Title:An Overview of CDK Enzyme Inhibitors in Cancer Therapy
Volume: 23
Issue: 8
Author(s): Peddaguravagari Mounika, Bannimath Gurupadayya*, Honnavalli Yogish Kumar and Bannimath Namitha
Affiliation:
- Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS Academy of Higher Education & Research,
Mysuru, 570015, India
Keywords:
Cyclins, CDK, gene expression, cell cycle regulation, cancer, inhibition.
Abstract: The ability to address the cell cycle in cancer therapy brings up new medication development
possibilities. Cyclin-dependent kinases are a group of proteins that control the progression of the
cell cycle. The CDK/cyclin complexes are activated when specific CDK sites are phosphorylated. Because
of their non-selectivity and severe toxicity, most first-generation CDK inhibitors (also known as
pan-CDK inhibitors) have not been authorized for clinical usage. Despite this, significant progress has
been made in allowing pan-CDK inhibitors to be employed in clinical settings. Pan-CDK inhibitors'
toxicity and side effects have been lowered in recent years because of the introduction of combination
therapy techniques. As a result of this, pan-CDK inhibitors have regained a lot of clinical potential as a
combination therapy approach. The CDK family members have been introduced in this overview, and
their important roles in cell cycle control have been discussed. Then, we have described the current
state of CDK inhibitor research, with a focus on inhibitors other than CDK4/6. We have mentioned
first-generation pan-CDKIs, flavopiridol and roscovitine, as well as second-generation CDKIs, dinaciclib,
P276-00, AT7519, TG02, roniciclib, and RGB-286638, based on their research phases, clinical
trials, and cancer targeting. CDKIs are CDK4/6, CDK7, CDK9, and CDK12 inhibitors. Finally, we
have looked into the efficacy of CDK inhibitors and PD1/PDL1 antibodies when used together, which
could lead to the development of a viable cancer treatment strategy.
