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CDK inhibitors in cancer therapy, an overview of recent development
M Zhang, L Zhang, R Hei, X Li, H Cai… - American journal of …, 2021 - pmc.ncbi.nlm.nih.gov
Dysregulated cell division, which leads to aberrant cell proliferation, is one of the key
hallmarks of cancer. Therefore, therapeutic targets that block cell division would be effective …
hallmarks of cancer. Therefore, therapeutic targets that block cell division would be effective …
CDK7 inhibitors as anticancer drugs
Abstract Cyclin-dependent kinase 7 (CDK7), along with cyclin H and MAT1, forms the CDK-
activating complex (CAK), which directs progression through the cell cycle via T-loop …
activating complex (CAK), which directs progression through the cell cycle via T-loop …
High-resolution cryo-EM of the human CDK-activating kinase for structure-based drug design
Rational design of next-generation therapeutics can be facilitated by high-resolution
structures of drug targets bound to small-molecule inhibitors. However, application of …
structures of drug targets bound to small-molecule inhibitors. However, application of …
CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer
The MYC oncoproteins are thought to stimulate tumor cell growth and proliferation through
amplification of gene transcription, a mechanism that has thwarted most efforts to inhibit …
amplification of gene transcription, a mechanism that has thwarted most efforts to inhibit …
Targeting cell-cycle machinery in cancer
Abnormal activity of the core cell-cycle machinery is seen in essentially all tumor types and
represents a driving force of tumorigenesis. Recent studies revealed that cell-cycle proteins …
represents a driving force of tumorigenesis. Recent studies revealed that cell-cycle proteins …
RNA cytosine methylation and methyltransferases mediate chromatin organization and 5-azacytidine response and resistance in leukaemia
The roles of RNA 5-methylcytosine (RNA: m5C) and RNA: m5C methyltransferases (RCMTs)
in lineage-associated chromatin organization and drug response/resistance are unclear …
in lineage-associated chromatin organization and drug response/resistance are unclear …
[HTML][HTML] Development of a selective CDK7 covalent inhibitor reveals predominant cell-cycle phenotype
Summary Cyclin-dependent kinase 7 (CDK7) regulates both cell cycle and transcription, but
its precise role remains elusive. We previously described THZ1, a CDK7 inhibitor, which …
its precise role remains elusive. We previously described THZ1, a CDK7 inhibitor, which …
Genomic modelling of the ESR1 Y537S mutation for evaluating function and new therapeutic approaches for metastatic breast cancer
Drugs that inhibit estrogen receptor-α (ER) activity have been highly successful in treating
and reducing breast cancer progression in ER-positive disease. However, resistance to …
and reducing breast cancer progression in ER-positive disease. However, resistance to …
Quantifying CDK inhibitor selectivity in live cells
Concerted multidisciplinary efforts have led to the development of Cyclin-Dependent Kinase
inhibitors (CDKi's) as small molecule drugs and chemical probes of intracellular CDK …
inhibitors (CDKi's) as small molecule drugs and chemical probes of intracellular CDK …
ICEC0942, an orally bioavailable selective inhibitor of CDK7 for cancer treatment
Recent reports indicate that some cancer types are especially sensitive to transcription
inhibition, suggesting that targeting the transcriptional machinery provides new approaches …
inhibition, suggesting that targeting the transcriptional machinery provides new approaches …