Functional consequences of spatial, temporal and ligand bias of G protein-coupled receptors

AD Tóth, G Turu, L Hunyady - Nature Reviews Nephrology, 2024 - nature.com
G protein-coupled receptors (GPCRs) regulate every aspect of kidney function by mediating
the effects of various endogenous and exogenous substances. A key concept in GPCR …

The translational value of ligand‐receptor binding kinetics in drug discovery

H Liu, H Zhang, AP IJzerman… - British Journal of …, 2024 - Wiley Online Library
The translation of in vitro potency of a candidate drug, as determined by traditional
pharmacology metrics (such as EC50/IC50 and KD/Ki values), to in vivo efficacy and safety …

G protein–coupled receptor endocytosis generates spatiotemporal bias in β-arrestin signaling

AD Tóth, B Szalai, OT Kovács, D Garger, S Prokop… - Science …, 2024 - science.org
The stabilization of different active conformations of G protein–coupled receptors is thought
to underlie the varying efficacies of biased and balanced agonists. Here, profiling the …

Existence of quantum pharmacology in Sartans: evidence in isolated rabbit iliac arteries

LK Gadanec, J Swiderski, V Apostolopoulos… - International Journal of …, 2023 - mdpi.com
Quantum pharmacology introduces theoretical models to describe the possibility of ultra-
high dilutions to produce biological effects, which may help to explain the placebo effect …

From inflammation to metastasis: The central role of miR-155 in modulating NF-κB in cancer

S Mohan, MA Hakami, HG Dailah, A Khalid… - … -Research and Practice, 2024 - Elsevier
Cancer is a multifaceted, complex disease characterized by unchecked cell growth, genetic
mutations, and dysregulated signalling pathways. These factors eventually cause evasion of …

[HTML][HTML] Direct Vascular Effects of Angiotensin II (A Systematic Short Review)

GL Nádasy, A Balla, G Dörnyei, L Hunyady… - International Journal of …, 2024 - mdpi.com
The octapeptide angiotensin II (Ang II) is a circulating hormone as well as a locally formed
agonist synthesized by the angiotensin-converting enzyme (ACE) of endothelial cells. It …

Receptor endocytosis orchestrates the spatiotemporal bias of β-arrestin signaling

AD Tóth, B Szalai, OT Kovács, D Garger, S Prokop… - bioRxiv, 2023 - biorxiv.org
The varying efficacy of biased and balanced agonists is generally explained by the
stabilization of different active receptor conformations. In this study, systematic profiling of …

Drugs associated with tachyphylaxis: results from a retrospective pharmacovigilance study using disproportionality analysis

K Sridharan - European Journal of Hospital Pharmacy, 2025 - ejhp.bmj.com
Background Tachyphylaxis is the rapid development of drug tolerance following repeated
administration. Objectives To evaluate the United States Food and Drug Administration …

Estudo das relações funcionais entre proteínas O-gluconaciladas ea sinalização do receptor de angiotensina II do tipo 1

JA Silva Neto - 2023 - teses.usp.br
Os receptores de sete domínios de membrana (GPCR) são proteínas que, ao serem
ativadas por hormônios, neurotransmissores ou fármacos, disparam vias de sinalização …