Effective cancer therapy based on selective drug delivery into cells across their membrane using receptor-mediated...

Area of Science:

• Oncology
• Biotechnology
• Drug Delivery

Background:

• Cancer remains a leading global cause of death with significant unmet treatment needs.
• Current anti-cancer therapies face challenges including off-target effects, drug resistance, and poor tissue distribution.
• Receptor-mediated endocytosis (RME) presents a promising strategy to address these limitations.

Purpose of the Study:

• To review the potential and benefits of drug design and development utilizing RME for cancer therapy.
• To highlight how RME facilitates targeted drug delivery into cancer cells.

Main Methods:

• Utilizing specific cancer biomarkers (e.g., integrin, HER2, EGFR) overexpressed on cancer cells as targets.
• Employing ligands like cell-penetrating peptides (CPPs), tumor-homing peptides (THPs), and monoclonal antibodies (mAbs) to bind these receptors.
• Developing conjugates of ligands and drug payloads for RME, or using nanocarriers exploiting the enhanced permeability and retention (EPR) effect.

Main Results:

• RME enables targeted intracellular delivery of anti-cancer payloads via specific receptor binding.
• Ligand-payload conjugates and nanocarriers facilitate drug transport and subsequent release within cancer cells.
• Antibody drug conjugates (ADCs) leveraging RME are already established cancer treatments.

Conclusions:

• RME provides a powerful platform for developing advanced cancer therapeutics with improved targeting and efficacy.
• This approach holds significant promise for overcoming critical challenges in current cancer treatment strategies.
• Further drug design and development based on RME can lead to more effective cancer therapies.