Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition

Checkpoint kinase1 (CHK1) is an important biomarker in breast cancer having a role in chemotherapy response

(2015) M M Al-kaabi et al.   BRITISH JOURNAL OF CANCER

Randomized Phase II Trial of Gemcitabine Plus TH-302 Versus Gemcitabine in Patients With Advanced Pancreatic Cancer

(2015) Mitesh J. Borad et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase II Study of the Safety and Antitumor Activity of the Hypoxia-Activated Prodrug TH-302 in Combination With Doxorubicin in Patients With Advanced Soft Tissue Sarcoma

(2014) Sant P. Chawla et al.   JOURNAL OF CLINICAL ONCOLOGY

Dual Targeting of Hypoxia and Homologous Recombination Repair Dysfunction in Triple-Negative Breast Cancer

(2014) F. W. Hunter et al.   MOLECULAR CANCER THERAPEUTICS

CH-01 is a Hypoxia-Activated Prodrug That Sensitizes Cells to Hypoxia/Reoxygenation Through Inhibition of Chk1 and Aurora A

(2013) Cindy Cazares-Körner et al.   ACS Chemical Biology

Activity of the Hypoxia-Activated Prodrug, TH-302, in Preclinical Human Acute Myeloid Leukemia Models

(2013) S. Portwood et al.   CLINICAL CANCER RESEARCH

Identification of Preferred Chemotherapeutics for Combining with aCHK1Inhibitor

(2013) Yang Xiao et al.   MOLECULAR CANCER THERAPEUTICS

TH-302, a hypoxia-activated prodrug with broad in vivo preclinical combination therapy efficacy: optimization of dosing regimens and schedules

(2012) Qian Liu et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Discovery of Checkpoint Kinase Inhibitor (S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by Structure-Based Design and Optimization of Thiophenecarboxamide Ureas

(2012) Vibha Oza et al.   JOURNAL OF MEDICINAL CHEMISTRY

Homologous recombination repair-dependent cytotoxicity of the benzotriazine di-N-oxide CEN-209: Comparison with other hypoxia-activated prodrugs

(2011) Francis W. Hunter et al.   BIOCHEMICAL PHARMACOLOGY

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

Selective Tumor Hypoxia Targeting by Hypoxia-Activated Prodrug TH-302 Inhibits Tumor Growth in Preclinical Models of Cancer

(2011) J. D. Sun et al.   CLINICAL CANCER RESEARCH

Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of TH-302, a Hypoxia-Activated Prodrug, in Patients with Advanced Solid Malignancies

(2011) G. J. Weiss et al.   CLINICAL CANCER RESEARCH

Molecular and Cellular Pharmacology of the Hypoxia-Activated Prodrug TH-302

(2011) F. Meng et al.   MOLECULAR CANCER THERAPEUTICS

A Phase I Study of the Safety and Pharmacokinetics of the Hypoxia-Activated Prodrug TH-302 in Combination with Doxorubicin in Patients with Advanced Soft Tissue Sarcoma

(2011) Kristen N. Ganjoo et al.   ONCOLOGY

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

Drug Combination Studies and Their Synergy Quantification Using the Chou-Talalay Method

(2010) T.-C. Chou   CANCER RESEARCH

In vitro and In vivo Radiation Sensitization of Human Tumor Cells by a Novel Checkpoint Kinase Inhibitor, AZD7762

(2010) J. B. Mitchell et al.   CLINICAL CANCER RESEARCH

Death by releasing the breaks: CHK1 inhibitors as cancer therapeutics

(2010) Cynthia X. Ma et al.   TRENDS IN MOLECULAR MEDICINE

Checkpoint kinase inhibitors: a review of the patent literature

(2009) James W Janetka et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

ATR and Chk1 Suppress a Caspase-3–Dependent Apoptotic Response Following DNA Replication Stress

(2009) Katie Myers et al.   PLoS Genetics

Apoptosis induced by replication inhibitors in Chk1-depleted cells is dependent upon the helicase cofactor Cdc45

(2008) R Rodriguez et al.   CELL DEATH AND DIFFERENTIATION

Checkpoint Kinase 1 Down-Regulation by an Inducible Small Interfering RNA Expression System Sensitized In vivo Tumors to Treatment with 5-Fluorouracil

(2008) M. Ganzinelli et al.   CLINICAL CANCER RESEARCH

Potent and Highly Selective Hypoxia-Activated Achiral Phosphoramidate Mustards as Anticancer Drugs

(2008) Jian-Xin Duan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chk1 and Chk2 are differentially involved in homologous recombination repair and cell cycle arrest in response to DNA double-strand breaks induced by camptothecins

(2008) Min Huang et al.   MOLECULAR CANCER THERAPEUTICS

AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies

(2008) S. D. Zabludoff et al.   MOLECULAR CANCER THERAPEUTICS

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