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CDK4 and its closely related CDK6 play key roles in mammalian cell proliferation, they have ability to drive the progression of cells into the DNA synthetic (S) phase of the cell-division cycle, the enzymatic activities of CDK4 and CDK6 in the first gap phase (G1) of the cycle are governed by D-type cyclins expressed in response to various extracellular signals, including stimulatory mitogens, inhibitory cytokines, differentiation inducers, cell-cell contacts, and other spatial cues. More and more studies suggested that CDK4/6 regulated broad pathological processes, especially cancers through regulating cell cycle.
Cyclin-dependent kinase 4 (CDK4) also known as cell division protein kinase 4, is a member of the cyclin-dependent kinase family. It is an enzyme encoded by the CDK4 gene in human, which is catalytic subunit of the protein kinase complex and is important for cell cycle G1 phase progression.
Cell division protein kinase 6 (CDK6) is an enzyme encoded by the CDK6 gene, a member of member of the cyclin-dependent kinase family. It is regulated by Cyclin D proteins and Cyclin-dependent kinase inhibitor proteins. Just as the function of CDK4 on cell cycle, CDK6 is also a catalytic subunit of the protein kinase complex, important for the G1 phase progression and G1/S transition of the cell cycle. CDK6 participates in a positive feedback loop which activates transcription factors through a reaction cascade, where CDK6 and CDK4 act as a switch signal that first appears in G1, directing the cell towards S phase of the cell cycle.
CDK4 and CDK6 are important regulators of cell-cycle progression, whose enzymatic activity in the first gap phase (G1) of the cycle are governed by D-type cyclins expressed in response to various extracellular signals, such as stimulatory mitogens, inhibitory cytokines, differentiation inducers, cell-cell contacts, and others. Researches indicated that deletion of CDK4 or CDK6 has no significant effect on the survival of mice, while the deletion of both CDK4 and CDK6 leads to late embryonic lethality due to defective erythropoiesis. More studies suggested that CDK4 is crucial for pancreatic beta cells and pituitary glands, while CDK6 plays an important role in hematopoiesis.
Researches indicated that CDK4/6 has ability to phosphorylate the retinoblastoma protein priming it for inactivation by other CDKs later in G1, and releasing E2F transcription factors from the retinoblastoma protein constraint to allow their coordinate induction of a suite of genes whose activities are jointly required for initiation of S phase. Besides, in breast cancer cells and normal breast epithelium, the activity and expression of CDK4/6 and cyclin D is regulated by many mitogenic signaling pathways, such as the estrogen receptor, receptor tyrosine kinase (RTK) signaling pathways and the downstream PI3K-AKT-mTOR or RAS-RAF-MEK-ERK routes.
Approved Drugs
Palbociclib, ribociclib, abemaciclib, alvocidib, etc.
CDK4/6 Inhibitor
Palbociclib, ribociclib, abemaciclib, etc.
Neutropenia, thrombocytopenia, fatigue, diarrhea, anemia, and nausea.
Hormonal combinations CDK4/6 inhibitors in ER+ breast cancer
Palbociclib plus letrozole, palbociclib plus fulvestrant, abemaciclib plus fulvestrant, ribociclib plus LGX818 for BRAF-mutant melanoma
Ribociclib plus binimetinib for NRAS-mutant melanoma
CDK4/6 TestingCD BioSciences provides CDK4/6 testing services by Elisa, WB, IP, IHC or IF assay. The results of CDK4/6 testing are used to evaluate the activities of candidates against CDK4/6 or targeted diseases. You can choose one or more testing ways to detect the level of CDK4/6 according to your experiment.
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.
Antibody Drugs Development Services (show more)Antibody drugs exhibits many incomparable advantages, such as the high specificity, affinity, and efficiency, which is an emerging direction on targeted drug development.
CD BioSciences provides comprehensive services on CDK4/6 -targeted antibody drugs development with professional technology, extensive experience, and advanced equipment.
Pharmacological Experiments (show more)We will make a specific experimental plan according to your requirements, including but not limited to
Cancers Models Screening (show more)We will make specific cancer models to accelerate your targeted drug discovery project, including but not limited to
CD BioSciences will establish the specific cancer model according to your requirements to evaluation the inhibitory activity of your candidates targeted CDK4/6. We have various cell lines and the species of our animal models cover rats, mice, rabbits, dogs, and non-human primates.
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