CDK1 is a member of the cyclin-dependent kinases family. It exhibits broad function on regulating cell cycle for cell proliferation and organ development. The deletion of CDK1 in mice embryos cause the embryos death. Besides, phosphorylation of CDK1 has a crucial effect on mitotic progression, for example, incomplete DNA synthesis may lead to stabilization of this phosphorylation, preventing mitotic progression. However, there are more details on CDK1 need researchers to explore.
Cyclin-dependent kinase 1 (CDK1) is a highly conserved protein that functions as a serine/threonine kinase. It is a main regulator for cell cycle. Binding to its cyclin partners, CDK1 phosphorylation is initiated, thereby leads to cell cycle progression. CDK1 is the most critical cell cycle element for cell proliferation and organ development. Relative studies indicated that mice embryos deleting CDK2, CDK3, CDK4 and CDK6 are still able to undergo organogenesis, while organogenesis did not occur without CDK1. CDK1 can bind to different cyclins and is sufficient to regulate all the steps required for cell division. Cyclin B1 and its catalytic partner CDK1, also known as the mitotic promoting factor, belong to the fundamental kinase machinery regulating the progression from G2 to mitosis. Under normal growth conditions, mitochondrial localization of cyclin B1/CDK1 is attenuated during G1 phase due to a lack of cyclin B1 accumulation.
Forkhead protein Hcm1 is a transcriptional activator in coordinating gene expression with cell-cycle events. It controls the expression of genes that are transcribed during S-phase, while Hcm1 activity is regulated by CDK1. CDK1 phosphorylation both stimulates Hcm1 activity, by promoting its recruitment to target gene promoters, and inactivates it, by targeting it for ubiqutin-mediated degradation. Besides, CDK1 regulates cell cycle transcription factors and control activity of an individual transcription factor (activation or degradation) to coordinate cell cycle. CDK1 is the most critical cell cycle element for cell proliferation and organ development. CDK1 is involved not only in mitochondrial dynamics, but also in mitochondrial protein influx and bioenergetics, targeting CDK1 initiates mitochondria-initiated apoptosis.
Approved Drugs
Fostamatinib, etc.
Drugs in Development
Alsterpaullone, hymenialdisine, indirubin-3'-monoxime, olomoucine, etc.
RNA Polymerase ii Carboxy-Terminal Domain Kinase Activity
Fostamatinib, alsterpaullone, hymenialdisine, etc.
Fostamatinib exhibited embryo-fetal mortality or developmental abnormalities at exposures of 0.3-10 times the maximum recommended human dose.
CD BioSciences provides CDK1 testing services by Elisa, WB, IP, or IF assay. The results of CDK1 testing are used to evaluate the activities of candidates against CDK1 or targeted diseases. You can choose one or more testing ways to detect the level of CDK1 according to your experiment.
The goal of early drug discovery is to find novel lead compounds that have the desired potency, selectivity, and ADMET properties for pre-clinical evaluation.
CD BioSciences offers hit identification services to make your find targeted compounds more successful and faster.
We will make a specific experimental plan according to your requirements, including but not limited to
CD BioSciences will establish the specific disease model according to your requirements to evaluate the inhibitory activity of your candidates targeted CDK1. We have various cell lines and the species of our animal models cover rats, mice, rabbits, dogs, and non-human primates.