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
A pathway linking translation stress to checkpoint kinase 2 signaling in Neurospora crassa
Sign Up to like & getrecommendations! Published in 2019 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.1815396116
Abstract: Significance Checkpoint kinase 2 (CHK-2) is a key component of the DNA damage response (DDR) pathway and its activation mechanism is evolutionarily conserved. We show that PERIOD-4 (PRD-4), the CHK-2 ortholog of Neurospora crassa, is… read more here.
Keywords: translation stress; kinase; prd; translation ... See more keywords
Adverse Cerebral Cardiovascular Events Associated With Checkpoint Kinase 1 Inhibitors: A Systemic Review.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of cardiovascular pharmacology"
DOI: 10.1097/fjc.0000000000000997
Abstract: ABSTRACT Checkpoint kinase 1 (CHK1) plays a broad role in regulating the cell cycle process and is involved in the pathogenesis of various malignant tumors. Preclinical and animal studies have shown that CHK1 inhibitors can… read more here.
Keywords: chk1 inhibitors; cardiovascular events; checkpoint kinase; cerebral cardiovascular ... See more keywords
Abstract 4090: Preclinical pharmacokinetics of CASC-578, a novel, selective, potent, and orally bioavailable small molecule checkpoint kinase 1 inhibitor
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-4090
Abstract: Introduction: Checkpoint kinase 1 (Chk1) is a serine/threonine protein kinase that regulates cell division in response to genotoxic stress by arresting cell cycle progression in the S & G2 phases. Pharmacological inhibition of Chk1 is… read more here.
Keywords: potent orally; 578 novel; casc 578; kinase ... See more keywords
Selectively Targeting Checkpoint Kinase By Prexasertib Had Potent Anti-Tumor Activity As Single Agent or Combined with Other Chemotherapeutic Drugs in Diffuse Large B-Cell Lymphoma, Especially Double Hit Lymphoma
Sign Up to like & getrecommendations! Published in 2018 at "Blood"
DOI: 10.1182/blood-2018-99-110282
Abstract: Background: Relapsed/Refractory diffuse large B-cell lymphoma (DLBCL) patients had a poor prognosis, especially those relapsing within 12 months of completion therapy. Clinically, there is a need to identify and target pathways associated with acquired treatment… read more here.
Keywords: lymphoma; dlbcl; prexasertib; checkpoint kinase ... See more keywords
The clinical and molecular characteristics of patients with personal or family history of gastrointestinal malignancies/polyposis and checkpoint kinase 2 (CHEK2) mutations.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2021.39.3_suppl.44
Abstract: 44Background: Checkpoint Kinase 2 (CHEK 2) encodes the protein CHK2, a serine/threonine kinase involved in pathways that conduct DNA repair as well as apoptosis in response to initial DNA damage. G... read more here.
Keywords: kinase; characteristics patients; checkpoint kinase; clinical molecular ... See more keywords
Chromosome 11q loss and MYCN amplification demonstrate synthetic lethality with checkpoint kinase 1 inhibition in neuroblastoma
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Oncology"
DOI: 10.3389/fonc.2022.929123
Abstract: Neuroblastoma is the most common extracranial solid tumor found in children and despite intense multi-modal therapeutic approaches, low overall survival rates of high-risk patients persist. Tumors with heterozygous loss of chromosome 11q and MYCN amplification… read more here.
Keywords: chromosome 11q; checkpoint kinase; loss; 11q loss ... See more keywords
Checkpoint Kinase 1 Is a Key Signal Transducer of DNA Damage in the Early Mammalian Cleavage Embryo
Sign Up to like & getrecommendations! Published in 2023 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms24076778
Abstract: After fertilization, remodeling of the oocyte and sperm genome is essential for the successful initiation of mitotic activity in the fertilized oocyte and subsequent proliferative activity of the early embryo. Despite the fact that the… read more here.
Keywords: cleavage; dna; checkpoint kinase; kinase key ... See more keywords
Effects of a checkpoint kinase inhibitor, AZD7762, on tumor suppression and bone remodeling
Sign Up to like & getrecommendations! Published in 2018 at "International Journal of Oncology"
DOI: 10.3892/ijo.2018.4481
Abstract: Chemotherapy for suppressing tumor growth and metastasis tends to induce various effects on other organs. Using AZD7762, an inhibitor of checkpoint kinase (Chk) 1 and 2, the present study examined its effect on mammary tumor… read more here.
Keywords: inhibitor; tumor cells; bone; checkpoint kinase ... See more keywords