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CDK1-Targeted Drug Discovery Services

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.

Whatever information you want about CDK1 targeted drug discovery, you can find it here. For more details or related services, please feel free to contact us.

What is CDK1?

What is CDK1?

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.

The structure of CDK1
Fig 1. The structure of CDK1
How CDK1 Work?

How CDK1 Work?

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.

How CDK1 Work
How CDK1 Work
Direction of Drug Discovery Based on CDK1

Direction of Drug Discovery Based on CDK1

  • RNA Polymerase ii Carboxy-Terminal Domain Kinase Activity
  • Developing New Clinical Effects on CDK1 from Existing Drugs
Direction of Drug Discovery Based on CDK1
The Drugs Targeting CDK1

The Drugs Targeting CDK1

Classification of Drug Status

Approved Drugs
Fostamatinib, etc.
Drugs in Development
Alsterpaullone, hymenialdisine, indirubin-3'-monoxime, olomoucine, etc.

Classification of Mechanism of Action

RNA Polymerase ii Carboxy-Terminal Domain Kinase Activity
Fostamatinib, alsterpaullone, hymenialdisine, etc.

The Most Common Side Effects

The Most Common Side Effects

Fostamatinib exhibited embryo-fetal mortality or developmental abnormalities at exposures of 0.3-10 times the maximum recommended human dose.

What We Offer

CDK1 Testing CDK1 Testing

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.

Hit Identification Hit Identification (show more)

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.

  • High-Throughput Screening
  • CDK1-Targeted in Silico Virtual Screening
  • Fragment-Based Screening
  • High-Content Screening

Pharmacological Experiment Pharmacological Experiments (show more)

We will make a specific experimental plan according to your requirements, including but not limited to

  • Pharmacokinetics / Pharmacodynamics
  • Pharmacokinetics
  • Pharmacodynamics
  • Safety Pharmacology

Disease Models Screening Disease Models Screening (show more)

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.

Inquire Us Inquire Us

References

  1. Xie, B.; et al. Cyclin b1/cdk1-regulated mitochondrial bioenergetics in cell cycle progression and tumor resistance. Cancer Lett. 2019, 443(p.56-66.
  2. Benanti, J.A. Create, activate, destroy, repeat: Cdk1 controls proliferation by limiting transcription factor activity. Curr Genet. 2016, 62(2): p.271-6.
  3. Odle, R.I.; et al. Cdk1, the other 'master regulator' of autophagy. Trends Cell Biol. 2021, 31(2): p.95-107.
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