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pro vyhledávání: '"CHK1 Inhibitor MK-8776"'
Akademický článek
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Autor:
Woo-Chan Son, Seung Woo Chung, Hyo Won Chang, Youngro Byun, Gui Chul Kim, Foyez Mahmud, Seho Kweon, Jeong Uk Choi, Ji Won Kim, Hanul Lee, Sang Yoon Kim
Publikováno v:
Biomaterials. 182:35-43
Metronomic chemotherapy, which is defined as a low-dose and frequent administration of cytotoxic drugs without drug-free breaks, has been recently emerged as an alternative to traditional MTD therapy and has shown therapeutic benefit in breast cancer
Autor:
Jing-Quan Wang, Zhe-Sheng Chen, Dong-Hua Yang, Pranav Gupta, Ning Ji, Chao-Yun Cai, Xing-Duo Dong, Shuang Zhang, Yuqi Yang, Qingbin Cui
Publikováno v:
International Journal of Molecular Sciences
Volume 20
Issue 17
International Journal of Molecular Sciences, Vol 20, Iss 17, p 4095 (2019)
Volume 20
Issue 17
International Journal of Molecular Sciences, Vol 20, Iss 17, p 4095 (2019)
P-glycoprotein (P-gp), which is encoded by the ATP-binding cassette (ABC) transporter subfamily B member 1 (ABCB1) gene, is one of the most pivotal ABC transporters that transport its substrates across the cell membrane. Its overexpression is one of
Publikováno v:
Oncotarget
DNA damage activates Checkpoint kinase 1 (Chk1) to halt cell cycle progression thereby preventing further DNA replication and mitosis until the damage has been repaired. Consequently, Chk1 inhibitors have emerged as promising anticancer therapeutics
Autor:
Kerry Keertikar, Marc A. Labroli, Randall R. Rossman, Timothy J. Guzi, Michael P. Dwyer, Cory Poker
Publikováno v:
Tetrahedron Letters. 57:2601-2603
This Letter describes the development of a convergent, efficient route to the CHK1 inhibitor MK-8776. This synthetic approach relies upon the cyclization of a bispyrazole adduct 10 with a optically pure β-keto nitrile 9 to construct the pyrazolo[1,5
Autor:
Larry M. Karnitz, Mrinal M. Patnaik, Scott H. Kaufmann, Ivana Gojo, Jonathan Webster, Lawrence E. Morris, Amanda L. Blackford, Judith E. Karp, L. Austin Doyle, B. Douglas Smith, Lihua Wang, Raoul Tibes, Gary L. Rosner, Robert J. Kinders, Mark R. Litzow, Catherine J. Huntoon
Cytosine arabinoside (AraC) remains the backbone of most treatment regimens for acute myeloid leukemia (AML). Incorporation of AraC into DNA activates checkpoint kinase 1 (Chk1), leading to cell-cycle arrest and diminished AraC cytotoxicity, which ca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f59f0dae29b3c8ae532ad2068ee9e70
https://europepmc.org/articles/PMC5639924/
https://europepmc.org/articles/PMC5639924/
Autor:
Shao-jia Wang, Zhaozhi Yang, Xingxing Chen, Yan Feng, Xiaoli Yu, Jurui Luo, Xiaomao Guo, Li Zhang, Zhi-Rui Zhou
Publikováno v:
Acta Pharmacologica Sinica
MK-8776 is a recently described inhibitor that is highly selective for checkpoint kinase 1 (Chk1), which can weaken the DNA repair capacity in cancer cells to achieve chemo-sensitization. A number of studies show that MK-8776 enhances the cytotoxicit
Publikováno v:
BMC Cancer
Background Chk1 inhibitors have emerged as promising anticancer therapeutic agents particularly when combined with antimetabolites such as gemcitabine, cytarabine or hydroxyurea. Here, we address the importance of appropriate drug scheduling when gem
Interactions between the novel Chk1 inhibitor MK-8776 and the histone deacetylase (HDAC) inhibitor (HDACI) vorinostat were examined in human leukemia cells harboring wild-type (wt) or deficient p53. MK-8776 synergistically potentiated vorinostat-medi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49ccff20531e903421badc6d90d02b18
https://europepmc.org/articles/PMC3681875/
https://europepmc.org/articles/PMC3681875/
Autor:
Philip Kocienski
Publikováno v:
Synfacts. 12:0894-0894