Results 11 to 20 of about 834,721 (279)

Voltage-Dependent Dopamine Potency at D1-Like Dopamine Receptors

Frontiers in Pharmacology, 2020
In recent years, transmembrane voltage has been found to modify agonist potencies at several G protein-coupled receptors (GPCRs). Whereas the voltage sensitivities of the Gαi/o-coupled dopamine D2-like receptors (D2R, D3R, D4R) have previously been ...
Richard Ågren, Kristoffer Sahlholm, Kristoffer Sahlholm, Kristoffer Sahlholm   +3 more
doaj   +1 more source

Instrument-Free Protein Microarray Fabrication for Accurate Affinity Measurements

Biosensors, 2020
Protein microarrays have gained popularity as an attractive tool for various fields, including drug and biomarker development, and diagnostics. Thus, multiplexed binding affinity measurements in microarray format has become crucial.
Iris Celebi, Matthew T. Geib, Elisa Chiodi, Nese Lortlar Ünlü, Fulya Ekiz Kanik, Selim Ünlü   +5 more
doaj   +1 more source

Differential interaction of glimepiride and glibenclamide with the β-cell sulfonylurea receptor I. Binding characteristics [PDF]

, 1994
Glimepiride is a novel sulfonylurea drug for treatment of non-insulin-dependent diabetes mellitus with higher blood sugar lowering efficacy in diabetic patients than glibenclamide raising the question whether this characteristics is in line with ...
Aguilar-Bryan, Ashcroft, Ashcroft, Benovic, Bhathena, Boyd, Boyd, Boyd, Carpentier, Chick, French, Gaines, Geisen, Geisen, Gerich, Gylfe, Kaubisch, Kolterman, Kramer, Kramer, Müller, Nelson, Nelson, Niki, Niki, Niki, Niki, Panten, Popov, Praz, Schmid-Antomarchi, Schmid-Antomarchi, Sturgess, Sugiura, Weiland, Yalow   +35 more
core   +1 more source

Simultaneous Quantification of Protein Binding Kinetics in Whole Cells with Surface Plasmon Resonance Imaging and Edge Deformation Tracking

Membranes, 2020
Most drugs work by binding to receptors on the cell surface. Quantification of binding kinetics between drug and membrane protein is an essential step in drug discovery.
Wenwen Jing, Ashley Hunt, Nongjian Tao, Fenni Zhang, Shaopeng Wang   +4 more
doaj   +1 more source

Machine learning methods for developments of binding kinetic models in predicting protein‐ligand dissociation rate constants

Smart Molecules, 2023
Binding kinetic properties of protein–ligand complexes are crucial factors affecting the drug potency. Nevertheless, the current in silico techniques are insufficient in providing accurate and robust predictions for binding kinetic properties.
Yujing Zhao, Qilei Liu, Jian Du, Qingwei Meng, Lei Zhang   +4 more
doaj   +1 more source

A Single-Pass Type I Membrane Protein from the Apicomplexan Parasite Cryptosporidium parvum with Nanomolar Binding Affinity to Host Cell Surface

Microorganisms, 2021
Cryptosporidium parvum is a globally recognized zoonotic parasite of medical and veterinary importance. This parasite mainly infects intestinal epithelial cells and causes mild to severe watery diarrhea that could be deadly in patients with weakened or ...
Tianyu Zhang, Xin Gao, Dongqiang Wang, Jixue Zhao, Nan Zhang, Qiushi Li, Guan Zhu, Jigang Yin   +7 more
doaj   +1 more source

Understanding the Mechanism of Recognition of Gab2 by the N-SH2 Domain of SHP2

Life, 2020
Gab2 is a scaffold protein with a crucial role in colocalizing signaling proteins and it is involved in the regulation of several important molecular pathways.
Lorenzo Visconti, Francesca Malagrinò, Livia Pagano, Angelo Toto   +3 more
doaj   +1 more source

Ligation tunes protein reactivity in an ancient haemoglobin: kinetic evidence for an allosteric mechanism in Methanosarcina acetivorans protoglobin. [PDF]

PLoS ONE, 2012
Protoglobin from Methanosarcina acetivorans (MaPgb) is a dimeric globin with peculiar structural properties such as a completely buried haem and two orthogonal tunnels connecting the distal cavity to the solvent. CO binding to and dissociation from MaPgb
Stefania Abbruzzetti, Lesley Tilleman, Stefano Bruno, Cristiano Viappiani, Filip Desmet, Sabine Van Doorslaer, Massimo Coletta, Chiara Ciaccio, Paolo Ascenzi, Marco Nardini, Martino Bolognesi, Luc Moens, Sylvia Dewilde   +12 more
doaj   +1 more source

Low-affinity integrin states have faster ligand-binding kinetics than the high-affinity state

eLife, 2021
Integrin conformational ensembles contain two low-affinity states, bent-closed and extended-closed, and an active, high-affinity, extended-open state. It is widely thought that integrins must be activated before they bind ligand; however, one model holds
Jing Li, Jiabin Yan, Timothy A Springer
doaj   +1 more source

Kinetic mechanism of coupled binding in sodium-aspartate symporter GltPh

eLife, 2018
Many secondary active membrane transporters pump substrates against concentration gradients by coupling their uptake to symport of sodium ions. Symport requires the substrate and ions to be always transported together.
SeCheol Oh, Olga Boudker
doaj   +1 more source