Functions and inhibitors of CHK1 in cancer therapy
2024年6月1日 · The novel Chk1 inhibitor MK-8776 sensitizes human leukemia cells to HDAC inhibitors by targeting the intra-S checkpoint and DNA replication and repair
CHK1 inhibition is synthetically lethal with loss of B-family DNA ...
Checkpoint kinase 1 (CHK1) is a key mediator of the DNA damage response that regulates cell cycle progression, DNA damage repair and DNA replication. Small-molecule CHK1 inhibitors sensitise cancer cells to genotoxic agents and have shown single ...
ATR/CHK1 inhibitors and cancer therapy - PubMed
ATR/CHK1 inhibitors have been developed and are currently used either as single agents or paired with radiotherapy or a variety of genotoxic chemotherapies in preclinical and clinical studies. Here, we review the status of the development of ATR and CHK1 inhibitors.
Reality CHEK: Understanding the biology and clinical potential of CHK1
2021年1月28日 · CHK1 inhibitor and PARPi combinations are undergoing rapid increases in both preclinical and clinical studies (Table 1). The ATR/CHK1 axis stabilizes replication forks, and senses and initiates ssDNA repair thereby preventing DSB generation and aberrant mitosis.
Roles of Chk1 in Cell Biology and Cancer Therapy - PMC
Under conventional idea, a Chk1 inhibitor is combined with chemotherapy to enhance the therapy effect. In the novel approach derived from our latest research results, constitutively activating Chk1 under normal growth condition is sufficient to …
Chk1 Inhibition as a novel therapeutic strategy for treating triple ...
This finding suggests that Chk1 inhibitors either as single agents or in combination chemotherapy represents a viable therapeutic option for the treatment of triple-negative breast cancer. pChk1 (S296) tumor expression levels could serve as a useful biomarker to stratify patients who might benefit from Chk1 inhibitor therapy.
A Phase 1/2 trial of SRA737 (a Chk1 inhibitor) administered
2023年4月29日 · SRA737 (Sierra Oncology, Inc., San Mateo, California, USA) is a novel orally bioavailable selective Chk1 inhibitor that has shown single-agent preclinical activity in MYC-amplified models of...
The cancer therapeutic potential of Chk1 inhibitors: how …
2013年4月18日 · Chk1 was initially recognized as a regulator of the G2/M checkpoint, but has since been demonstrated to have additional roles in replication fork stability, replication origin firing and homologous recombination. Inhibition of these pathways can dramatically sensitize cells to some antimetabolites.
CHK1 Inhibition Is Synthetically Lethal with Loss of B-Family DNA ...
2020年4月15日 · Small-molecule CHK1 inhibitors sensitize cancer cells to genotoxic agents and have shown single-agent preclinical activity in cancers with high levels of replication stress. However, the underlying genetic determinants of CHK1 inhibitor sensitivity remain unclear.
Chk1 inhibitors for novel cancer treatment - PubMed
This review discusses the rationale of Chk1 as an anticancer target, the structural basis for designing Chk1 inhibitors, and recently disclosed Chk1 inhibitors.
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