Results 31 to 40 of about 3,259,253 (212)

FRET-based Microscopy Assay to Measure Activity of Membrane Amino Acid Transporters with Single-transporter Resolution

Bio-Protocol, 2021
Secondary active transporters reside in cell membranes transporting polar solutes like amino acids against steep concentration gradients, using electrochemical gradients of ions as energy sources.
Didar Ciftci, Gerard Huysmans, Xiaoyu Wang, Changhao He, Daniel Terry, Zhou Zhou, Gabriel Fitzgerald, Scott Blanchard, Olga Boudker   +8 more
doaj   +1 more source

Marine Natural Products Acting on the Acetylcholine-Binding Protein and Nicotinic Receptors: From Computer Modeling to Binding Studies and Electrophysiology

Marine Drugs, 2014
For a small library of natural products from marine sponges and ascidians, in silico docking to the Lymnaea stagnalis acetylcholine-binding protein (AChBP), a model for the ligand-binding domains of nicotinic acetylcholine receptors (nAChRs), was ...
Denis Kudryavtsev, Tatyana Makarieva, Natalia Utkina, Elena Santalova, Elena Kryukova, Christoph Methfessel, Victor Tsetlin, Valentin Stonik, Igor Kasheverov   +8 more
doaj   +1 more source

Application of the Gyrolab microfluidic platform to measure picomolar affinity of a PD-L1-binding Adnectin™ radioligand for positron emission tomography

BioTechniques, 2020
Advances in in vitro display and protein engineering yield therapeutics with affinities in the picomolar range. The Gyrolab® microfluidics platform uses the kinetic exclusion assay principle to measure subnanomolar solution affinities.
Zhou Dai, Juhi Juneja, Lumelle Schneeweis, Daniel Cohen, Frank Marsilio, Paul Morin, Ruchira DasGupta   +6 more
doaj   +1 more source

Validation of a [3H]Astemizole Binding Assay in HEK293 Cells Expressing HERG K+ Channels

Journal of Pharmacological Sciences, 2004
A radioligand binding assay for the HERG (human ether-a-go-go-related gene) K+ channel was developed to identify compounds which may have inhibitory activity and potential cardiotoxicity.
Peter J.S. Chiu, Karen F. Marcoe, Sidney E. Bounds, Chun-Hsiung Lin, Jin-Jye Feng, Atsui Lin, Fong-Chi Cheng, William J. Crumb, Richard Mitchell   +8 more
doaj   +1 more source

Design and validation of recombinant protein standards for quantitative Western blot analysis of cannabinoid CB1 receptor density in cell membranes: an alternative to radioligand binding methods

Microbial Cell Factories, 2022
Background Replacement of radioligand binding assays with antibody-antigen interaction-based approaches for quantitative analysis of G protein-coupled receptor (GPCR) levels requires the use of purified protein standards containing the antigen.
Miquel Saumell-Esnaola, Ainhoa Elejaga-Jimeno, Leyre Echeazarra, Leire Borrega-Román, Sergio Barrondo, Maider López de Jesús, Imanol González-Burguera, Alberto Gómez-Caballero, María Aranzazu Goicolea, Joan Sallés, Gontzal García del Caño   +10 more
doaj   +1 more source

Sodium Ions Affect GPR17 Conformational States and Functionality. [PDF]

Proteins
ABSTRACT Sodium is an allosteric modulator of several class‐A GPCR regulating active versus inactive conformation state and may be a critical issue for the optimization of crystallization procedures. Herein, the role of Na+ in the regulation of GPR17 conformational states was studied through MD simulations of GPR17 wild‐type and mutated on two ...
Palazzolo L, Daniele S, Bianchi D, Russo L, Capaldi S, Trincavelli ML, Eberini I.   +6 more
europepmc   +2 more sources

Functional Authentication of a Novel Gastropod Gonadotropin-Releasing Hormone Receptor Reveals Unusual Features and Evolutionary Insight. [PDF]

PLoS ONE, 2016
A gonadotropin-releasing hormone (GnRH)-like molecule was previously identified in a gastropod, Aplysia californica, and named ap-GnRH. In this study, we cloned the full-length cDNA of a putative ap-GnRH receptor (ap-GnRHR) and functionally authenticated
Scott I Kavanaugh, Pei-San Tsai
doaj   +1 more source

A Scintillation Proximity Assay for Real-Time Kinetic Analysis of Chemokine–Chemokine Receptor Interactions

Cells, 2022
Chemokine receptors are extensively involved in a broad range of physiological and pathological processes, making them attractive drug targets. However, despite considerable efforts, there are very few approved drugs targeting this class of seven ...
Stefanie Alexandra Eberle, Martin Gustavsson   +1 more
doaj   +1 more source

Characterization of muscarinic receptor binding by the novel radioligand, [3H]imidafenacin, in the bladder and other tissues of rats

Journal of Pharmacological Sciences, 2016
The present study aimed to directly characterize specific binding sites of tritium ([3H])-labeled imidafenacin, a new radioligand for labeling muscarinic receptors, in the bladder and other peripheral or central nervous tissues of rats.
Shiori Kuraoka, Yoshihiko Ito, Hirokazu Wakuda, Kazumasa Shinozuka, Satomi Onoue, Shizuo Yamada   +5 more
doaj   +1 more source

Summary of radioligand receptor binding assay components and reactions according to each receptor.

, 2015
Summary of radioligand receptor binding assay components and reactions according to each receptor.
Sek Peng Chin (737715), Lik Voon Kiew (534007), Lip Yong Chung (378399), Sri Devi Sukumaran (737716), Michael James Christopher Buckle (737717), Seetha Ramasamy (737714)   +5 more
core   +1 more source