Achieving effective and selective CK1 inhibitors through structure modification

p63 uses a switch-like mechanism to set the threshold for induction of apoptosis

(2020) Jakob Gebel et al.   Nature Chemical Biology

Design, Synthesis and Biological Evaluation of Isoxazole-Based CK1 Inhibitors Modified with Chiral Pyrrolidine Scaffolds

(2019) Andreas Luxenburger et al.   MOLECULES

Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ

(2019) Jae Wook Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε

(2018) Balbina García-Reyes et al.   JOURNAL OF MEDICINAL CHEMISTRY

Casein Kinase 1δ/ε Inhibitor, PF670462 Attenuates the Fibrogenic Effects of Transforming Growth Factor-β in Pulmonary Fibrosis

(2018) Christine R. Keenan et al.   Frontiers in Pharmacology

Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models

(2018) Waleed Minzel et al.   CELL

Combined Virtual and Experimental Screening for CK1 Inhibitors Identifies a Modulator of p53 and Reveals Important Aspects of in Silico Screening Performance

(2017) Vassilios Myrianthopoulos et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

State-dependent block of voltage-gated sodium channels by the casein-kinase 1 inhibitor IC261

(2017) Karl J. Föhr et al.   INVESTIGATIONAL NEW DRUGS

Discovery of potential neurodegenerative inhibitors in Alzheimer’s disease by casein kinase 1 structure-based virtual screening

(2017) Ricardo P. Rodrigues et al.   MEDICINAL CHEMISTRY RESEARCH

Optimized 4,5-Diarylimidazoles as Potent/Selective Inhibitors of Protein Kinase CK1δ and Their Structural Relation to p38α MAPK

(2017) Jakob Halekotte et al.   MOLECULES

The target landscape of clinical kinase drugs

(2017) Susan Klaeger et al.   SCIENCE

Pharmacological activation of wild-type p53 in the therapy of leukemia

(2016) Kensuke Kojima et al.   EXPERIMENTAL HEMATOLOGY

Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

(2016) Georg Petzold et al.   NATURE

Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS

(2015) Jan Krönke et al.   NATURE

Casein kinase 1 and Wnt/β-catenin signaling

(2014) Cristina-Maria Cruciat   CURRENT OPINION IN CELL BIOLOGY

Difluoro-dioxolo-benzoimidazol-benzamides As Potent Inhibitors of CK1δ and ε with Nanomolar Inhibitory Activity on Cancer Cell Proliferation

(2014) Julia Richter et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protein Kinase CK-1 Inhibitors As New Potential Drugs for Amyotrophic Lateral Sclerosis

(2014) Irene G. Salado et al.   JOURNAL OF MEDICINAL CHEMISTRY

CSNK1α1 mediates malignant plasma cell survival

(2014) Y Hu et al.   LEUKEMIA

The CK1 Family: Contribution to Cellular Stress Response and Its Role in Carcinogenesis

(2014) Uwe Knippschild et al.   Frontiers in Oncology

Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties

(2013) Mathieu Bibian et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway

(2013) Anne-Sophie Huart et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Ligand–Protein Interactions of Selective Casein Kinase 1δ Inhibitors

(2013) Scot Mente et al.   JOURNAL OF MEDICINAL CHEMISTRY

2-Benzamido-N-(1H-benzo[d]imidazol-2-yl)thiazole-4-carboxamide derivatives as potent inhibitors of CK1δ/ε

(2012) Joachim Bischof et al.   AMINO ACIDS

Exploiting Synthetic Lethality for the Therapy of ABC Diffuse Large B Cell Lymphoma

(2012) Yibin Yang et al.   CANCER CELL

Discovery of N6-phenyl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamine derivatives as novel CK1 inhibitors using common-feature pharmacophore model based virtual screening and hit-to-lead optimization

(2012) Ling-Ling Yang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structural Basis for the Potent and Selective Inhibition of Casein Kinase 1 Epsilon

(2012) Alexander M. Long et al.   JOURNAL OF MEDICINAL CHEMISTRY

The complex world of WNT receptor signalling

(2012) Christof Niehrs   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Secreted and Transmembrane Wnt Inhibitors and Activators

(2012) C.-M. Cruciat et al.   Cold Spring Harbor Perspectives in Biology

Structure-Based Design of Potent and Selective CK1γ Inhibitors

(2012) Hongbing Huang et al.   ACS Medicinal Chemistry Letters

A Small Molecule Modulates Circadian Rhythms through Phosphorylation of the Period Protein

(2011) Jae Wook Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Inhibition of Wnt/β-Catenin Signaling by p38 MAP Kinase Inhibitors Is Explained by Cross-Reactivity with Casein Kinase Iδ/ɛ

(2011) Folkert Verkaar et al.   CHEMISTRY & BIOLOGY

Structural Basis for the Interaction between Casein Kinase 1 Delta and a Potent and Selective Inhibitor

(2011) Alexander Long et al.   JOURNAL OF MEDICINAL CHEMISTRY

IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/ɛ and Wnt/β-catenin independent inhibition of mitotic spindle formation

(2011) J K Cheong et al.   ONCOGENE

Protein Kinase CK1αLS Promotes Vascular Cell Proliferation and Intimal Hyperplasia

(2010) Mikhail P. Panchenko et al.   AMERICAN JOURNAL OF PATHOLOGY

Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α

(2010) Curtis A Thorne et al.   Nature Chemical Biology

Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes

(2010) Q.-J. Meng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

High-Throughput Chemical Screen Identifies a Novel Potent Modulator of Cellular Circadian Rhythms and Reveals CKIα as a Clock Regulatory Kinase

(2010) Tsuyoshi Hirota et al.   PLOS BIOLOGY

Autophosphorylation of carboxy-terminal residues inhibits the activity of protein kinase CK1α

(2009) Mauricio Budini et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

3,4-Diaryl-isoxazoles and -imidazoles as Potent Dual Inhibitors of p38α Mitogen Activated Protein Kinase and Casein Kinase 1δ†

(2009) Christian Peifer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Inhibition of Casein Kinase 1  Minimally Alters Circadian Clock Period

(2009) K. M. Walton et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

The gatekeeper mutation T315I confers resistance against small molecules by increasing or restoring the ABL-kinase activity accompanied by aberrant transphosphorylation of endogenous BCR, even in loss-of-function mutants of BCR/ABL

(2009) A A Mian et al.   LEUKEMIA

Casein Kinase 1 Delta Regulates the Pace of the Mammalian Circadian Clock

(2009) J.-P. Etchegaray et al.   MOLECULAR AND CELLULAR BIOLOGY

Targeting protein kinases in central nervous system disorders

(2009) Laura K. Chico et al.   NATURE REVIEWS DRUG DISCOVERY

Immunohistochemical Characterisation of Cell-Type Specific Expression of CK1δ in Various Tissues of Young Adult BALB/c Mice

(2009) Jürgen Löhler et al.   PLoS One

A Novel Consensus Phosphorylation Motif in Sulfatide- and Cholesterol-3-sulfate-Binding Protein Substrates for CK1 in Vitro

(2008) Fumitaka Kawakami et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Anti-apoptotic and growth-stimulatory functions of CK1 delta and epsilon in ductal adenocarcinoma of the pancreas are inhibited by IC261 in vitro and in vivo

(2008) C Brockschmidt et al.   GUT

Inhibition of casein kinase 1-epsilon induces cancer-cell-selective, PERIOD2-dependent growth arrest

(2008) Wan Seok Yang et al.   GENOME BIOLOGY