Results 81 to 90 of about 3,259,253 (212)

Correlation between the data obtained from platypus Mel1c and those obtained with clawed frog Mel1c.

, 2018
Data were obtained in a binding assay with 2-[125I]-iodomelatonin as the radioligand. See Fig 5.
Céline Legros (588091), Valerie Simonneaux (4952047), Isabelle Riest-Fery (4952035), Célia Gautier (4952038), Olivier Nosjean (414204), Frank Grützner (42240), Jean A. Boutin (229503), Sophie-Penelope Guenin (4952044), Tahlia Jade Perry (4952041)   +8 more
core   +1 more source

Analyzing Radioligand Binding Data [PDF]

, 2000
A radioligand is a radioactively labeled drug that can associate with a receptor, transporter, enzyme, or any protein of interest. Measuring the rate and extent of binding provides information on the number of binding sites, and their affinity and ...
Neubig, Richard, Richard Neubig, Harvey Motulsky, Motulsky, Harvey   +3 more
core   +1 more source

Prostate Cancer Patient‐Derived Organoids (PDOs) as Functional Avatars for Antisense Oligonucleotide (ASO)‐Based Personalized Therapy

Advanced Healthcare Materials, Volume 15, Issue 41, 6 November 2026.
Prostate patient‐derived organoids (PDOs) were established from TURP and biopsy specimens with >90% success and retain key features of their tissues of origin, making them functional avatars for antisense oligonucleotide (ASO) therapy . Transfecting single cells outside the Matrigel matrix and then reconstituting organoids overcomes the 3D delivery ...
Thi Thom Tran, Thi Tu Uyen Phan, Michael Baboudjian, Quang Hieu Duong, Ines Sousa, Thi Thuy Le, Virginie Baylot, Sophie Giusiano, Laurent Daniel, Pauline Brige, Benjamin Guillet, Cyrille Bastide, Carmen Garrido, David Taïeb, Thi Khanh Le, Palma Rocchi   +15 more
wiley   +1 more source

Do Brain Extracellular Fluid Concentrations Predict PET‐Inferred Receptor Occupancy in Human CNS? A Mechanistic Model‐Based Analysis of Dopamine D2 Receptor Ligands

Clinical Pharmacology &Therapeutics, Volume 120, Issue 5, Page 1389-1401, November 2026.
A mechanistic CNS PBPK model framework was applied to eight antipsychotic D2 receptor ligands, comparing brain extracellular fluid (brainECF) and brain cell membrane (brainM) as biophase for predicting human receptor occupancy compared against PET neuroimaging data. BrainM concentrations showed improved agreement with PET‐derived receptor occupancy for
Divakar Budda, J.G. Coen van Hasselt, Elizabeth C.M. de Lange   +2 more
wiley   +1 more source

Impact of correlated PBPK parameters on intra‐patient global sensitivity analysis in molecular radiotherapy

Medical Physics, Volume 53, Issue 11, November 2026.
Abstract Background Physiologically based pharmacokinetic (PBPK) models integrated into digital twins provide a robust framework for optimizing individualized molecular radiotherapy (MRT). Nevertheless, uncertainties in PBPK‐model‐derived dosimetry can compromise the reliability of dosimetry‐guided treatment planning and individualized therapy ...
Elham Yousefzadeh‐Nowshahr, Deni Hardiansyah, Valentina Vasic, Anna‐Lena Theisen, Johannes Tran‐Gia, Philipp E. Hartrampf, Ambros J. Beer, Michael Lassmann, Gerhard Glatting   +8 more
wiley   +1 more source

Receptor kinetics: Binding flux‐based approaches offer complementary insight into how ligand binding evolves with time

British Journal of Pharmacology, Volume 183, Issue 21, Page 6444-6457, November 2026.
Background and Purpose Binding kinetics are essentially based on rate constants. Yet, this view has been challenged by the idea that ‘binding fluxes’ are dynamic and therefore more relevant. Those fluxes refer to the rate at which a target/receptor changes from one state into another through ligand/drug binding or a conformational change.
Georges Vauquelin, Terry Kenakin, Dominique Maes   +2 more
wiley   +1 more source

Development and validation of a mass spectrometry binding assay for mGlu5 receptor

, 2020
International audienceMass spectrometry (MS) binding assays are a label-free alternative to radioligand or fluorescence binding assays, so the readout is based on direct mass spectrometric detection of the test ligand.
Serra, Carmen, Goudet, Cyril, Muñoz, Lourdes, Catena, Juanlo, Catena, Juan Lorenzo, Berizzi, Alice, Malhaire, Fanny, Llebaria, Amadeu, Berizzi, Alice E., Ricart-Ortega, Maria, Lebon, Guillaume   +10 more
core   +1 more source

Synthesis and initial in vitro characterization of a new P2X7R radioligand [18F]IUR-1602 [PDF]

, 2019
The overexpression of P2X7R is associated with neuroinflammation and plays an important role in various neurodegenerative diseases. The [18F]fluoropropyl derivative of GSK1482160, [18F]IUR-1602, has been first prepared and examined as a new potential ...
Hutchins, Gary D., Peters, Jonathan S., Zheng, Qi-Huang, Glick-Wilson, Barbara E., Green, Mark A., Zarrinmayeh, Hamideh, Gao, Mingzhang, Wang, Min, Territo, Paul R., Meyer, Jill A.   +9 more
core   +1 more source

Structure-Based Identification of Potent Natural Product Chemotypes as Cannabinoid Receptor 1 Inverse Agonists

Molecules, 2018
Natural products are an abundant source of potential drugs, and their diversity makes them a rich and viable prospective source of bioactive cannabinoid ligands.
Pankaj Pandey, Kuldeep K. Roy, Haining Liu, Guoyi Ma, Sara Pettaway, Walid F. Alsharif, Rama S. Gadepalli, John M. Rimoldi, Christopher R. McCurdy, Stephen J. Cutler, Robert J. Doerksen   +10 more
doaj   +1 more source

Parkinson's disease under dopamine replacement therapy as a human framework for studying addiction‐relevant mechanisms

Psychiatry and Clinical Neurosciences, Volume 80, Issue 11, Page 877-888, November 2026.
Addiction is a chronic relapsing condition characterized by compulsive reward seeking and impaired behavioral control, associated with major individual and societal burden. Mechanistic investigation in humans remains constrained by ethical limitations, uncontrolled exposure histories, and ecological confounds.
Vanessa Fleury, Elvira Pirondini, Damien Benis, Tiffany Corbet, Gabriel Thorens, Christian Lüscher, Paul Krack   +6 more
wiley   +1 more source