Results 41 to 50 of about 3,259,253 (212)

Discovery of novel dual adenosine A1/A2A receptor antagonists using deep learning, pharmacophore modeling and molecular docking.

open access: yesPLoS Computational Biology, 2021
Adenosine receptors (ARs) have been demonstrated to be potential therapeutic targets against Parkinson's disease (PD). In the present study, we describe a multistage virtual screening approach that identifies dual adenosine A1 and A2A receptor ...
Mukuo Wang   +4 more
doaj   +1 more source

Optical Control of the Glucocorticoid Receptor Activity With a Photoswitchable Agonist

open access: yesAngewandte Chemie, EarlyView.
A photoswitchable glucocorticoid receptor agonist enables optical control of receptor activity, achieving picomolar potency and partial agonism that preferentially maintains anti‐inflammatory signaling over canonical transcriptional activation. ABSTRACT Glucocorticoids (GCs) are widely prescribed anti‐inflammatory agents whose clinical utility is ...
Zoe Sessions   +8 more
wiley   +2 more sources

DESIGN AND SYNTHESIS OF A PIPERAZINE DERIVATIVE AS A HIGH AFFINITY 5-HTIA RECEPTOR LIGAND

open access: yesZagazig Journal of Pharmaceutical Sciences, 1993
Serotonin (5-HT) 1A receptors have been shown to have physiological, biochemical pharmacological and clinical values. The piperazino derivative 1 was rationally designed as a bulky, lipophilic N4-substituted arylpiperazine. Radioligand binding assay of 1
Mohamed El-Bermawy
doaj   +1 more source

Oxytocin receptor binding sites in the periphery of the neonatal mouse. [PDF]

open access: yesPLoS ONE, 2017
Oxytocin (OXT) is a pleiotropic regulator of physiology and behavior. An emerging body of evidence demonstrates a role for OXT in the transition to postnatal life of the infant. To identify potential sites of OXT action via the OXT receptor (OXTR) in the
Maria A Greenwood, Elizabeth A D Hammock
doaj   +1 more source

Assay of CB1 Receptor Binding.

open access: yes, 2016
Type-1 cannabinoid receptor (CB1), one of the main targets of endocannabinoids, plays a key role in several pathophysiological conditions that affect both central nervous system and peripheral tissues.
CATANI, MV   +6 more
core   +2 more sources

Radioligand binding methods: practical guide and tips

open access: yes, 1993
Radioligand binding assays are a relatively simple but extremely powerful tool for studying receptors. They allow an analysis of the interactions of hormones, neurotransmitters, growth factors, and related drugs with the receptors, studies of receptor ...
D. B. Bylund, M. L. Toews
core   +1 more source

Diagnostic value of combined islet antigen‐reactive T cells and autoantibodies assays for type 1 diabetes mellitus

open access: yesJournal of Diabetes Investigation, 2021
Aims/Introduction Type 1 diabetes mellitus is a T cell‐mediated autoimmune disease. However, the determination of the autoimmune status of type 1 diabetes mellitus relies on islet autoantibodies (Abs), as T‐cell assay is not routinely carried out.
Wei Tang   +6 more
doaj   +1 more source

Quantification of the Surface Expression of G Protein-coupled Receptors Using Intact Live-cell Radioligand Binding Assays

open access: yesBio-Protocol, 2020
G protein-coupled receptors (GPCRs) are the most structurally diverse family of signaling proteins and regulate a variety of cell function. For most GPCRs, the cell surface is their functional destination where they are able to respond a wide range of ...
Xin Xu, Guangyu Wu
doaj   +1 more source

Stage‐Specific Patterns of Imaging and Non‐Motor Biomarkers in Spinocerebellar Ataxia Type 3

open access: yesAnnals of Clinical and Translational Neurology, EarlyView.
ABSTRACT Objective Advancements in disease‐modifying therapies for spinocerebellar ataxia Type 3 (SCA3) underscore the need for robust biomarkers to monitor disease progression and evaluate treatment efficacy. Although motor phenotypes have been well characterized, less is known about non‐motor and imaging‐based features across different disease stages.
Chun Li   +17 more
wiley   +1 more source

Dual‐Target Nectin‐4/FAP Heterobivalent Probe 68Ga/177Lu‐FZ‐NF‐1 for Triple‐Negative Breast Cancer: Preclinical Theranostic Evaluation and First‐in‐Human Translation

open access: yesAdvanced Science, EarlyView.
A novel hetero‐bivalent agent, 68Ga/177Lu‐FZ‐NF‐1, concurrently targets Nectin‐4 and FAP in triple‐negative breast cancer. It yields significant preclinical tumor regression and clinically identifies additional metastatic lesions missed by 18F‐FDG PET, demonstrating promising theranostic potential for personalized management.
Ye Li   +13 more
wiley   +1 more source

Home - About - Disclaimer - Privacy