Targeting cell cycle kinases and kinesins in anticancer drug development

Area of Science:

• Cell Biology
• Cancer Biology
• Pharmacology

Background:

• The cell cycle is tightly regulated by cyclin-dependent kinases (CDKs) and non-CDK kinases like Aurora and polo-like kinases, alongside checkpoint proteins.
• Mitotic kinesins are crucial for mitotic spindle assembly and function, also contributing to cell cycle regulation.
• Disruption of cell cycle control is a key characteristic of cancer development.

Purpose of the Study:

• To explore the therapeutic potential of inhibiting cell cycle regulators and mitotic kinesins in cancer treatment.
• To highlight the rationale behind developing inhibitors targeting kinases and kinesins due to their frequent upregulation in tumors.

Main Methods:

• Review of existing literature on cell cycle regulation, kinases, and mitotic kinesins in cancer.
• Analysis of the implications of genetic and epigenetic alterations leading to overexpression of these proteins in various tumor types.
• Examination of the current status of novel inhibitor compounds in clinical trials.

Main Results:

• Upregulation of cell cycle kinases and mitotic kinesins is observed across numerous cancer types.
• Inhibition of these targets presents a rational approach for selective targeting of malignant cells.
• Several novel inhibitor compounds are currently undergoing clinical evaluation.

Conclusions:

• Targeting cell cycle regulatory proteins and mitotic kinesins represents a promising avenue for novel cancer therapeutics.
• Despite challenges with potency and specificity, ongoing clinical trials indicate continued interest and progress in this therapeutic area.