Part III: Novel checkpoint kinase 2 (Chk2) inhibitors; design, synthesis and biological evaluation of pyrimidine-benzimidazole conjugates.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.01.072
Abstract: Recently a dramatic development of the cancer drug discovery has been shown in the field of targeted cancer therapy. Checkpoint kinase 2 (Chk2) inhibitors offer a promising approach to enhance the effectiveness of cancer chemotherapy.… read more here.
Keywords: checkpoint kinase; chk2; kinase chk2; chk2 inhibitors ... See more keywords
Inhibition of Chk2 promotes neuroprotection, axon regeneration, and functional recovery after CNS injury
Sign Up to like & getrecommendations! Published in 2022 at "Science Advances"
DOI: 10.1126/sciadv.abq2611
Abstract: DNA double-strand breaks occur in many acute and long-term neurological conditions, including neurodegeneration, neurotrauma, and stroke. Nonrepaired breaks chronically activate the DNA damage response in neurons, leading to neural dysfunction and apoptosis. Here, we show… read more here.
Keywords: chk2; inhibition chk2; chk2 promotes; functional recovery ... See more keywords
CHK2 overexpression and mislocalisation within mitotic structures enhances chromosomal instability and hepatocellular carcinoma progression
Sign Up to like & getrecommendations! Published in 2017 at "Gut"
DOI: 10.1136/gutjnl-2016-313114
Abstract: Objective Chromosomal instability (CIN) is the most common form of genomic instability, which promotes hepatocellular carcinoma (HCC) progression by enhancing tumour heterogeneity, drug resistance and immunity escape. CIN per se is an important factor of… read more here.
Keywords: hcc; progression; chk2; chromosomal instability ... See more keywords
DNA Damage Response Protein CHK2 Regulates Metabolism in Liver Cancer
Sign Up to like & getrecommendations! Published in 2021 at "Cancer Research"
DOI: 10.1158/0008-5472.can-20-3134
Abstract: This study uncovers a link between a central effector of DNA damage response, CHK2, and cellular metabolism, revealing potential therapeutic strategies for targeting hepatocellular carcinoma. Defective mitosis with chromosome missegregation can have a dramatic effect… read more here.
Keywords: chk2; damage; damage response; dna damage ... See more keywords
Computational analysis of high-risk SNPs in human CHK2 gene responsible for hereditary breast cancer: A functional and structural impact
Sign Up to like & getrecommendations! Published in 2019 at "PLoS ONE"
DOI: 10.1371/journal.pone.0220711
Abstract: Nowadays CHK2 mutation is studied frequently in hereditary breast and ovarian cancer patients in addition to BRCA1/BRCA2. CHK2 is a tumor suppressor gene that encodes a serine/threonine kinase, also involved in pathways such as DNA… read more here.
Keywords: risk; breast; chk2 gene; chk2 ... See more keywords
53BP1 regulates cell cycle arrest in esophageal cancer model.
Sign Up to like & getrecommendations! Published in 2019 at "European review for medical and pharmacological sciences"
DOI: 10.26355/eurrev_201901_16874
Abstract: OBJECTIVE This study aims to investigate effects of checkpoint kinase, mediator of DNA damage checkpoint 1 (MDC1) and p53-binding protein 1 (53BP1) silencing on p53, checkpoint kinase 1 and 2 (CHK1 and CHK2), and CHK2-T68… read more here.
Keywords: chk1 chk2; group; chk2; expression ... See more keywords
CHK2 Promotes Metabolic Stress-Induced Autophagy through ULK1 Phosphorylation
Sign Up to like & getrecommendations! Published in 2022 at "Antioxidants"
DOI: 10.3390/antiox11061166
Abstract: Reactive oxygen species (ROS) act as a signaling intermediate to promote cellular adaptation to maintain homeostasis by regulating autophagy during pathophysiological stress. However, the mechanism by which ROS promotes autophagy is still largely unknown. Here,… read more here.
Keywords: chk2; atm chk2; metabolic stress; stress induced ... See more keywords
Baicalein Induces G2/M Cell Cycle Arrest Associated with ROS Generation and CHK2 Activation in Highly Invasive Human Ovarian Cancer Cells
Sign Up to like & getrecommendations! Published in 2023 at "Molecules"
DOI: 10.3390/molecules28031039
Abstract: Ovarian cancer is a lethal gynecological cancer because drug resistance often results in treatment failure. The CHK2, a tumor suppressor, is considered to be an important molecular target in ovarian cancer due to its role… read more here.
Keywords: cancer cells; chk2; arrest; activation ... See more keywords
CHK2 is involved in the p53-independent radiosensitizing effects of valproic acid
Sign Up to like & getrecommendations! Published in 2017 at "Oncology Letters"
DOI: 10.3892/ol.2017.5792
Abstract: Radiotherapy is an effective treatment for the majority of types of localized solid cancer. However, the risk of side effects to the surrounding normal tissues limits radiotherapeutic approaches. Whilst the mechanism of action of valproic… read more here.
Keywords: radiosensitizing effects; effects valproic; present study; valproic acid ... See more keywords