Cargando…

Exploring the Effect of Cyclization of Histamine H(1) Receptor Antagonists on Ligand Binding Kinetics

[Image: see text] There is an increasing interest in guiding hit optimization by considering the target binding kinetics of ligands. However, compared to conventional structure–activity relationships, structure–kinetics relationships have not been as thoroughly explored, even for well-studied archet...

Descripción completa

Detalles Bibliográficos
Autores principales:	Wang, Zhiyong, Bosma, Reggie, Kuhne, Sebastiaan, van den Bor, Jelle, Garabitian, Wrej, Vischer, Henry F., Wijtmans, Maikel, Leurs, Rob, de Esch, Iwan J.P.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2021
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8154229/ https://www.ncbi.nlm.nih.gov/pubmed/34056427 http://dx.doi.org/10.1021/acsomega.0c06358

Ejemplares similares

Route to Prolonged Residence Time at the Histamine H(1) Receptor: Growing from Desloratadine to Rupatadine
por: Bosma, Reggie, et al.
Publicado: (2019)

Covalent Inhibition of the Histamine H(3) Receptor
por: Wágner, Gábor, et al.
Publicado: (2019)

Development of novel fluorescent histamine H(1)-receptor antagonists to study ligand-binding kinetics in living cells
por: Stoddart, Leigh A., et al.
Publicado: (2018)

A Photoswitchable Agonist for the Histamine H(3) Receptor, a Prototypic Family A G‐Protein‐Coupled Receptor
por: Hauwert, Niels J., et al.
Publicado: (2019)

BRET-Based Biosensors to Measure Agonist Efficacies in Histamine H(1) Receptor-Mediated G Protein Activation, Signaling and Interactions with GRKs and β-Arrestins
por: Verweij, Eléonore W. E., et al.
Publicado: (2022)

The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor
por: Bosma, Reggie, et al.
Publicado: (2017)

4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H(3) Receptor Agonists with in Vivo Central Nervous System Activity
por: Wágner, Gábor, et al.
Publicado: (2019)

PSW-Designer: An Open-Source Computational Platform for the Design and Virtual Screening of Photopharmacological Ligands
por: Simon, Icaro A., et al.
Publicado: (2023)

A toolbox of molecular photoswitches to modulate the CXCR3 chemokine receptor with light
por: Gómez-Santacana, Xavier, et al.
Publicado: (2019)

Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology
por: Hauwert, Niels J., et al.
Publicado: (2018)

Analysis of Missense Variants in the Human Histamine Receptor Family Reveals Increased Constitutive Activity of E410(6.30×30)K Variant in the Histamine H(1) Receptor
por: Ma, Xiaoyuan, et al.
Publicado: (2021)

Identification of TSPAN4 as Novel Histamine H(4) Receptor Interactor
por: Ma, Xiaoyuan, et al.
Publicado: (2021)

Optical control of the β(2)-adrenergic receptor with opto-prop-2: A cis-active azobenzene analog of propranolol
por: Bosma, Reggie, et al.
Publicado: (2022)

Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H(3) Receptor
por: Mocking, Tamara A. M., et al.
Publicado: (2019)

Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor
por: Bosma, Reggie, et al.
Publicado: (2019)

Development of a Conformational Histamine H(3) Receptor Biosensor for the Synchronous Screening of Agonists and Inverse Agonists
por: Schihada, Hannes, et al.
Publicado: (2020)

Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H(4) and the ion channel serotonin 5-HT(3A)
por: Verheij, Mark H.P., et al.
Publicado: (2011)

Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H(1) Receptor
por: Kok, Zhi Yuan, et al.
Publicado: (2022)

Function-specific virtual screening for GPCR ligands using a combined scoring method
por: Kooistra, Albert J., et al.
Publicado: (2016)

Metabolic profiling of ligands for the chemokine receptor CXCR3 by liquid chromatography-mass spectrometry coupled to bioaffinity assessment
por: Mladic, Marija, et al.
Publicado: (2015)

Differential Role of Serines and Threonines in Intracellular Loop 3 and C-Terminal Tail of the Histamine H(4) Receptor in β-Arrestin and G Protein-Coupled Receptor Kinase Interaction, Internalization, and Signaling
por: Verweij, Eléonore W. E., et al.
Publicado: (2020)

4-Hydroxypiperidines and Their Flexible 3-(Amino)propyloxy Analogues as Non-Imidazole Histamine H(3) Receptor Antagonist: Further Structure–Activity Relationship Exploration and In Vitro and In Vivo Pharmacological Evaluation
por: Olszewska, Beata, et al.
Publicado: (2018)

Histamine antagonists promote cancer immunosurveillance
por: Liu, Peng, et al.
Publicado: (2023)

Histamine and Skin Barrier: Are Histamine Antagonists Useful for the Prevention or Treatment of Atopic Dermatitis?
por: De Benedetto, Anna, et al.
Publicado: (2015)

Targeted LC–MS derivatization for aldehydes and carboxylic acids with a new derivatization agent 4-APEBA
por: Eggink, Mark, et al.
Publicado: (2010)

Short- and Long-Term Social Recognition Memory Are Differentially Modulated by Neuronal Histamine
por: Rani, Barbara, et al.
Publicado: (2021)

Growth of cultured human glioma tumour cells can be regulated with histamine and histamine antagonists.
por: Van der Ven, L. T., et al.
Publicado: (1993)

A NanoBRET-Based H(3)R Conformational Biosensor to Study Real-Time H(3) Receptor Pharmacology in Cell Membranes and Living Cells
por: Ma, Xiaoyuan, et al.
Publicado: (2022)

KLIFS: a structural kinase-ligand interaction database
por: Kooistra, Albert J., et al.
Publicado: (2016)

Effects of Olopatadine Hydrochloride, a Histamine H(1) Receptor Antagonist, on Histamine-Induced Skin Responses
por: Hashimoto, Takashi, et al.
Publicado: (2010)

In vitro effects of histamine receptor 1 antagonists on proliferation and histamine release in canine neoplastic mast cells
por: Gamperl, Susanne, et al.
Publicado: (2020)

Effects of histamine and various histamine receptor antagonists on gene expression profiles of macrophages during compressive strain
por: Schröder, Agnes, et al.
Publicado: (2021)

Fragment Screening Yields a Small‐Molecule Stabilizer of 14‐3‐3 Dimers That Modulates Client Protein Interactions
por: Brink, Hendrik J., et al.
Publicado: (2022)

Determinants of cyclization–decyclization kinetics of short DNA with sticky ends
por: Jeong, Jiyoun, et al.
Publicado: (2020)

Bromo-Cyclobutenaminones as New Covalent UDP-N-Acetylglucosamine Enolpyruvyl Transferase (MurA) Inhibitors
por: Hamilton, David J., et al.
Publicado: (2020)

Green Drug Discovery: Novel Fragment Space from the Biomass-Derived Molecule Dihydrolevoglucosenone (Cyrene(TM))
por: Dekker, Tom, et al.
Publicado: (2023)

Histamine H1 antagonists and clinical characteristics of febrile seizures
por: Zolaly, Mohammed A
Publicado: (2012)

Multiple Targeting Approaches on Histamine H(3) Receptor Antagonists
por: Khanfar, Mohammad A., et al.
Publicado: (2016)

Effects of Histamine Receptor Antagonist Cetirizine on Orthodontic Tooth Movement
por: Sperl, Gregor, et al.
Publicado: (2020)

Modulation of cellular signaling by herpesvirus-encoded G protein-coupled receptors
por: de Munnik, Sabrina M., et al.
Publicado: (2015)

Cannot write session to /tmp/vufind_sessions/sess_a7b4gaea5om5nir061di77v3p6