From combinations to multitarget‐directed ligands: A continuum in Alzheimer's disease polypharmacology

C Albertini, A Salerno… - Medicinal Research …, 2021 - Wiley Online Library
The continued drug discovery failures in complex neurodegenerative diseases, including
Alzheimer's disease (AD), has raised questions about the classical paradigm “one‐drug …

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases

D Vanda, P Zajdel, M Soural - European Journal of Medicinal Chemistry, 2019 - Elsevier
This article provides an overview of compounds based on imidazo [1, 2-a] pyridine, imidazo
[1, 5-a] pyridine, imidazo [4, 5-b] pyridine and imidazo [4, 5-c] pyridine scaffolds, which act as …

Novel benzothiazole derivatives as multitargeted-directed ligands for the treatment of Alzheimer's disease

DE Hafez, M Dubiel, G La Spada, M Catto… - Journal of Enzyme …, 2023 - Taylor & Francis
Neurodegenerative diseases such as Alzheimer's disease (AD) are multifactorial with
several different pathologic mechanisms. Therefore, it is assumed that multitargeted-directed …

Multitarget‐Directed Ligands Combining Cholinesterase and Monoamine Oxidase Inhibition with Histamine H3R Antagonism for Neurodegenerative Diseases

ÓM Bautista‐Aguilera, S Hagenow… - Angewandte Chemie …, 2017 - Wiley Online Library
The therapy of complex neurodegenerative diseases requires the development of
multitarget‐directed drugs (MTDs). Novel indole derivatives with inhibitory activity towards …

Histamine H3 receptor antagonists/inverse agonists: Where do they go?

N Ghamari, O Zarei, JA Arias-Montaño, D Reiner… - Pharmacology & …, 2019 - Elsevier
Since the discovery of the histamine H 3 receptor in 1983, tremendous advances in the
pharmacological aspects of H 3 receptor antagonists/inverse agonists have been …

[HTML][HTML] Tracing the origins of IgE, mast cells, and allergies by studies of wild animals

LT Hellman, S Akula, M Thorpe, Z Fu - Frontiers in immunology, 2017 - frontiersin.org
In most industrialized countries, allergies have increased in frequency quite dramatically
during the past 50 years. Estimates show that 20–30% of the populations are affected …

G protein-coupled receptors in acquired epilepsy: Druggability and translatability

Y Yu, DT Nguyen, J Jiang - Progress in neurobiology, 2019 - Elsevier
As the largest family of membrane proteins in the human genome, G protein-coupled
receptors (GPCRs) constitute the targets of more than one-third of all modern medicinal …

Novel indanone derivatives as MAO B/H3R dual-targeting ligands for treatment of Parkinson's disease

A Affini, S Hagenow, A Zivkovic… - European journal of …, 2018 - Elsevier
The design of multi-targeting ligands was developed in the last decades as an innovative
therapeutic concept for Parkinson's disease (PD) and other neurodegenerative disorders. As …

Search for new multi-target compounds against Alzheimer's disease among histamine H3 receptor ligands

M Bajda, D Łażewska, J Godyń, P Zaręba… - European Journal of …, 2020 - Elsevier
Multi-target-directed ligands seem to be an interesting approach to the treatment of complex
disorders such as Alzheimer's disease. The aim of the present study was to find novel …

A Photoswitchable Agonist for the Histamine H3 Receptor, a Prototypic Family AG‐Protein‐Coupled Receptor

NJ Hauwert, TAM Mocking… - Angewandte …, 2019 - Wiley Online Library
Spatiotemporal control over biochemical signaling processes involving G protein‐coupled
receptors (GPCRs) is highly desired for dissecting their complex intracellular signaling. We …