Strategic development of AZD1775, a Wee1 kinase inhibitor, for cancer therapy

A Phase I Clinical Trial of AZD1775 in Combination with Neoadjuvant Weekly Docetaxel and Cisplatin before Definitive Therapy in Head and Neck Squamous Cell Carcinoma

(2018) Eduardo Méndez et al.   CLINICAL CANCER RESEARCH

Targeting the DNA Damage Response in OSCC with TP53 Mutations

(2018) A. Lindemann et al.   JOURNAL OF DENTAL RESEARCH

Targeting the replication stress response in cancer

(2018) Josep V. Forment et al.   PHARMACOLOGY & THERAPEUTICS

Identification of CDC25 as a Common Therapeutic Target for Triple-Negative Breast Cancer

(2018) Jeff C. Liu et al.   Cell Reports

Inhibition of WEE1 kinase and cell cycle checkpoint activation sensitizes head and neck cancers to natural killer cell therapies

(2018) Jay Friedman et al.   Journal for ImmunoTherapy of Cancer

Loss of the Cyclin-Dependent Kinase Inhibitor 1 in the Context of Brachyury-Mediated Phenotypic Plasticity Drives Tumor Resistance to Immune Attack

(2018) Duane H. Hamilton et al.   Frontiers in Oncology

Directing the use of DDR kinase inhibitors in cancer treatment

(2017) Inger Brandsma et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

DNA repair factor RAD18 and DNA polymerase Polκ confer tolerance of oncogenic DNA replication stress

(2017) Yang Yang et al.   JOURNAL OF CELL BIOLOGY

Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors

(2017) Jin-Yi Zhu et al.   JOURNAL OF MEDICINAL CHEMISTRY

A comprehensive complex systems approach to the study and analysis of mammalian cell cycle control system in the presence of DNA damage stress

(2017) Ali Abroudi et al.   JOURNAL OF THEORETICAL BIOLOGY

CDK4/6 Inhibitors Sensitize Rb-positive Sarcoma Cells to Wee1 Kinase Inhibition through Reversible Cell-Cycle Arrest

(2017) Ashleigh M. Francis et al.   MOLECULAR CANCER THERAPEUTICS

Modeling Therapy Resistance in BRCA1/2 -Mutant Cancers

(2017) Amy Dréan et al.   MOLECULAR CANCER THERAPEUTICS

Moving Synergistically Acting Drug Combinations to the Clinic by Comparing Sequential versus Simultaneous Drug Administrations

(2017) Saketh S. Dinavahi et al.   MOLECULAR PHARMACOLOGY

Regulation of G2/M Transition by Inhibition of WEE1 and PKMYT1 Kinases

(2017) et al.   MOLECULES

Orthotopic patient-derived xenografts of paediatric solid tumours

(2017) Elizabeth Stewart et al.   NATURE

Activation of WEE1 confers resistance to PI3K inhibition in glioblastoma

(2017) Shaofang Wu et al.   NEURO-ONCOLOGY

Suppression of Sirt1 sensitizes lung cancer cells to WEE1 inhibitor MK-1775-induced DNA damage and apoptosis

(2017) G Chen et al.   ONCOGENE

Manipulating DNA damage-response signaling for the treatment of immune-mediated diseases

(2017) Jonathan P. McNally et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

G2-checkpoint targeting and radiosensitization of HPV/p16-positive HNSCC cells through the inhibition of Chk1 and Wee1

(2017) Chia-Jung Busch et al.   RADIOTHERAPY AND ONCOLOGY

WEE1 inhibition by MK1775 as a single-agent therapy inhibits ovarian cancer viability

(2017) Minghui Zhang et al.   Oncology Letters

Prolonged mitotic arrest induced by Wee1 inhibition sensitizes breast cancer cells to paclitaxel

(2017) Cody W. Lewis et al.   Oncotarget

WEE1 epigenetically modulates 5-hmC levels by pY37-H2B dependent regulation of IDH2 gene expression

(2017) Nupam P. Mahajan et al.   Oncotarget

Mutational status of TP53 defines the efficacy of Wee1 inhibitor AZD1775 in KRAS-mutant non-small cell lung cancer

(2017) Bo Mi Ku et al.   Oncotarget

Novel DNA targeted therapies for head and neck cancers: clinical potential and biomarkers

(2017) Mary Glorieux et al.   Oncotarget

WEE1 inhibition targets cell cycle checkpoints for triple negative breast cancers to overcome cisplatin resistance

(2017) Hongping Zheng et al.   Scientific Reports

Bistability of mitotic entry and exit switches during open mitosis in mammalian cells

(2016) Nadia Hégarat et al.   BIOESSAYS

Inhibition of CHK1 and WEE1 as a new therapeutic approach in diffuse large B cell lymphomas with MYC deregulation

(2016) Valentina Restelli et al.   BRITISH JOURNAL OF HAEMATOLOGY

DNA damage response as a therapeutic target in gynecological cancers

(2016) Alexandra Leary et al.   CURRENT OPINION IN ONCOLOGY

Cyclin E as a potential therapeutic target in high grade serous ovarian cancer

(2016) J. Kanska et al.   GYNECOLOGIC ONCOLOGY

Wee1 Kinase Inhibitor AZD1775 Radiosensitizes Hepatocellular Carcinoma Regardless of TP53 Mutational Status Through Induction of Replication Stress

(2016) Kyle C. Cuneo et al.   INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS

Phase II Study of WEE1 Inhibitor AZD1775 Plus Carboplatin in Patients With TP53-Mutated Ovarian Cancer Refractory or Resistant to First-Line Therapy Within 3 Months

(2016) Suzanne Leijen et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Study Evaluating WEE1 Inhibitor AZD1775 As Monotherapy and in Combination With Gemcitabine, Cisplatin, or Carboplatin in Patients With Advanced Solid Tumors

(2016) Suzanne Leijen et al.   JOURNAL OF CLINICAL ONCOLOGY

Cell cycle checkpoint in cancer: a therapeutically targetable double-edged sword

(2016) Roberta Visconti et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Expression and prognostic value of the WEE1 kinase in gliomas

(2016) Darija Music et al.   JOURNAL OF NEURO-ONCOLOGY

Quantitative Phosphoproteomics Reveals Wee1 Kinase as a Therapeutic Target in a Model of Proneural Glioblastoma

(2016) Rebecca S. Lescarbeau et al.   MOLECULAR CANCER THERAPEUTICS

PAXIP1 Potentiates the Combination of WEE1 Inhibitor AZD1775 and Platinum Agents in Lung Cancer

(2016) Ankita Jhuraney et al.   MOLECULAR CANCER THERAPEUTICS

A Genome-wide CRISPR Screen Identifies CDC25A as a Determinant of Sensitivity to ATR Inhibitors

(2016) Sergio Ruiz et al.   MOLECULAR CELL

Wee1 inhibition potentiates Wip1-dependent p53-negative tumor cell death during chemotherapy

(2016) V Clausse et al.   Cell Death & Disease

Combined inhibition of Wee1 and Chk1 gives synergistic DNA damage in S-phase due to distinct regulation of CDK activity and CDC45 loading

(2016) Sissel Hauge et al.   Oncotarget

Synergistic anti-leukemic interactions between panobinostat and MK-1775 in acute myeloid leukemia ex vivo

(2015) Wenxiu Qi et al.   CANCER BIOLOGY & THERAPY

Inhibiting WEE1 Selectively Kills Histone H3K36me3-Deficient Cancers by dNTP Starvation

(2015) Sophia X. Pfister et al.   CANCER CELL

Synergistic antitumor interactions between MK-1775 and panobinostat in preclinical models of pancreatic cancer

(2015) Guan Wang et al.   CANCER LETTERS

Cyclin-dependent kinase pathway aberrations in diverse malignancies: clinical and molecular characteristics

(2015) Shumei Kato et al.   CELL CYCLE

Wee-1 Kinase Inhibition Sensitizes High-Risk HPV+ HNSCC to Apoptosis Accompanied by Downregulation of MCl-1 and XIAP Antiapoptotic Proteins

(2015) N. Tanaka et al.   CLINICAL CANCER RESEARCH

The Efficacy of the Wee1 Inhibitor MK-1775 Combined with Temozolomide Is Limited by Heterogeneous Distribution across the Blood-Brain Barrier in Glioblastoma

(2015) J. L. Pokorny et al.   CLINICAL CANCER RESEARCH

An overview of tyrosine kinase inhibitors for the treatment of epithelial ovarian cancer

(2015) Zhijie Wang et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Tumor suppressive effects of WEE1 gene silencing could not enhance immunopotentiation effects of CD80 and 4-1BBL co-stimulation in human T cells

(2015) Mansooreh Jaberipour et al.   Journal of Cancer Research and Therapeutics

Phase I Study of Single-Agent AZD1775 (MK-1775), a Wee1 Kinase Inhibitor, in Patients With Refractory Solid Tumors

(2015) Khanh Do et al.   JOURNAL OF CLINICAL ONCOLOGY

Functional Genetic Screen Identifies Increased Sensitivity to WEE1 Inhibition in Cells with Defects in Fanconi Anemia and HR Pathways

(2015) M. Aarts et al.   MOLECULAR CANCER THERAPEUTICS

Homologous-recombination-deficient tumours are dependent on Polθ-mediated repair

(2015) Raphael Ceccaldi et al.   NATURE

Whole–genome characterization of chemoresistant ovarian cancer

(2015) Ann-Marie Patch et al.   NATURE

Targeting of Carbon Ion-Induced G2Checkpoint Activation in Lung Cancer Cells Using Wee-1 Inhibitor MK-1775

(2015) Hongyu Ma et al.   RADIATION RESEARCH

The role and mechanism of WEE1 on the cisplatin resistance reversal of the HepG2/DDP human hepatic cancer cell line

(2015) WEIFENG ZHAO et al.   Oncology Letters

Mdm2 inhibition confers protection of p53-proficient cells from the cytotoxic effects of Wee1 inhibitors

(2015) Yizhu Li et al.   Oncotarget

AZD1775 sensitizes T cell acute lymphoblastic leukemia cells to cytarabine by promoting apoptosis over DNA repair

(2015) James B. Ford et al.   Oncotarget

A subset of cancer cell lines is acutely sensitive to the Chk1 inhibitor MK-8776 as monotherapy due to CDK2 activation in S phase

(2015) Nandini Sakurikar et al.   Oncotarget

Genome-wide CRISPR-Cas9 Screens Reveal Loss of Redundancy between PKMYT1 and WEE1 in Glioblastoma Stem-like Cells

(2015) Chad M. Toledo et al.   Cell Reports

Sensitization of Pancreatic Cancers to Gemcitabine Chemoradiation by WEE1 Kinase Inhibition Depends on Homologous Recombination Repair

(2015) Tasneem Kausar et al.   NEOPLASIA

Combined inhibition of Chk1 and Wee1 as a new therapeutic strategy for mantle cell lymphoma

(2015) Rosaria Chilà et al.   Oncotarget

Genetic inhibition of the atypical kinase Wee1 selectively drives apoptosis of p53 inactive tumor cells

(2014) William N Pappano et al.   BMC CANCER

Abrogating G2/M checkpoint through WEE1 inhibition in combination with chemotherapy as a promising therapeutic approach for mesothelioma

(2014) Paola Indovina et al.   CANCER BIOLOGY & THERAPY

WEE1 Inhibition Alleviates Resistance to Immune Attack of Tumor Cells Undergoing Epithelial-Mesenchymal Transition

(2014) D. H. Hamilton et al.   CANCER RESEARCH

Combined Inhibition of Wee1 and PARP1/2 for Radiosensitization in Pancreatic Cancer

(2014) D. Karnak et al.   CLINICAL CANCER RESEARCH

Wee1 is a novel independent prognostic marker of poor survival in post-chemotherapy ovarian carcinoma effusions

(2014) Ana Slipicevic et al.   GYNECOLOGIC ONCOLOGY

Downmodulation of Tumor Suppressor p53 by T Cell Receptor Signaling Is Critical for Antigen-Specific CD4+ T Cell Responses

(2014) Masashi Watanabe et al.   IMMUNITY

A regimen combining the Wee1 inhibitor AZD1775 with HDAC inhibitors targets human acute myeloid leukemia cells harboring various genetic mutations

(2014) L Zhou et al.   LEUKEMIA

Integrated genomic analysis identifies the mitotic checkpoint kinase WEE1 as a novel therapeutic target in medulloblastoma

(2014) Peter S Harris et al.   Molecular Cancer

Wee-1 Kinase Inhibition Overcomes Cisplatin Resistance Associated with High-Risk TP53 Mutations in Head and Neck Cancer through Mitotic Arrest Followed by Senescence

(2014) A. A. Osman et al.   MOLECULAR CANCER THERAPEUTICS

WEE1 murine deficiency induces hyper-activation of APC/C and results in genomic instability and carcinogenesis

(2014) A Vassilopoulos et al.   ONCOGENE

Efficient Induction of Apoptosis by Wee1 Kinase Inhibition in Hepatocellular Carcinoma Cells

(2014) Tomomi Kogiso et al.   PLoS One

Pyrimidine-Based Tricyclic Molecules as Potent and Orally Efficacious Inhibitors of Wee1 Kinase

(2014) Yunsong Tong et al.   ACS Medicinal Chemistry Letters

High expression of wee1 is associated with malignancy in vulvar squamous cell carcinoma patients

(2013) Gry Irene Magnussen et al.   BMC CANCER

A Wee1 checkpoint inhibits anaphase onset

(2013) Noel Lianga et al.   JOURNAL OF CELL BIOLOGY

Etoposide Selectively Ablates Activated T Cells To Control the Immunoregulatory Disorder Hemophagocytic Lymphohistiocytosis

(2013) T. S. Johnson et al.   JOURNAL OF IMMUNOLOGY

Inhibition of Wee1 Sensitizes Cancer Cells to Antimetabolite Chemotherapeutics In Vitro and In Vivo, Independent of p53 Functionality

(2013) A. A. Van Linden et al.   MOLECULAR CANCER THERAPEUTICS

Preclinical Evaluation of the WEE1 Inhibitor MK-1775 as Single-Agent Anticancer Therapy

(2013) A. D. Guertin et al.   MOLECULAR CANCER THERAPEUTICS

Targeting Wee1 for the treatment of pediatric high-grade gliomas

(2013) Sabine Mueller et al.   NEURO-ONCOLOGY

Wee1 Inhibition by MK-1775 Leads to Tumor Inhibition and Enhances Efficacy of Gemcitabine in Human Sarcomas

(2013) Jenny M. Kreahling et al.   PLoS One

WEE1 tyrosine kinase, a novel epigenetic modifier

(2013) Kiran Mahajan et al.   TRENDS IN GENETICS

Combined inhibition of Wee1 and Hsp90 activates intrinsic apoptosis in cancer cells

(2012) Aki Iwai et al.   CELL CYCLE

Combined inhibition of Chk1 and Wee1: In vitro synergistic effect translates to tumor growth inhibition in vivo

(2012) Laura Carrassa et al.   CELL CYCLE

H2B Tyr37 phosphorylation suppresses expression of replication-dependent core histone genes

(2012) Kiran Mahajan et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

High Expression of Wee1 Is Associated with Poor Disease-Free Survival in Malignant Melanoma: Potential for Targeted Therapy

(2012) Gry Irene Magnussen et al.   PLoS One

Forced Mitotic Entry of S-Phase Cells as a Therapeutic Strategy Induced by Inhibition of WEE1

(2012) Marieke Aarts et al.   Cancer Discovery

WEE1 inhibition sensitizes osteosarcoma to radiotherapy

(2011) Jantine PosthumaDeBoer et al.   BMC CANCER

Therapeutic targeting of Chk1 in NSCLC stem cells during chemotherapy

(2011) M Bartucci et al.   CELL DEATH AND DIFFERENTIATION

MK-1775, a Potent Wee1 Inhibitor, Synergizes with Gemcitabine to Achieve Tumor Regressions, Selectively in p53-Deficient Pancreatic Cancer Xenografts

(2011) N. V. Rajeshkumar et al.   CLINICAL CANCER RESEARCH

WEE1 Kinase Targeting Combined with DNA-Damaging Cancer Therapy Catalyzes Mitotic Catastrophe

(2011) P. C. De Witt Hamer et al.   CLINICAL CANCER RESEARCH

MK-1775, a Novel Wee1 Kinase Inhibitor, Radiosensitizes p53-Defective Human Tumor Cells

(2011) K. A. Bridges et al.   CLINICAL CANCER RESEARCH

MK1775, a Selective Wee1 Inhibitor, Shows Single-Agent Antitumor Activity against Sarcoma Cells

(2011) J. M. Kreahling et al.   MOLECULAR CANCER THERAPEUTICS

Targeting Radiation-Induced G2 Checkpoint Activation with the Wee-1 Inhibitor MK-1775 in Glioblastoma Cell Lines

(2011) B. Sarcar et al.   MOLECULAR CANCER THERAPEUTICS

Navigating the kinome

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

Global Profiling of Signaling Networks: Study of Breast Cancer Stem Cells and Potential Regulation

(2011) H. Wang et al.   ONCOLOGIST

MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil

(2010) Hiroshi Hirai et al.   CANCER BIOLOGY & THERAPY

In Silico Analysis of Kinase Expression Identifies WEE1 as a Gatekeeper against Mitotic Catastrophe in Glioblastoma

(2010) Shahryar E. Mir et al.   CANCER CELL

Regulators of cyclin-dependent kinases are crucial for maintaining genome integrity in S phase

(2010) Halfdan Beck et al.   JOURNAL OF CELL BIOLOGY

The T-box transcription factor Brachyury promotes epithelial-mesenchymal transition in human tumor cells

(2010) Romaine I. Fernando et al.   JOURNAL OF CLINICAL INVESTIGATION

Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents

(2009) H. Hirai et al.   MOLECULAR CANCER THERAPEUTICS

The Cdc14B-Cdh1-Plk1 Axis Controls the G2 DNA-Damage-Response Checkpoint

(2008) Florian Bassermann et al.   CELL