Reality CHEK: Understanding the biology and clinical potential of CHK1

Participation of the ATR/CHK1 pathway in replicative stress targeted therapy of high-grade ovarian cancer

(2020) Patrycja Gralewska et al.   Journal of Hematology & Oncology

Exploring the Synergy between PARP and CHK1 Inhibition in Matched BRCA2 Mutant and Corrected Cells

(2020) Hannah L Smith et al.   Cancers

ATR signalling mediates the prosurvival function of phospho-NPM against PIDDosome mediated cell death

(2020) Disha Hiregange et al.   CELLULAR SIGNALLING

Checkpoint Kinase 1 Inhibition Enhances Cisplatin Cytotoxicity and Overcomes Cisplatin Resistance in SCLC by Promoting Mitotic Cell Death

(2019) Wei-Hsun Hsu et al.   Journal of Thoracic Oncology

Checkpoint kinase 1 is essential for fetal and adult hematopoiesis

(2019) Fabian Schuler et al.   EMBO REPORTS

SPRTN protease and checkpoint kinase 1 cross-activation loop safeguards DNA replication

(2019) Swagata Halder et al.   Nature Communications

Prexasertib, a checkpoint kinase inhibitor: from preclinical data to clinical development

(2019) Gesuino Angius et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

The CHK1 Inhibitor Prexasertib Exhibits Monotherapy Activity in High-Grade Serous Ovarian Cancer Models and Sensitizes to PARP Inhibition

(2019) Kalindi Parmar et al.   CLINICAL CANCER RESEARCH

Deubiquitinating enzyme USP3 controls CHK1 chromatin association and activation

(2018) Yu-Che Cheng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

SCFβ-TrCP ubiquitinates CHK1 in an AMPK-dependent manner in response to glucose deprivation

(2018) Ying Ma et al.   Molecular Oncology

Chk1 KA1 domain auto-phosphorylation stimulates biological activity and is linked to rapid proteasomal degradation

(2018) Eun-Yeung Gong et al.   Scientific Reports

Intramolecular autoinhibition of checkpoint kinase 1 is mediated by conserved basic motifs of the C-terminal kinase–associated 1 domain

(2017) Ryan P. Emptage et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Prexasertib, a cell cycle checkpoint kinases 1 and 2 inhibitor, increases in vitro toxicity of PARP inhibition by preventing Rad51 foci formation in BRCA wild type high-grade serous ovarian cancer

(2017) Ethan Brill et al.   Oncotarget

Chk1 Inhibitor SCH900776 Effectively Potentiates the Cytotoxic Effects of Platinum-Based Chemotherapeutic Drugs in Human Colon Cancer Cells

(2017) Jarmila Herůdková et al.   NEOPLASIA

Phase I Study of GDC-0425, a Checkpoint Kinase 1 Inhibitor, in Combination with Gemcitabine in Patients with Refractory Solid Tumors

(2016) Jeffrey R. Infante et al.   CLINICAL CANCER RESEARCH

Conformational Change of Human Checkpoint Kinase 1 (Chk1) Induced by DNA Damage

(2016) Xiangzi Han et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

CHK1 Inhibition Radiosensitizes Head and Neck Cancers to Paclitaxel-Based Chemoradiotherapy

(2016) H. E. Barker et al.   MOLECULAR CANCER THERAPEUTICS

CHK1 as a therapeutic target to bypass chemoresistance in AML

(2016) Laure David et al.   Science Signaling

CHK1 as a therapeutic target to bypass chemoresistance in AML

(2016) Laure David et al.   Science Signaling

ATM and ATR signaling at a glance

(2015) P. Awasthi et al.   JOURNAL OF CELL SCIENCE

Phase I Dose-Escalation Trial of Checkpoint Kinase 1 Inhibitor MK-8776 As Monotherapy and in Combination With Gemcitabine in Patients With Advanced Solid Tumors

(2015) Adil I. Daud et al.   JOURNAL OF CLINICAL ONCOLOGY

LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms

(2015) C. King et al.   MOLECULAR CANCER THERAPEUTICS

Biology of Poly(ADP-Ribose) Polymerases: The Factotums of Cell Maintenance

(2015) Peter Bai   MOLECULAR CELL

Interaction of Chk1 with Treslin Negatively Regulates the Initiation of Chromosomal DNA Replication

(2015) Cai Guo et al.   MOLECULAR CELL

ATM and ATR as therapeutic targets in cancer

(2015) Anika Maria Weber et al.   PHARMACOLOGY & THERAPEUTICS

The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma

(2015) Mike I. Walton et al.   Oncotarget

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

(2015) Rosaria Chilà et al.   Oncotarget

ATM-mediated stabilization of ZEB1 promotes DNA damage response and radioresistance through CHK1

(2014) Peijing Zhang et al.   NATURE CELL BIOLOGY

Roles of Chk1 in cell biology and cancer therapy

(2013) Youwei Zhang et al.   INTERNATIONAL JOURNAL OF CANCER

Pim kinases phosphorylate Chk1 and regulate its functions in acute myeloid leukemia

(2013) L L Yuan et al.   LEUKEMIA

Causes and consequences of replication stress

(2013) Michelle K. Zeman et al.   NATURE CELL BIOLOGY

Candidate tumor suppressor BTG3 maintains genomic stability by promoting Lys63-linked ubiquitination and activation of the checkpoint kinase CHK1

(2013) Y.-C. Cheng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A phase II study of UCN-01 in combination with irinotecan in patients with metastatic triple negative breast cancer

(2012) Cynthia X. Ma et al.   BREAST CANCER RESEARCH AND TREATMENT

Unique functions of CHK1 and WEE1 underlie synergistic anti-tumor activity upon pharmacologic inhibition

(2012) Amy D Guertin et al.   Cancer Cell International

Combination Therapy Targeting the Chk1 and Wee1 Kinases Shows Therapeutic Efficacy in Neuroblastoma

(2012) M. R. Russell et al.   CANCER RESEARCH

MYC Regulation of CHK1 and CHK2 Promotes Radioresistance in a Stem Cell-like Population of Nasopharyngeal Carcinoma Cells

(2012) W.-J. Wang et al.   CANCER RESEARCH

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

(2012) Laura Carrassa et al.   CELL CYCLE

CCT244747 Is a Novel Potent and Selective CHK1 Inhibitor with Oral Efficacy Alone and in Combination with Genotoxic Anticancer Drugs

(2012) M. I. Walton et al.   CLINICAL CANCER RESEARCH

Phase I and Pharmacologic Trial of Cytosine Arabinoside with the Selective Checkpoint 1 Inhibitor Sch 900776 in Refractory Acute Leukemias

(2012) J. E. Karp et al.   CLINICAL CANCER RESEARCH

CHK1 targets spleen tyrosine kinase (L) for proteolysis in hepatocellular carcinoma

(2012) Jian Hong et al.   JOURNAL OF CLINICAL INVESTIGATION

Targeting Chk1 in p53-deficient triple-negative breast cancer is therapeutically beneficial in human-in-mouse tumor models

(2012) Cynthia X. Ma et al.   JOURNAL OF CLINICAL INVESTIGATION

Discovery of 3-Alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as Selective, Orally Bioavailable CHK1 Inhibitors

(2012) Michael Lainchbury et al.   JOURNAL OF MEDICINAL CHEMISTRY

CRL4CDT2 Targets CHK1 for PCNA-Independent Destruction

(2012) J. Huh et al.   MOLECULAR AND CELLULAR BIOLOGY

P90 RSK arranges Chk1 in the nucleus for monitoring of genomic integrity during cell proliferation

(2012) Ping Li et al.   MOLECULAR BIOLOGY OF THE CELL

Synthetic lethality of Chk1 inhibition combined with p53 and/or p21 loss during a DNA damage response in normal and tumor cells

(2012) S Origanti et al.   ONCOGENE

Molecular Resistance Fingerprint of Pemetrexed and Platinum in a Long-Term Survivor of Mesothelioma

(2012) Oluf Dimitri Røe et al.   PLoS One

Therapeutic targeting of Chk1 in NSCLC stem cells during chemotherapy

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

Assessment of Chk1 Phosphorylation as a Pharmacodynamic Biomarker of Chk1 Inhibition

(2011) L. A. Parsels et al.   CLINICAL CANCER RESEARCH

ATM gene alterations in chronic lymphocytic leukemia patients induce a distinct gene expression profile and predict disease progression

(2011) A. Guarini et al.   HAEMATOLOGICA

Prolonged mitotic arrest triggers partial activation of apoptosis, resulting in DNA damage and p53 induction

(2011) James D. Orth et al.   MOLECULAR BIOLOGY OF THE CELL

Targeting the Replication Checkpoint Using SCH 900776, a Potent and Functionally Selective CHK1 Inhibitor Identified via High Content Screening

(2011) T. J. Guzi et al.   MOLECULAR CANCER THERAPEUTICS

Preclinical Development of the Novel Chk1 Inhibitor SCH900776 in Combination with DNA-Damaging Agents and Antimetabolites

(2011) R. Montano et al.   MOLECULAR CANCER THERAPEUTICS

ATM Mutations in Patients with Hereditary Pancreatic Cancer

(2011) Nicholas J. Roberts et al.   Cancer Discovery

Knockdown of Chk1 sensitizes human colon carcinoma HCT116 cells in a p53-dependent manner to lidamycin through abrogation of a G2/M checkpoint and induction of apoptosis

(2010) Yu Pan et al.   CANCER BIOLOGY & THERAPY

Loss of ATM/Chk2/p53 Pathway Components Accelerates Tumor Development and Contributes to Radiation Resistance in Gliomas

(2010) Massimo Squatrito et al.   CANCER CELL

Mechanism of Radiosensitization by the Chk1/2 Inhibitor AZD7762 Involves Abrogation of the G2Checkpoint and Inhibition of Homologous Recombinational DNA Repair

(2010) Meredith A. Morgan et al.   CANCER RESEARCH

New Insights into Checkpoint Kinase 1 in the DNA Damage Response Signaling Network

(2010) Y. Dai et al.   CLINICAL CANCER RESEARCH

14-3-3γ mediates Cdc25A proteolysis to block premature mitotic entry after DNA damage

(2010) Kousuke Kasahara et al.   EMBO JOURNAL

Chk1 Haploinsufficiency Results in Anemia and Defective Erythropoiesis

(2010) Nathan C. Boles et al.   PLoS One

Chk1 promotes replication fork progression by controlling replication initiation

(2010) E. Petermann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

DDB1 Targets Chk1 to the Cul4 E3 Ligase Complex in Normal Cycling Cells and in Cells Experiencing Replication Stress

(2009) V. Leung-Pineda et al.   CANCER RESEARCH

Gemcitabine sensitization by checkpoint kinase 1 inhibition correlates with inhibition of a Rad51 DNA damage response in pancreatic cancer cells

(2009) L. A. Parsels et al.   MOLECULAR CANCER THERAPEUTICS

The F Box Protein Fbx6 Regulates Chk1 Stability and Cellular Sensitivity to Replication Stress

(2009) You-Wei Zhang et al.   MOLECULAR CELL

NEK11 regulates CDC25A degradation and the IR-induced G2/M checkpoint

(2009) Marina Melixetian et al.   NATURE CELL BIOLOGY

G2 checkpoint abrogation and checkpoint kinase-1 targeting in the treatment of cancer

(2008) N Bucher et al.   BRITISH JOURNAL OF CANCER

Ataxia-telangiectasia: from a rare disorder to a paradigm for cell signalling and cancer

(2008) Martin F. Lavin   NATURE REVIEWS MOLECULAR CELL BIOLOGY

ATR: an essential regulator of genome integrity

(2008) Karlene A. Cimprich et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

The checkpoint kinases Chk1 and Chk2 regulate the functional associations between hBRCA2 and Rad51 in response to DNA damage

(2008) E M Bahassi et al.   ONCOGENE

Essential function of Chk1 can be uncoupled from DNA damage checkpoint and replication control

(2008) D. Wilsker et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA