Adequate NADK/NADK2 level is essential to the proper functioning of redox and folate cycles and the purine biosynthesis pathway, and as well as maintenance of GSIS response. During aging, diminished NADK/NADK2 expression alters the metabolic status quo, increasing AICAR production. The latter activates AMPK and suppresses GSIS.
Guan‐Jie Li+6 more
wiley +1 more source
Adenosine stimulates the basolateral 50 pS K+ channel in renal proximal tubule via adenosine-A1 receptor. [PDF]
Liu H+5 more
europepmc +1 more source
A Xanthine Derivative With Novel Heat Shock Protein 90‐Alpha Inhibitory and Senolytic Properties
This study aimed to find safe senolytic drugs that selectively eliminate senescent cells. Focusing on HSP90 inhibitors, we employed a virtual screening to identify novel, safer compounds (A). K5, a xanthinic candidate, effectively eliminated senescent cells in various cellular models (B), extended lifespan in flies, and reduced aging signs in mice (C).
Sandra Atlante+24 more
wiley +1 more source
Investigation of adenosine A1 receptor-mediated β-arrestin 2 recruitment using a split-luciferase assay. [PDF]
Saecker L, Häberlein H, Franken S.
europepmc +1 more source
ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison+15 more
wiley +1 more source
Small molecule allosteric modulation of the adenosine A1 receptor. [PDF]
Nguyen ATN+5 more
europepmc +1 more source
Progress on the development of Class A GPCR‐biased ligands
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales+20 more
wiley +1 more source
Ex Vivo Feedback Control of Neurotransmission Using a Photocaged Adenosine A1 Receptor Agonist. [PDF]
Craey E+14 more
europepmc +1 more source
G protein‐coupled receptors (GPCRs) play a crucial role in cell function by transducing signals from the extracellular environment to the inside of the cell. They mediate the effects of various stimuli, including hormones, neurotransmitters, ions, photons, food tastants and odorants, and are renowned drug targets.
Małgorzata M. Kogut‐Günthel+11 more
wiley +1 more source
Cancer-Related Somatic Mutations in Transmembrane Helices Alter Adenosine A1 Receptor Pharmacology. [PDF]
Wang X+6 more
europepmc +1 more source