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

Discovery of a Highly Selective STK16 Kinase Inhibitor

(2016) Feiyang Liu et al.   ACS Chemical Biology

A Landscape of Pharmacogenomic Interactions in Cancer

(2016) Francesco Iorio et al.   CELL

Unprecedently Large-Scale Kinase Inhibitor Set Enabling the Accurate Prediction of Compound–Kinase Activities: A Way toward Selective Promiscuity by Design?

(2016) Serge Christmann-Franck et al.   Journal of Chemical Information and Modeling

EGFR inhibitors identified as a potential treatment for chordoma in a focused compound screen

(2016) Susanne Scheipl et al.   JOURNAL OF PATHOLOGY

Pharmacological Inhibition of the Protein Kinase MRK/ZAK Radiosensitizes Medulloblastoma

(2016) D. Markowitz et al.   MOLECULAR CANCER THERAPEUTICS

Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds

(2016) Gregory J. Crowther et al.   PLoS One

Integrated genetic and pharmacologic interrogation of rare cancers

(2016) Andrew L. Hong et al.   Nature Communications

Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni

(2016) Thavy Long et al.   PLoS Neglected Tropical Diseases

Identification of Small Molecule Inhibitors That Block the Toxoplasma gondii Rhoptry Kinase ROP18

(2016) Catherine Simpson et al.   ACS Infectious Diseases

Identification of “Preferred” Human Kinase Inhibitors for Sleeping Sickness Lead Discovery. Are Some Kinases Better than Others for Inhibitor Repurposing?

(2016) Emanuele Amata et al.   ACS Infectious Diseases

Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules

(2015) Andrew K. Urick et al.   ACS Chemical Biology

Rational Polypharmacology: Systematically Identifying and Engaging Multiple Drug Targets To Promote Axon Growth

(2015) Hassan Al-Ali et al.   ACS Chemical Biology

Ten things you should know about protein kinases: IUPHAR Review 14

(2015) Doriano Fabbro et al.   BRITISH JOURNAL OF PHARMACOLOGY

Systematic Mapping of Kinase Addiction Combinations in Breast Cancer Cells by Integrating Drug Sensitivity and Selectivity Profiles

(2015) Agnieszka Szwajda et al.   CHEMISTRY & BIOLOGY

Low cost whole-organism screening of compounds for anthelmintic activity

(2015) Sarah Preston et al.   INTERNATIONAL JOURNAL FOR PARASITOLOGY

Integrated Approaches for Genome-wide Interrogation of the Druggable Non-olfactory G Protein-coupled Receptor Superfamily

(2015) Bryan L. Roth et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting cancer with kinase inhibitors

(2015) Stefan Gross et al.   JOURNAL OF CLINICAL INVESTIGATION

KINATEST-ID: A Pipeline To Develop Phosphorylation-Dependent Terbium Sensitizing Kinase Assays

(2015) Andrew M. Lipchik et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A chemical-genetic interaction map of small molecules using high-throughput imaging in cancer cells

(2015) M. Breinig et al.   Molecular Systems Biology

Comprehensive characterization of the Published Kinase Inhibitor Set

(2015) Jonathan M Elkins et al.   NATURE BIOTECHNOLOGY

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

A historical overview of protein kinases and their targeted small molecule inhibitors

(2015) Robert Roskoski   PHARMACOLOGICAL RESEARCH

FDA-approved small-molecule kinase inhibitors

(2015) Peng Wu et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Harnessing Connectivity in a Large-Scale Small-Molecule Sensitivity Dataset

(2015) B. Seashore-Ludlow et al.   Cancer Discovery

LIM kinase inhibitors disrupt mitotic microtubule organization and impair tumor cell proliferation

(2015) Katerina Mardilovich et al.   Oncotarget

Identification and Structure–Function Analysis of Subfamily Selective G Protein-Coupled Receptor Kinase Inhibitors

(2014) Kristoff T. Homan et al.   ACS Chemical Biology

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

(2014) Stuart W. J. Ember et al.   ACS Chemical Biology

The Arabidopsis Kinome: phylogeny and evolutionary insights into functional diversification

(2014) Monika Zulawski et al.   BMC GENOMICS

Functional Characterization of CFI-400945, a Polo-like Kinase 4 Inhibitor, as a Potential Anticancer Agent

(2014) Jacqueline M. Mason et al.   CANCER CELL

Chemical Interrogation of the Malaria Kinome

(2014) Emily R. Derbyshire et al.   CHEMBIOCHEM

Seeding Collaborations to Advance Kinase Science with the GSK Published Kinase Inhibitor Set (PKIS)

(2014) David Drewry et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Making Sense of Large-Scale Kinase Inhibitor Bioactivity Data Sets: A Comparative and Integrative Analysis

(2014) Jing Tang et al.   Journal of Chemical Information and Modeling

Pharmacological Profiling of Kinase Dependency in Cell Lines across Triple-Negative Breast Cancer Subtypes

(2014) L. S. Fink et al.   MOLECULAR CANCER THERAPEUTICS

GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors

(2014) Curtis A Thorne et al.   Nature Chemical Biology

Advances in targeting cyclic nucleotide phosphodiesterases

(2014) Donald H. Maurice et al.   NATURE REVIEWS DRUG DISCOVERY

Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders

(2014) Katrina J. Falkenberg et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death

(2014) Joanne M. Hildebrand et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Kinase Pathway Dependence in Primary Human Leukemias Determined by Rapid Inhibitor Screening

(2012) J. W. Tyner et al.   CANCER RESEARCH

A public-private partnership to unlock the untargeted kinome

(2012) Stefan Knapp et al.   Nature Chemical Biology

Tackling Drought Stress: RECEPTOR-LIKE KINASES Present New Approaches

(2012) Alex Marshall et al.   PLANT CELL

STK33 kinase inhibitor BRD-8899 has no effect on KRAS-dependent cancer cell viability

(2012) T. Luo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The role of GRK6 in animal models of Parkinson's Disease and L-DOPA treatment

(2012) Francesca Managò et al.   Scientific Reports

A theoretical entropy score as a single value to express inhibitor selectivity

(2011) Joost CM Uitdehaag et al.   BMC BIOINFORMATICS

An Integrated In Vitro and In Vivo High-Throughput Screen Identifies Treatment Leads for Ependymoma

(2011) Jennifer M. Atkinson et al.   CANCER CELL

Too many roads not taken

(2011) Aled M. Edwards et al.   NATURE

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Navigating the kinome

(2011) James T Metz et al.   Nature Chemical Biology

The (un)targeted cancer kinome

(2010) Oleg Fedorov et al.   Nature Chemical Biology

Kinome-wide RNAi studies in human multiple myeloma identify vulnerable kinase targets, including a lymphoid-restricted kinase, GRK6

(2009) R. E. Tiedemann et al.   BLOOD

Assessment of Chemical Coverage of Kinome Space and Its Implications for Kinase Drug Discovery

(2008) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY