A Dual Inhibitor of DYRK1A and GSK3β for β‐Cell Proliferation: Aminopyrazine Derivative GNF4877

Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor

(2020) Kunal Kumar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133

(2020) Yahu A. Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

GLP-1 receptor agonists synergize with DYRK1A inhibitors to potentiate functional human β cell regeneration

(2020) Courtney Ackeifi et al.   Science Translational Medicine

Generation of highly potent DYRK1A-dependent inducers of human β-Cell replication via Multi-Dimensional compound optimization

(2019) Paul A. Allegretti et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics

(2018) Dnyandev B. Jarhad et al.   JOURNAL OF MEDICINAL CHEMISTRY

DYRK1A inhibition and cognitive rescue in a Down syndrome mouse model are induced by new fluoro-DANDY derivatives

(2018) Fernanda Neumann et al.   Scientific Reports

Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity

(2018) Kunal Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation

(2018) Kunal Kumar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Combined Inhibition of DYRK1A, SMAD, and Trithorax Pathways Synergizes to Induce Robust Replication in Adult Human Beta Cells

(2018) Peng Wang et al.   Cell Metabolism

Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors: a survey of recent patent literature

(2017) Thu Lan Nguyen et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Human beta cell mass and function in diabetes: Recent advances in knowledge and technologies to understand disease pathogenesis

(2017) Chunguang Chen et al.   Molecular Metabolism

SerpinB1 Promotes Pancreatic β Cell Proliferation

(2016) Abdelfattah El Ouaamari et al.   Cell Metabolism

Pancreas-Specific Delivery of β-Cell Proliferating Small Molecules

(2016) Xueshi Hao et al.   ChemMedChem

Inhibition of DYRK1A Stimulates Human β-Cell Proliferation

(2016) Ercument Dirice et al.   DIABETES

Novel factors modulating human β-cell proliferation

(2016) J. Shirakawa et al.   DIABETES OBESITY & METABOLISM

Selective inhibition of the kinase DYRK1A by targeting its folding process

(2016) Isao Kii et al.   Nature Communications

Meridianin derivatives as potent Dyrk1A inhibitors and neuroprotective agents

(2015) Rammohan R. Yadav et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

10-Iodo-11H-indolo[3,2-c]quinoline-6-carboxylic Acids Are Selective Inhibitors of DYRK1A

(2015) Hannes Falke et al.   JOURNAL OF MEDICINAL CHEMISTRY

A novel DYRK1A (Dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologiesin vitro

(2015) Séverine Coutadeur et al.   JOURNAL OF NEUROCHEMISTRY

A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication

(2015) Peng Wang et al.   NATURE MEDICINE

Inhibition of DYRK1A and GSK3B induces human β-cell proliferation

(2015) Weijun Shen et al.   Nature Communications

Development of DANDYs, New 3,5-Diaryl-7-azaindoles Demonstrating Potent DYRK1A Kinase Inhibitory Activity

(2013) Stéphanie Gourdain et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small-Molecule Inducer of β Cell Proliferation Identified by High-Throughput Screening

(2013) Weijun Shen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Liver-Derived Systemic Factors Drive β Cell Hyperplasia in Insulin-Resistant States

(2013) Abdelfattah El Ouaamari et al.   Cell Reports

Recent Advances in the Design, Synthesis, and Biological Evaluation of Selective DYRK1A Inhibitors: A New Avenue for a Disease Modifying Treatment of Alzheimer’s?

(2012) Breland Smith et al.   ACS Chemical Neuroscience

Synthesis of chromeno[3,4-b]indoles as Lamellarin D analogues : A novel DYRK1A inhibitor class

(2012) Cleopatra Neagoie et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Selectivity, Cocrystal Structures, and Neuroprotective Properties of Leucettines, a Family of Protein Kinase Inhibitors Derived from the Marine Sponge Alkaloid Leucettamine B

(2012) Tania Tahtouh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk)

(2011) Andrew S. Rosenthal et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structural features underlying the selectivity of the kinase inhibitors NBC and dNBC: role of a nitro group that discriminates between CK2 and DYRK1A

(2011) Stefania Sarno et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Synthesis and biological evaluation of new 3-(6-hydroxyindol-2-yl)-5-(Phenyl) pyridine or pyrazine V-Shaped molecules as kinase inhibitors and cytotoxic agents

(2011) Pamela Kassis et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Emerging treatments for the prevention of type 1 diabetes

(2010) Philip Raskin et al.   EXPERT OPINION ON EMERGING DRUGS

Mechanisms of amine accumulation in, and egress from, lysosomes

(2010) Stephen DB Goldman et al.   Bioanalysis

Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A

(2010) Yasushi Ogawa et al.   Nature Communications

Generation of potent and selective kinase inhibitors by combinatorial biosynthesis of glycosylated indolocarbazoles

(2009) César Sánchez et al.   CHEMICAL COMMUNICATIONS