A CDC7-selective Inhibitor, TAK-931, suppresses homologous recombination repair activity to enhance antiproliferative activity of a PARP inhibitor
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چکیده
منابع مشابه
Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma.
The mitogen-activated protein kinase (MAPK) pathway is particularly important for the survival and proliferation of melanoma cells. Somatic mutations in BRAF and NRAS are frequently observed in melanoma. Recently, the BRAF inhibitors vemurafenib and dabrafenib have emerged as promising agents for the treatment of melanoma patients with BRAF-activating mutations. However, as BRAF inhibitors indu...
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A series of benzylamino inhibitors of acetylcholinesterase (AChE) have been designed based on a working hypothesis of the enzyme s active site. These compounds were tested for their inhibitory activities on AChE and potent inhibitors were further evaluated in terms of central selectivity. These studies led to a discovery of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4, 5-tetrahydro-1H-1-benzazep...
متن کاملFunctional ex vivo assay to select homologous recombination-deficient breast tumors for PARP inhibitor treatment.
PURPOSE Poly(ADP-ribose) polymerase (PARP) inhibitors are promising targeted treatment options for hereditary breast tumors with a homologous recombination (HR) deficiency caused by BRCA1 or BRCA2 mutations. However, the functional consequence of BRCA gene mutations is not always known and tumors can be HR deficient for other reasons than BRCA gene mutations. Therefore, we aimed to develop a fu...
متن کاملFunctional ex vivo assay to select Homologous Recombination deficient breast tumors for PARP inhibitor treatment Running title: Functional assay for PARP inhibitor treatment
Departments of Genetics, Pathology, Radiation Oncology, Medical Oncology and Cancer Genomics Center Netherlands, Erasmus University Medical Center, Rotterdam, The Netherlands Department of Clinical Genetics, VU University Medical Center, Amsterdam, The Netherlands Division of Molecular Pathology, Netherlands Cancer Institute, Amsterdam, The Netherlands Departments of Toxicogenetics and Human Ge...
متن کاملProgression through mitosis promotes PARP inhibitor-induced cytotoxicity in homologous recombination-deficient cancer cells
Mutations in homologous recombination (HR) genes BRCA1 and BRCA2 predispose to tumorigenesis. HR-deficient cancers are hypersensitive to Poly (ADP ribose)-polymerase (PARP) inhibitors, but can acquire resistance and relapse. Mechanistic understanding how PARP inhibition induces cytotoxicity in HR-deficient cancer cells is incomplete. Here we find PARP inhibition to compromise replication fork s...
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ژورنال
عنوان ژورنال: European Journal of Cancer
سال: 2020
ISSN: 0959-8049
DOI: 10.1016/s0959-8049(20)31167-9