Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration

The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification

(2021) Carrow I. Wells et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Defining the Neural Kinome: Strategies and Opportunities for Small Molecule Drug Discovery to Target Neurodegenerative Diseases

(2020) Andrea I Krahn et al.   ACS Chemical Neuroscience

Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1

(2020) Andrew Fensome et al.   BIOORGANIC & MEDICINAL CHEMISTRY

TBK1 phosphorylates mutant Huntingtin and suppresses its aggregation and toxicity in Huntington's disease models

(2020) Ramanath Narayana Hegde et al.   EMBO JOURNAL

The Dark Kinase Knowledgebase: an online compendium of knowledge and experimental results of understudied kinases

(2020) Matthew E Berginski et al.   NUCLEIC ACIDS RESEARCH

Development and Therapeutic Potential of NUAKs Inhibitors

(2020) Muhammad Faisal et al.   JOURNAL OF MEDICINAL CHEMISTRY

WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop

(2019) Megan J. Agajanian et al.   Cell Reports

Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor

(2019) Douglas W. Thomson et al.   ACS Medicinal Chemistry Letters

SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK)

(2019) Christopher R. M. Asquith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Conservation of structure, function and inhibitor binding in UNC-51-like kinase 1 and 2 (ULK1/2)

(2019) Apirat Chaikuad et al.   BIOCHEMICAL JOURNAL

Macromolecular structure determination using X-rays, neutrons and electrons: recent developments in Phenix

(2019) Dorothee Liebschner et al.   Acta Crystallographica Section D-Structural Biology

LINCS Data Portal 2.0: next generation access point for perturbation-response signatures

(2019) Vasileios Stathias et al.   NUCLEIC ACIDS RESEARCH

SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K

(2019) Carrow Wells et al.   ACS Medicinal Chemistry Letters

Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update

(2019) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Glimmers in illuminating the druggable genome

(2018) Griffin Rodgers et al.   NATURE REVIEWS DRUG DISCOVERY

Common and rare TBK1 variants in early-onset Alzheimer disease in a European cohort

(2018) Jan Verheijen et al.   NEUROBIOLOGY OF AGING

DA+ data acquisition and analysis software at the Swiss Light Source macromolecular crystallography beamlines

(2018) Justyna Aleksandra Wojdyla et al.   JOURNAL OF SYNCHROTRON RADIATION

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

(2018) Andrew Fensome et al.   JOURNAL OF MEDICINAL CHEMISTRY

Coral: Clear and Customizable Visualization of Human Kinome Data

(2018) Kathleen S. Metz et al.   Cell Systems

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

(2017) Andrew P. Crew et al.   JOURNAL OF MEDICINAL CHEMISTRY

TBK1: a new player in ALS linking autophagy and neuroinflammation

(2017) James A. Oakes et al.   Molecular Brain

Progress towards a public chemogenomic set for protein kinases and a call for contributions

(2017) David H. Drewry et al.   PLoS One

Reduction of Nuak1 Decreases Tau and Reverses Phenotypes in a Tauopathy Mouse Model

(2016) Cristian A. Lasagna-Reeves et al.   NEURON

Pharmacological Inhibition of ULK1 Kinase Blocks Mammalian Target of Rapamycin (mTOR)-dependent Autophagy

(2015) Katy J. Petherick et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Haploinsufficiency of TBK1 causes familial ALS and fronto-temporal dementia

(2015) Axel Freischmidt et al.   NATURE NEUROSCIENCE

Identification and Further Development of Potent TBK1 Inhibitors

(2014) André Richters et al.   ACS Chemical Biology

Dysfunction of Endocytic Kinase AAK1 in ALS

(2014) Bingxing Shi et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Evaluating TBK1 as a Therapeutic Target in Cancers with Activated IRF3

(2014) Asli Muvaffak et al.   MOLECULAR CANCER RESEARCH

Crystal Structure and Mechanism of Activation of TANK-Binding Kinase 1

(2013) Amede Larabi et al.   Cell Reports

Synthesis and structure–activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases

(2012) Edward G. McIver et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of a High-Throughput Assay for Identifying Inhibitors of TBK1 and IKKε

(2012) Jessica E. Hutti et al.   PLoS One

Novel cross-talk within the IKK family controls innate immunity

(2011) Kristopher Clark et al.   BIOCHEMICAL JOURNAL

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY