Development of tubulin polymerization inhibitors as anticancer agents

Area of Science:

• Biochemistry
• Molecular Biology
• Pharmacology

Background:

• Microtubules, composed of α- and β-tubulin, are vital for cellular functions and are implicated in tumorigenesis.
• Inhibiting tubulin polymerization is a critical strategy for developing effective anticancer treatments.
• Tubulin is a highly promising target for drug discovery in cancer therapy.

Purpose of the Study:

• To review natural products and synthetic analogs as tubulin inhibitors.
• To examine the interaction sites of these inhibitors on tubulin.
• To cover novel tubulin inhibitors and patents from 2018-2023 for cancer treatment.

Main Methods:

• Literature search of scientific and patent databases (PubMed, Espacenet, ScienceDirect, Patent Guru).
• Focus on tubulin inhibitors, their mechanisms, and recent developments.
• Analysis of patents related to tubulin inhibition for cancer treatment (2018-2023).

Main Results:

• Identified natural products and synthetic compounds targeting tubulin polymerization.
• Highlighted the significance of colchicine-site binding inhibitors for overcoming drug resistance.
• Noted the potential of antibody-drug conjugates (ADCs) for tubulin inhibition in cancer therapy.

Conclusions:

• Tubulin remains a key target for anticancer drug development.
• Colchicine-site inhibitors offer a promising avenue due to their ability to bypass P-glycoprotein-mediated resistance.
• Novel strategies like ADCs show potential for advancing tubulin-targeted cancer therapies.