Taliani… - Journal of medicinal …, 2016 - ACS Publications
G-protein-coupled receptor kinase 2 (GRK2) is a G-protein-coupled receptor kinase that is
ubiquitously expressed in many tissues and regulates various intracellular mechanisms. The …

Pharmacological inhibition of GRK2 improves cardiac metabolism and function in experimental heart failure

M Ciccarelli, D Sorriento, A Fiordelisi… - ESC Heart …, 2020 - Wiley Online Library
Aims The effects of GRK2 inhibition on myocardial metabolism in heart failure (HF) are
unchartered. In this work, we evaluated the impact of pharmacological inhibition of GRK2 by …

Antidiabetic and Cardioprotective Effects of Pharmacological Inhibition of GRK2 in db/db Mice

E Cipolletta, J Gambardella, A Fiordelisi… - International journal of …, 2019 - mdpi.com
Despite the availability of several therapies for the management of blood glucose in diabetic
patients, most of the treatments do not show benefits on diabetic cardiomyopathy, while …

“Freeze, don't move”: how to arrest a suspect in heart failure–a review on available GRK2 inhibitors

D Sorriento, M Ciccarelli, E Cipolletta… - Frontiers in …, 2016 - frontiersin.org
Cardiovascular disease and heart failure (HF) still collect the largest toll of death in western
societies and all over the world. A growing number of molecular mechanisms represent …

Development of inflammatory immune response-related drugs based on G protein-coupled receptor kinase 2

C Han, Y Li, Y Wang, D Cui, T Luo, Y Zhang… - Cellular Physiology and …, 2018 - karger.com
G protein-coupled receptor kinase 2 (GRK2), as a vital Ser/Thr kinase, is an important
regulatory protein in the inflammatory immune response (IIR) by maintaining the balance …

[HTML][HTML] Dual role of GRK5 in cancer development and progression

J Gambardella, A Franco, C Del Giudice… - Translational …, 2016 - ncbi.nlm.nih.gov
GRK5 is a multifunctional protein that is able to move within the cell in response to various
stimuli to regulate key intracellular signaling from receptor activation, on plasmamembrane …

Antiplasmodial activity study of angiotensin II via Ala scan analogs

AF Silva, EL Bastos, MDT Torres… - Journal of Peptide …, 2014 - Wiley Online Library
Angiotensin II (AII) as well as analog peptides shows antimalarial activity against
Plasmodium gallinaceum and Plasmodium falciparum, but the exact mechanism of action is …

Design, synthesis and efficacy of novel G protein-coupled receptor kinase 2 inhibitors

A Carotenuto, E Cipolletta, I Gomez-Monterrey… - European journal of …, 2013 - Elsevier
G protein-coupled receptor kinase 2 (GRK2) is a relevant signaling node of the cellular
transduction network, playing major roles in the physiology of various organs/tissues …

On the design of tailored liposomes for KRX29 peptide delivery

S Bochicchio, M Sala, A Spensiero, MC Scala… - New Journal of …, 2017 - pubs.rsc.org
The high interest in therapeutic peptides, due to the specificity of their mechanisms of action,
has stimulated the research of new delivery strategies to overcome bioavailability problems …