SCFβ‐TrCP ubiquitinates CHK1 in an AMPK‐dependent manner in response to glucose deprivation
Sign Up to like & getrecommendations! Published in 2019 at "Molecular Oncology"
DOI: 10.1002/1878-0261.12403
Abstract: The ATR/CHK1 pathway is a key effector of cellular response to DNA damage and therefore is a critical regulator of genomic stability. While the ATR/CHK1 pathway is often inactivated by mutations, CHK1 itself is rarely… read more here.
Keywords: chk1; response glucose; glucose deprivation; deprivation ... See more keywords
Evaluation of CHK1 activation in vulvar squamous cell carcinoma and its potential as a therapeutic target in vitro
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Medicine"
DOI: 10.1002/cam4.1638
Abstract: CHK1 is an important regulator of the cell cycle and DNA damage response, and its altered expression has been identified in various tumors. Chk1 inhibitors are currently being evaluated as monotherapy and as potentiators of… read more here.
Keywords: chk1; pchk1ser317 pchk1ser296; pchk1ser296 pchk1ser280; vulvar squamous ... See more keywords
Chk1 activation attenuates sensitivity of lapatinib in HER2‐positive gastric cancer
Sign Up to like & getrecommendations! Published in 2018 at "Cell Biology International"
DOI: 10.1002/cbin.10922
Abstract: The ATM and Rad3‐related (ATR)/checkpoint kinase 1 (Chk1) pathway plays a pivotal role in DNA damage sensor and modulating homologous recombination. Recently, emerging evidence demonstrated that Chk1 phosphorylation was associated with chemotherapy and radiotherapy resistance.… read more here.
Keywords: chk1; positive gastric; her2 positive; gastric cancer ... See more keywords
Design, Synthesis, and Biological Evaluation of 2‐Aminothiazole Derivatives as Novel Checkpoint Kinase 1 (CHK1) Inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "ChemMedChem"
DOI: 10.1002/cmdc.202200664
Abstract: A series of 2‐aminothiazole derivatives were designed, synthesized on the basis of bioisosterism strategy and evaluated for their CHK1 inhibitory activity. Most of them exhibited potent CHK1 inhibition, and excellent antiproliferative activity against MV‐4‐11 and… read more here.
Keywords: design synthesis; chk1; kinase; activity ... See more keywords
Determination of CHK1 Cellular Localization by Immunofluorescence Microscopy.
Sign Up to like & getrecommendations! Published in 2021 at "Methods in molecular biology"
DOI: 10.1007/978-1-0716-1217-0_1
Abstract: Many proteins involved in the DNA damage pathway shuttle between the cytoplasm and nucleus, and their localizations are important for functions. In that regard, immunofluorescence microscopy has been widely used to delineate the temporal and… read more here.
Keywords: chk1; microscopy; cellular localization; immunofluorescence microscopy ... 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
PARP activity fine-tunes the DNA replication choreography of Chk1-depleted cells.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of molecular biology"
DOI: 10.1016/j.jmb.2021.166949
Abstract: Checkpoint Kinase 1 (Chk1) prevents DNA damage by adjusting the replication choreography in the face of replication stress. Chk1 depletion provokes slow and asymmetrical fork movement, yet the signals governing such changes remain unclear. We… read more here.
Keywords: chk1; replication choreography; fork; chk1 depleted ... See more keywords
An adaptor protein BmSte50 interacts with BmSte11 MAPKKK and is involved in host infection, conidiation, melanization, and sexual development in Bipolaris maydis
Sign Up to like & getrecommendations! Published in 2020 at "Mycoscience"
DOI: 10.1016/j.myc.2019.10.003
Abstract: Abstract A mitogen-activated protein kinase (MAPK) signaling pathway regulates specialized cellular responses to external stimuli. In Bipolaris maydis, a Chk1 MAPK orthologous to Fus3/Kss1 MAPKs of Saccharomyces cerevisiae is known to regulate various developmental processes,… read more here.
Keywords: chk1; chk1 cascade; bmste50; sexual development ... 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
Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1).
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01186
Abstract: Mutations in leucine-rich repeat kinase 2 (LRRK2), such as G2019S, are associated with an increased risk of developing Parkinson's disease. Surrogates for the LRRK2 kinase domain based on checkpoint kinase 1 (CHK1) mutants were designed,… read more here.
Keywords: chk1; leucine rich; kinase; lrrk2 inhibitors ... See more keywords
p53-NEIL1 co-abnormalities induce genomic instability and promote synthetic lethality with Chk1 inhibition in multiple myeloma having concomitant 17p13(del) and 1q21(gain)
Sign Up to like & getrecommendations! Published in 2022 at "Oncogene"
DOI: 10.1038/s41388-022-02227-8
Abstract: Recurrent cytogenetic abnormalities are the main hallmark of multiple myeloma (MM) and patients having 2 or more high-risk prognostic events are associated with extremely poor outcome. 17p13(del) and 1q21(gain) are critical and independent high-risk cytogenetic… read more here.
Keywords: 1q21 gain; 17p13 del; del 1q21; chk1 ... See more keywords