Quantifying CDK inhibitor selectivity in live cells

Quantifying Target Occupancy of Small Molecules Within Living Cells

(2020) M.B. Robers et al.   Annual Review of Biochemistry

Discovery and characterization of SY-1365, a selective, covalent inhibitor of CDK7

(2019) Shanhu Hu et al.   CANCER RESEARCH

Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials

(2019) Ann Lin et al.   Science Translational Medicine

A Photoaffinity Displacement Assay and Probes to Study the Cyclin-Dependent Kinase Family

(2019) Emma K. Grant et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015–2019)

(2019) Concepción Sánchez-Martínez et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment

(2018) Hetal Patel et al.   MOLECULAR CANCER THERAPEUTICS

Kinase inhibitors: the road ahead

(2018) Fleur M. Ferguson et al.   NATURE REVIEWS DRUG DISCOVERY

How selective are pharmacological inhibitors of cell cycle-regulating cyclin-dependent kinases?

(2018) Radek Jorda et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update

(2018) Solomon Tadesse et al.   JOURNAL OF MEDICINAL CHEMISTRY

Binding Kinetics Survey of the Drugged Kinome

(2018) Victoria Georgi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors

(2018) Meiyang Xi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes

(2017) Qian Zhao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibitors of cyclin-dependent kinases as cancer therapeutics

(2017) Steven R. Whittaker et al.   PHARMACOLOGY & THERAPEUTICS

Preclinical characterization of abemaciclib in hormone receptor positive breast cancer

(2017) Raquel Torres-Guzmán et al.   Oncotarget

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

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

Conformational Adaption May Explain the Slow Dissociation Kinetics of Roniciclib (BAY 1000394), a Type I CDK Inhibitor with Kinetic Selectivity for CDK2 and CDK9

(2016) Pelin Ayaz et al.   ACS Chemical Biology

Effects of target binding kinetics onin vivodrug efficacy: koff, konand rebinding

(2016) Georges Vauquelin   BRITISH JOURNAL OF PHARMACOLOGY

Small-molecule kinase inhibitors: an analysis of FDA-approved drugs

(2016) Peng Wu et al.   DRUG DISCOVERY TODAY

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

(2016) Aurélie Mallinger et al.   JOURNAL OF MEDICINAL CHEMISTRY

Treating cancer with selective CDK4/6 inhibitors

(2016) Ben O'Leary et al.   Nature Reviews Clinical Oncology

Acquired CDK6 amplification promotes breast cancer resistance to CDK4/6 inhibitors and loss of ER signaling and dependence

(2016) C Yang et al.   ONCOGENE

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8

(2016) Philippe Bergeron et al.   ACS Medicinal Chemistry Letters

Type II Inhibitors Targeting CDK2

(2015) Leila T. Alexander et al.   ACS Chemical Biology

NanoLuc Complementation Reporter Optimized for Accurate Measurement of Protein Interactions in Cells

(2015) Andrew S. Dixon et al.   ACS Chemical Biology

A Novel CDK7 Inhibitor of the Pyrazolotriazine Class Exerts Broad-Spectrum Antiviral Activity at Nanomolar Concentrations

(2015) Corina Hutterer et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Cyclin dependent kinase (CDK) inhibitors as anticancer drugs

(2015) Concepción Sánchez-Martínez et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Translating slow-binding inhibition kinetics into cellular and in vivo effects

(2015) Grant K Walkup et al.   Nature Chemical Biology

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

(2015) Trevor Dale et al.   Nature Chemical Biology

Application of BRET to monitor ligand binding to GPCRs

(2015) Leigh A Stoddart et al.   NATURE METHODS

The history and future of targeting cyclin-dependent kinases in cancer therapy

(2015) Uzma Asghar et al.   NATURE REVIEWS DRUG DISCOVERY

Target engagement and drug residence time can be observed in living cells with BRET

(2015) Matthew B. Robers et al.   Nature Communications

A novel small-molecule MRCK inhibitor blocks cancer cell invasion

(2014) Mathieu Unbekandt et al.   Cell Communication and Signaling

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor

(2014) Nicholas Kwiatkowski et al.   NATURE

Cyclin-dependent kinases

(2014) Marcos Malumbres   GENOME BIOLOGY

Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors

(2013) Tara R. Rheault et al.   ACS Medicinal Chemistry Letters

Cyclin-dependent kinase 5 regulates E2F transcription factor through phosphorylation of Rb protein in neurons

(2012) Akira Futatsugi et al.   CELL CYCLE

Perspective of Cyclin-dependent kinase 9 (CDK9) as a Drug Target

(2012) Vladimir Krystof et al.   CURRENT PHARMACEUTICAL DESIGN

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Rebinding: or why drugs may act longerin vivothan expected from theirin vitrotarget residence time

(2010) Georges Vauquelin   Expert Opinion on Drug Discovery

The Development of a Selective Cyclin-Dependent Kinase Inhibitor That Shows Antitumor Activity

(2009) S. Ali et al.   CANCER RESEARCH

CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients

(2009) A Pardanani et al.   LEUKEMIA

Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines

(2009) M. S. Squires et al.   MOLECULAR CANCER THERAPEUTICS

Cyclin-dependent kinases: a family portrait

(2009) Marcos Malumbres et al.   NATURE CELL BIOLOGY

Identification ofN-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design†

(2008) Paul G. Wyatt et al.   JOURNAL OF MEDICINAL CHEMISTRY

CDK8 is a colorectal cancer oncogene that regulates β-catenin activity

(2008) Ron Firestein et al.   NATURE