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 …

The omnipresence of DYRK1A in human diseases

E Deboever, A Fistrovich, C Hulme… - International journal of …, 2022 - mdpi.com
The increasing population will challenge healthcare, particularly because the worldwide
population has never been older. Therapeutic solutions to age-related disease will be …

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 …

Function and inhibition of DYRK1A: emerging roles of treating multiple human diseases

Y Yang, X Fan, Y Liu, D Ye, C Liu, H Yang, Z Su… - Biochemical …, 2023 - Elsevier
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is an evolutionarily
conserved protein kinase and the most studied member of the Dual-specificity tyrosine …

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 …

[HTML][HTML] Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity

OM Al-Saad, M Gabr, SS Darwish, M Rullo… - European Journal of …, 2024 - Elsevier
In neurodegenerative diseases, using a single molecule that can exert multiple effects to
modify the disease may have superior activity over the classical “one molecule-one target” …

Ligand-based discovery of a small molecule as inhibitor of α-synuclein amyloid formation

L De Luca, S Vittorio, S Peña-Díaz, G Pitasi… - International journal of …, 2022 - mdpi.com
α-Synuclein (α-Syn) aggregates are implicated in Parkinson's disease (PD), so inhibitors of
α-Syn aggregation have been intensively explored. It has been demonstrated that small …

Dual targeting of inflammation and β-cell dysfunction for therapy of diabetes mellitus

F Mustafa, M Abdel-Halim, R Abdel-Moniem… - Journal of Drug Delivery …, 2024 - Elsevier
Diabetes Mellitus (DM) is a chronic metabolic disorder characterized by β-cell loss and
inflammation. From a therapeutic standpoint, it would be necessary to halt the uncontrolled …

Polydentate N,O-Ligands Possessing Unsymmetrical Urea Fragments Attached to a p-Cresol Scaffold

SE Todorova, RI Rusew, BL Shivachev, VB Kurteva - Molecules, 2023 - mdpi.com
In this study, three series of polydentate N, O-ligands possessing unsymmetrical urea
fragments attached to ap-cresol scaffold are obtained, namely mono-and bi-substituted open …

A Unique Perspective on Lead Compounds for Dementia with the Lewy Body

M Subramani, A Sivaperuman, R Natarajan… - Medicinal …, 2023 - ingentaconnect.com
Dementia with Lewy Bodies is a neurodegenerative disorder characterised by abnormal α-
synuclein aggregate accumulation in Lewy Bodies and Lewy Neurites and the most …