DYRK1A inhibitors for disease therapy: Current status and perspectives

T Liu, Y Wang, J Wang, C Ren, H Chen… - European journal of …, 2022 - Elsevier
Dual-specificity tyrosine phosphorylation-regulated kinase 1 A (DYRK1A) is a conserved
protein kinase that plays essential roles in various biological processes. It is located in the …

A review on synthetic inhibitors of dual-specific tyrosine phosphorylation-regulated kinase 1A (DYRK1A) for the treatment of Alzheimer's disease (AD)

P Gehlot, R Pathak, S Kumar, NK Choudhary… - Bioorganic & Medicinal …, 2024 - Elsevier
Alzheimer's disease (AD) is a complex disorder that is influenced by a number of variables,
such as age, gender, environmental factors, disease, lifestyle, infections, and many more …

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 …

EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model

JM Delabar, MAGB Gomes, M Fructuoso… - European Journal of …, 2024 - Elsevier
Overexpression of the chromosome 21 DYRK1A gene induces morphological defects and
cognitive impairments in individuals with Down syndrome (DS) and in DS mice models …

Discovery of novel 6-hydroxybenzothiazole urea derivatives as dual Dyrk1A/α-synuclein aggregation inhibitors with neuroprotective effects

YT AlNajjar, M Gabr, AK ElHady, M Salah… - European journal of …, 2022 - Elsevier
A role of Dyrk1A in the progression of Down syndrome–related Alzheimer's disease (AD) is
well supported. However, the involvement of Dyrk1A in the pathogenesis of Parkinson's …

Regiodivergent Synthesis of Brominated Pyridylthiophenes by Overriding the Inherent Substrate Bias

M Hosoya, A Mori, K Okano - Synlett, 2024 - thieme-connect.com
A regiocontrolled functionalization of a pyridylthiophene scaffold was accomplished.
Regioselectivity for deprotonation of the pyridylthiophene was switched by changing the …

From Dyrk1A inhibitors to a novel class of antiviral agents: Targeting Enterovirus EV-A71 with 2-aryl-substituted thiophene scaffolds

PM Keddis, TKM Tu, H Scherer, AM Kany… - European Journal of …, 2025 - Elsevier
Abstract Enterovirus A71 (EV-A71) is a major causative agent of hand, foot, and mouth
disease (HFMD) especially in children. The majority of EV-A71 cases are mild, however …

Discovery of novel 5-methoxybenzothiophene hydrazides as metabolically stable Clk1 inhibitors with high potency and unprecedented Clk1 isoenzyme selectivity

DS El-Gamil, AK ElHady, PJ Chen, TL Hwang… - European Journal of …, 2023 - Elsevier
Clk1 kinase is a key modulator of the pre-mRNA alternative splicing machinery which has
been proposed as a promising target for treatment of various tumour types, Duchenne's …

Development of novel amide–derivatized 2, 4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide …

SS Darwish, M Abdel-Halim, AK ElHady… - European Journal of …, 2018 - Elsevier
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (Dyrk1A) is a potential target
in Alzheimer's disease (AD) because of the established correlation between its over …

Development of novel conformationally restricted selective Clk1/4 inhibitors through creating an intramolecular hydrogen bond involving an imide linker

DS El-Gamil, AK ElHady, PJ Chen, TL Hwang… - European Journal of …, 2022 - Elsevier
As prime regulators of pre-mRNA alternative splicing, different Clk isoforms were found to be
overexpressed in various tumour types and have received much attention recently as …