[HTML][HTML] Protective effects of caffeine against palmitate-induced lipid toxicity in primary rat hepatocytes is associated with modulation of adenosine receptor A1 …

JC Arroyave-Ospina, M Buist-Homan, M Schmidt… - Biomedicine & …, 2023 - Elsevier
Background Epidemiological evidence has shown an association between coffee
consumption and reduced risk for chronic liver diseases, including metabolic-dysfunction …

[HTML][HTML] Class A and C GPCR dimers in neurodegenerative diseases

AB Caniceiro, B Bueschbell, AC Schiedel… - Current …, 2022 - ncbi.nlm.nih.gov
Neurodegenerative diseases affect over 30 million people worldwide with an ascending
trend. Most individuals suffering from these irreversible brain damages belong to the elderly …

Single Stabilizing Point Mutation Enables High‐Resolution Co‐Crystal Structures of the Adenosine A2A Receptor with Preladenant Conjugates

T Claff, TA Klapschinski… - Angewandte Chemie …, 2022 - Wiley Online Library
The G protein‐coupled adenosine A2A receptor (A2AAR) is an important new (potential)
drug target in immuno‐oncology, and for neurodegenerative diseases. Preladenant and its …

A Chemical Biological Approach to Study G Protein-Coupled Receptors: Labeling the Adenosine A1 Receptor Using an Electrophilic Covalent Probe

BLH Beerkens, C Koc, R Liu, BI Florea… - ACS Chemical …, 2022 - ACS Publications
G protein-coupled receptors (GPCRs) have been known for decades as attractive drug
targets. This has led to the development and approval of many ligands targeting GPCRs …

Selective A3 Adenosine Receptor Antagonist Radioligand for Human and Rodent Species

RR Suresh, ZG Gao, V Salmaso, E Chen… - ACS Medicinal …, 2022 - ACS Publications
The A3 adenosine receptor (A3AR) is a target for pain, ischemia, and inflammatory disease
therapy. Among the ligand tools available are selective agonists and antagonists, including …

Thymosin beta 4: A potential novel adjunct treatment for bacterial keratitis

G Sosne, EA Berger - International immunopharmacology, 2023 - Elsevier
Microbial keratitis is a rapidly progressing, visually debilitating infection of the cornea that
can lead to corneal scarring, endophthalmitis, and perforation. Corneal opacification or …

Adenosine Receptor Ligands, Probes, and Functional Conjugates: A 20-Year History of Pyrazolo[4,3-e][1,2,4]Triazolo[1,5-c]Pyrimidines (PTP)

F Prencipe, T Da Ros, E Cescon, I Grieco… - … Receptors and their …, 2023 - Springer
Adenosine receptors are G protein-coupled receptors (GPCRs) involved in several
processes in the human body. Their involvement in pathologies like coronary vasodilation …

Development of subtype-selective covalent ligands for the adenosine A 2B receptor by tuning the reactive group

BLH Beerkens, X Wang, M Avgeropoulou… - RSC Medicinal …, 2022 - pubs.rsc.org
Signalling through the adenosine receptors (ARs), in particular through the adenosine A2B
receptor (A2BAR), has been shown to play a role in a variety of pathological conditions …

Development of Putative Bivalent Dicovalent Ligands for the Adenosine A1 Receptor

CM Payne, JA Baltos, M Langiu, C Sinh Lu… - …, 2024 - Wiley Online Library
Accumulating evidence suggests that G protein‐coupled receptors (GPCRs) can exist and
function in homodimer and heterodimer forms. The adenosine A1 receptor (A1R) has been …

Once Upon a Time Adenosine and Its Receptors: Historical Survey and Perspectives as Potential Targets for Therapy in Human Diseases

D Catarzi, F Varano, S Calenda, E Vigiani… - Purinergic Receptors and …, 2023 - Springer
Endogenous autacoid adenosine plays important physiological roles in various tissues and
organs by acting through A1, A2A, A2B, and A3 receptors. Dysregulated extracellular …