Drugging ATR: progress in the development of specific inhibitors for the treatment of cancer

Potentiation of tumor responses to DNA damaging therapy by the selective ATR inhibitor VX-970

(2015) Amy B. Hall et al.   Oncotarget

Identification of ATR-Chk1 Pathway Inhibitors That Selectively Target p53-Deficient Cells without Directly Suppressing ATR Catalytic Activity

(2014) M. Kawasumi et al.   CANCER RESEARCH

ATR Inhibitors VE-821 and VX-970 Sensitize Cancer Cells to Topoisomerase I Inhibitors by Disabling DNA Replication Initiation and Fork Elongation Responses

(2014) R. Josse et al.   CANCER RESEARCH

Phosphatidylinositol 3-Kinase (PI3K) and Phosphatidylinositol 3-Kinase-Related Kinase (PIKK) Inhibitors: Importance of the Morpholine Ring

(2014) Martin Andrs et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Synthetic Lethal Screen Reveals Enhanced Sensitivity to ATR Inhibitor Treatment in Mantle Cell Lymphoma with ATM Loss-of-Function

(2014) Daniel L. Menezes et al.   MOLECULAR CANCER RESEARCH

Development of pharmacodynamic biomarkers for ATR inhibitors

(2014) Tao Chen et al.   Molecular Oncology

General synthetic strategies towards N-alkyl sulfoximine building blocks for medicinal chemistry and the use of dimethylsulfoximine as a versatile precursor

(2014) Frederick W. Goldberg et al.   TETRAHEDRON

Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors

(2014) Paul A Barsanti et al.   ACS Medicinal Chemistry Letters

Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors

(2014) Paul A Barsanti et al.   ACS Medicinal Chemistry Letters

Sulfoximines: A Neglected Opportunity in Medicinal Chemistry

(2013) Ulrich Lücking   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Characterization of Torin2, an ATP-Competitive Inhibitor of mTOR, ATM, and ATR

(2013) Q. Liu et al.   CANCER RESEARCH

Targeting ATR in DNA damage response and cancer therapeutics

(2013) Emmanouil Fokas et al.   CANCER TREATMENT REVIEWS

Wee1 kinase as a target for cancer therapy

(2013) Khanh Do et al.   CELL CYCLE

The Lab Oddity Prevails: Discovery of Pan-CDK Inhibitor (R)-S-Cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY 1000394) for the Treatment of Cancer

(2013) Ulrich Lücking et al.   ChemMedChem

Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): A Potent and Selective Inhibitor of ATR Protein Kinase with Monotherapy in Vivo Antitumor Activity

(2013) Kevin M. Foote et al.   JOURNAL OF MEDICINAL CHEMISTRY

mTOR kinase structure, mechanism and regulation

(2013) Haijuan Yang et al.   NATURE

The ATM protein kinase: regulating the cellular response to genotoxic stress and more

(2013) Yosef Shiloh et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

ATM signalling and cancer

(2013) C A Cremona et al.   ONCOGENE

Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family

(2012) M. Raymond V. Finlay et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor

(2012) M. Raymond V. Finlay et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The novel ATR inhibitor VE-821 increases sensitivity of pancreatic cancer cells to radiation and chemotherapy

(2012) Remko Prevo et al.   CANCER BIOLOGY & THERAPY

Discovery of Novel Potent and Highly Selective Glycogen Synthase Kinase-3β (GSK3β) Inhibitors for Alzheimer’s Disease: Design, Synthesis, and Characterization of Pyrazines

(2012) Stefan Berg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation

(2012) E Fokas et al.   Cell Death & Disease

ATR signalling: more than meeting at the fork

(2011) Edward A. Nam et al.   BIOCHEMICAL JOURNAL

Phylogenomics of phosphoinositide lipid kinases: perspectives on the evolution of second messenger signaling and drug discovery

(2011) James R Brown et al.   BMC EVOLUTIONARY BIOLOGY

Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines

(2011) A Peasland et al.   BRITISH JOURNAL OF CANCER

Targeting the S and G2 checkpoint to treat cancer

(2011) Tao Chen et al.   DRUG DISCOVERY TODAY

Discovery of 9-(6-Aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a Potent, Selective, and Orally Available Mammalian Target of Rapamycin (mTOR) Inhibitor for Treatment of Cancer

(2011) Qingsong Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent and Selective Inhibitors of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Protein Kinase as Potential Anticancer Agents

(2011) Jean-Damien Charrier et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal–Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK)

(2011) J. Jean Cui et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR

(2011) Philip M Reaper et al.   Nature Chemical Biology

Exploiting oncogene-induced replicative stress for the selective killing of Myc-driven tumors

(2011) Matilde Murga et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations

(2011) Luis I Toledo et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Chemical methodology as a source of small-molecule checkpoint inhibitors and heat shock protein 70 (Hsp70) modulators

(2011) D. M. Huryn et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Combining ATR Suppression with Oncogenic Ras Synergistically Increases Genomic Instability, Causing Synthetic Lethality or Tumorigenesis in a Dosage-Dependent Manner

(2010) O. Gilad et al.   CANCER RESEARCH

The DNA-dependent protein kinase (DNA-PK): More than just a case of making ends meet?

(2010) Richard Hill et al.   CELL CYCLE

The DNA-damage response in human biology and disease

(2009) Stephen P. Jackson et al.   NATURE

Inhibition of ATR protein kinase activity by schisandrin B in DNA damage response

(2009) H. Nishida et al.   NUCLEIC ACIDS RESEARCH

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity

(2008) S.-M. Maira et al.   MOLECULAR CANCER THERAPEUTICS

ATR: an essential regulator of genome integrity

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