An overview of cdc2‐like kinase 1 (Clk1) inhibitors and their therapeutic indications
Over the past decade, Clk1 has been identified as a promising target for the treatment of
various diseases, in which deregulated alternative splicing plays a role. First small …
various diseases, in which deregulated alternative splicing plays a role. First small …
Comparative efficacy and selectivity of pharmacological inhibitors of DYRK and CLK protein kinases
MF Lindberg, E Deau, J Arfwedson… - Journal of medicinal …, 2023 - ACS Publications
Dual-specificity, tyrosine phosphorylation-regulated kinases (DYRKs) and cdc2-like kinases
(CLKs) play a large variety of cellular functions and are involved in several diseases …
(CLKs) play a large variety of cellular functions and are involved in several diseases …
Leucettinib-21, a DYRK1A Kinase Inhibitor as Clinical Drug Candidate for Alzheimer's Disease and Down Syndrome
L Meijer, E Chrétien, D Ravel - Journal of Alzheimer's …, 2024 - journals.sagepub.com
Alzheimer's disease (AD) and Down syndrome (DS) share a common therapeutic target, the
dual-specificity, tyrosine phosphorylation activated kinase 1A (DYRK1A). Abnormally active …
dual-specificity, tyrosine phosphorylation activated kinase 1A (DYRK1A). Abnormally active …
Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B
E Deau, MF Lindberg, F Miege, D Roche… - Journal of Medicinal …, 2023 - ACS Publications
Dual-specificity, tyrosine phosphorylation-regulated kinases (DYRKs) and cdc2-like kinases
(CLKs) recently attracted attention due to their central involvement in various pathologies …
(CLKs) recently attracted attention due to their central involvement in various pathologies …
Discovery of ZJCK-6-46: A Potent, Selective, and Orally Available Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A Inhibitor for the Treatment of …
H Chen, X Gao, X Li, C Yu, W Liu, J Qiu… - Journal of Medicinal …, 2024 - ACS Publications
Targeting dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) has been
verified to regulate the progression of tau pathology as a promising treatment for Alzheimer's …
verified to regulate the progression of tau pathology as a promising treatment for Alzheimer's …
Targeting the DYRK1A kinase prevents cancer progression and metastasis and promotes cancer cells response to G1/S targeting chemotherapy drugs
Metastatic cancer remains incurable as patients eventually loose sensitivity to targeted
therapies and chemotherapies, further leading to poor clinical outcome. Thus, there is a …
therapies and chemotherapies, further leading to poor clinical outcome. Thus, there is a …
Discovery and functional characterization of a potent, selective, and metabolically stable PROTAC of the protein kinases DYRK1A and DYRK1B
G Wilms, K Schofield, S Maddern, C Foley… - Journal of Medicinal …, 2024 - ACS Publications
Small-molecule-induced protein degradation has emerged as a promising pharmacological
modality for inactivating disease-relevant protein kinases. DYRK1A and DYRK1B are …
modality for inactivating disease-relevant protein kinases. DYRK1A and DYRK1B are …
Efficacy of DYRK1A inhibitors in novel models of Down syndrome acute lymphoblastic leukemia
SL Carey-Smith, MH Simad, K Panchal… - …, 2024 - pmc.ncbi.nlm.nih.gov
Despite significant advances, outcomes for children with Down syndrome (DS, trisomy 21)
who develop acute lymphoblastic leukemia (ALL) remain poor. Reports of large DSALL …
who develop acute lymphoblastic leukemia (ALL) remain poor. Reports of large DSALL …
Natural Bioactive Compounds from Marine Invertebrates That Modulate Key Targets Implicated in the Onset of Type 2 Diabetes Mellitus (T2DM) and Its Complications
M Casertano, A Vito, A Aiello, C Imperatore, M Menna - Pharmaceutics, 2023 - mdpi.com
Background: Type 2 diabetes mellitus (T2DM) is an ongoing, risky, and costly health
problem that therefore always requires new treatment options. Moreover, although several …
problem that therefore always requires new treatment options. Moreover, although several …
DYRK1A inhibitors leucettines and TGF-β inhibitor additively stimulate insulin production in beta cells, organoids, and isolated mouse islets
The decreased β-cell mass and impaired β-cell functionality are the primary causes of
diabetes mellitus (DM). Nevertheless, the underlying molecular mechanisms by which β-cell …
diabetes mellitus (DM). Nevertheless, the underlying molecular mechanisms by which β-cell …