How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition—The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine

A short divergent approach to highly substituted carbazoles and β-carbolines via in situ-generated diketoindoles

(2020) Martin Untergehrer et al.   TETRAHEDRON LETTERS

A Novel Approach to Highly Substituted β-Carbolines via Reductive Ring Transformation of 2-Acyl-3-isoxazolylindoles

(2020) Alexandra Kamlah et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

DFG-1 residue controls inhibitor binding mode and affinity providing a basis for rational design of kinase inhibitor selectivity

(2020) Martin Schröder et al.   JOURNAL OF MEDICINAL CHEMISTRY

The DYRK Family of Kinases in Cancer: Molecular Functions and Therapeutic Opportunities

(2020) Jacopo Boni et al.   Cancers

New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis

(2019) Helmi Tazarki et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

[b]-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors

(2019) Christian Lechner et al.   MOLECULES

Development of novel 2,4-bispyridyl thiophene–based compounds as highly potent and Selective Dyrk1A inhibitors. Part I: Benzamide and benzylamide derivatives

(2018) Sarah S. Darwish et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Isoform selectivity of harmine-conjugated 1,2,3-triazoles against human monoamine oxidase

(2018) Saqlain Haider et al.   Future Medicinal Chemistry

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

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

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

DYRK1A: A Promising Drug Target for Islet Transplant–Based Diabetes Therapies

(2016) Bengt-Frederik Belgardt et al.   DIABETES

Selectivity Profiling and Biological Activity of Novel β-Carbolines as Potent and Selective DYRK1 Kinase Inhibitors

(2015) Katharina Rüben et al.   PLoS One

Computational & experimental evaluation of the structure/activity relationship of β-carbolines as DYRK1A inhibitors

(2014) Binia Drung et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors

(2014) Amélie Bruel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

DYRK1A: A Potential Drug Target for Multiple Down Syndrome Neuropathologies

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

Structures of Down Syndrome Kinases, DYRKs, Reveal Mechanisms of Kinase Activation and Substrate Recognition

(2013) Meera Soundararajan et al.   STRUCTURE

Structure–activity relationship study of beta-carboline derivatives as haspin kinase inhibitors

(2012) Gregory D. Cuny et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Specific CLK Inhibitors from a Novel Chemotype for Regulation of Alternative Splicing

(2011) Oleg Fedorov et al.   CHEMISTRY & BIOLOGY

7,8-Dichloro-1-oxo-β-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes

(2011) Kilian Huber et al.   JOURNAL OF MEDICINAL CHEMISTRY

β-Carboline Compounds, Including Harmine, Inhibit DYRK1A and Tau Phosphorylation at Multiple Alzheimer's Disease-Related Sites

(2011) Danielle Frost et al.   PLoS One

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

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

Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation

(2009) Nora Göckler et al.   FEBS Journal

Synthesis and cytotoxic activities of 1-benzylidine substituted β-carboline derivatives

(2008) Rihui Cao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure of human monoamine oxidase A at 2.2-A resolution: The control of opening the entry for substrates/inhibitors

(2008) S.-Y. Son et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA