Structure–Activity Relationships and Biological Evaluation of 7-Substituted Harmine Analogs for Human β-Cell Proliferation

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

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

Improvements to the APBS biomolecular solvation software suite

(2017) Elizabeth Jurrus et al.   PROTEIN SCIENCE

Development of a reliable automated screening system to identify small molecules and biologics that promote human β-cell regeneration

(2016) Kristie I. Aamodt et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Inhibition of DYRK1A Stimulates Human β-Cell Proliferation

(2016) Ercument Dirice et al.   DIABETES

Selective inhibition of the kinase DYRK1A by targeting its folding process

(2016) Isao Kii et al.   Nature Communications

Leucettine L41, a DYRK1A-preferential DYRKs/CLKs inhibitor, prevents memory impairments and neurotoxicity induced by oligomeric Aβ25–35 peptide administration in mice

(2015) Gaëlle Naert et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

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

Effect of targeted estrogen delivery using glucagon-like peptide-1 on insulin secretion, insulin sensitivity and glucose homeostasis

(2015) Joseph P. Tiano et al.   Scientific Reports

Dyrk1A induces pancreatic β cell mass expansion and improves glucose tolerance

(2014) Latif Rachdi et al.   CELL CYCLE

DYRK1A: A Potential Drug Target for Multiple Down Syndrome Neuropathologies

(2014) Walter Becker et al.   CNS & Neurological Disorders-Drug Targets

Synthesis and Antiviral and Fungicidal Activity Evaluation of β-Carboline, Dihydro-β-carboline, Tetrahydro-β-carboline Alkaloids, and Their Derivatives

(2014) Hongjian Song et al.   JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

Design and Synthesis of Thiazolo[5,4-f]quinazolines as DYRK1A Inhibitors, Part II

(2014) Alicia Foucourt et al.   MOLECULES

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

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

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

Targeted estrogen delivery reverses the metabolic syndrome

(2012) Brian Finan et al.   NATURE MEDICINE

Adenosine kinase inhibition selectively promotes rodent and porcine islet  -cell replication

(2012) J. P. Annes et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Web servers and services for electrostatics calculations with APBS and PDB2PQR

(2011) Samir Unni et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

Synthesis, Protein Kinase Inhibitory Potencies, and in Vitro Antiproliferative Activities of Meridianin Derivatives

(2011) Francis Giraud et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and evaluation of β-carboline derivatives as potential monoamine oxidase inhibitors

(2010) J. Reniers et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Activation, regulation, and inhibition of DYRK1A

(2010) Walter Becker et al.   FEBS Journal

The role of DYRK1A in neurodegenerative diseases

(2010) Jerzy Wegiel et al.   FEBS Journal

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

(2010) Yasushi Ogawa et al.   Nature Communications

Quinalizarin as a potent, selective and cell-permeable inhibitor of protein kinase CK2

(2009) Giorgio Cozza et al.   BIOCHEMICAL JOURNAL

Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins

(2009) Rufine Akue-Gedu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

QSAR analysis of pyrazolidine-3,5-diones derivatives as Dyrk1A inhibitors

(2009) Kyung Ah Koo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2009) César Sánchez et al.   CHEMICAL COMMUNICATIONS

Pd-Catalyzed Conversion of Aryl Chlorides, Triflates, and Nonaflates to Nitroaromatics

(2009) Brett P. Fors et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Two New Peltogynoids fromAcacia niloticaDelile with Kinase Inhibitory Activity

(2009) Augustine Ahmadu et al.   PLANTA MEDICA

Green Tea Polyphenols Rescue of Brain Defects Induced by Overexpression of DYRK1A

(2009) Fayçal Guedj et al.   PLoS One

Meriolins (3-(Pyrimidin-4-yl)-7-azaindoles): Synthesis, Kinase Inhibitory Activity, Cellular Effects, and Structure of a CDK2/Cyclin A/Meriolin Complex†

(2008) Aude Echalier et al.   JOURNAL OF MEDICINAL CHEMISTRY