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Compound class: Synthetic organic
Comment: Dinaciclib is a potent cyclin-dependent kinase (CDK) inhibitor, inhibiting the CDK4 and 6 isoforms . Dinaciclib has also been reported to interact with the acetyl-lysine recognition domain of the bromodomain testis-specific protein BRDT . BRDT is a member of the BET family of bromodomain-containing proteins which are considered to be atypical kinases.
SARS-CoV-2: SARS-CoV-2 may regulate the host cell cycle to enhance viral replication, and in vitro phosphoproteomics analysis suggests that viral hijacking of the CDK signalling pathway may, at least in part, mediate this mechanism . Pharmacological inhibition of the CDK pathway with dinaciclib has anti-SARS-CoV-2 activity in two model cells lines, A549-ACE2 cells (IC50 32 nM) and Vero E6 cells (IC50 127 nM).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.|
|Summary of Clinical Use|
|A Phase 3 clinical trial in chronic lymphocytic leukemia (CLL) patients has been completed (see NCT01580228).|
|Mechanism Of Action and Pharmacodynamic Effects|
|The CDK4/6 pathway is key to regulating cell growth in many types of human cancer [1,7-8], such as genetic subtypes of non-small cell lung cancer (NSCLC, [3,7,9], melanoma, Mantle cell lymphoma (MCL), and ovarian and breast cancers [3-4]. Inhibiting this pathway prevents cell cycle transition from G1 to S phase, induces cell senescence and in some cases results in apoptosis .|