Induction of endomitosis-like event in HeLa cells following CHK1 inhibitor treatment.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2019.09.046
Abstract: The effects of CHK1 inhibitor on cell cycle kinetics have not been fully investigated yet. In this study, we closely analyzed this kinetics using a CHK1 inhibitor (PF00477736) in HeLa cells expressing fluorescent ubiquitination-based cell… read more here.
Keywords: endomitosis like; inhibitor; chk1 inhibitor; cell ... See more keywords
Excess histone H3 is a competitive Chk1 inhibitor that controls cell-cycle remodeling in the early Drosophila embryo
Sign Up to like & getrecommendations! Published in 2021 at "Current Biology"
DOI: 10.1016/j.cub.2021.03.035
Abstract: The DNA damage checkpoint is crucial to protect genome integrity.1,2 However, the early embryos of many metazoans sacrifice this safeguard to allow for rapid cleavage divisions that are required for speedy development. At the mid-blastula… read more here.
Keywords: chk1; chk1 inhibitor; drosophila embryo; cell cycle ... See more keywords
Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00994
Abstract: Checkpoint kinase 1 (CHK1) plays an important role in the DNA damage response pathway, being a potential anti-cancer drug target. In this study, we used a strategy for trifluoromethyl substitution to obtain orally bioavailable CHK1… read more here.
Keywords: chk1; orally bioavailable; amino; chk1 inhibitor ... See more keywords
Up-regulation of the PI3K/AKT and RHO/RAC/PAK signalling pathways in CHK1 inhibitor resistant Eµ-Myc lymphoma cells
Sign Up to like & getrecommendations! Published in 2022 at "Biochemical Journal"
DOI: 10.1042/bcj20220103
Abstract: The development of resistance and the activation of bypass pathway signalling represents a major problem for the clinical application of protein kinase inhibitors. While investigating the effect of either a c-Rel deletion or RelAT505A phosphosite… read more here.
Keywords: pi3k; inhibitor; chk1 inhibitor; myc ... See more keywords
Keeping RelApse in Chk: molecular mechanisms of Chk1 inhibitor resistance in lymphoma
Sign Up to like & getrecommendations! Published in 2022 at "Biochemical Journal"
DOI: 10.1042/bcj20220461
Abstract: Chk1 is a member of the DNA damage response pathway, whose loss leads to replication stress and genome instability. Because of its protective role against lethal levels of DNA replication stress, Chk1 has been studied… read more here.
Keywords: inhibitor resistance; mechanisms chk1; chk1; chk1 inhibitor ... See more keywords
A pan-cancer transcriptome analysis identifies replication fork and innate immunity genes as modifiers of response to the CHK1 inhibitor prexasertib
Sign Up to like & getrecommendations! Published in 2020 at "Oncotarget"
DOI: 10.18632/oncotarget.27400
Abstract: The combined influence of oncogenic drivers, genomic instability, and/or DNA damage repair deficiencies increases replication stress in cancer. Cells with high replication stress rely on the upregulation of checkpoints like those governed by CHK1 for… read more here.
Keywords: cancer; innate immunity; chk1 inhibitor; prexasertib ... See more keywords