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Updated: Mar 24, 2026

A Flow Cytometry-Based Cell Surface Protein Binding Assay for Assessing Selectivity and Specificity of an Anticancer Aptamer
Published on: September 13, 2022
Small Molecules for Active Targeting in Cancer
Chin S Kue1, Anyanee Kamkaew2, Kevin Burgess2
1Department of Pharmacology, Faculty of Medicine, University of Malaya, 50603, Kuala Lumpur, Malaysia.
Abstract:
For the purpose of this review, active targeting in cancer research encompasses strategies wherein a ligand for a cell surface receptor expressed on tumor cells is used to deliver a cytotoxic or imaging cargo. This area of research is more than two decades old, but in those 20 and more years, how many receptors have been studied extensively? What kinds of the ligands are used for active targeting? Are they mostly naturally occurring molecules such as folic acid, or synthetic substances developed in campaigns for medicinal chemistry efforts? This review outlines the most important receptor or ligand combinations that have been used in active targeting to answer these questions, and therefore to address the most important one of all: is research in active targeting affording diminishing returns, or is this an area for which the potential far exceeds progress made so far?
Insights
Active targeting in cancer research uses ligands to deliver drugs to tumor cells. This review examines receptor-ligand pairs to assess if this field shows diminishing returns or holds untapped potential.
Area of Science:
- Oncology
- Pharmacology
- Biochemistry
Background:
- Active targeting in cancer research involves using ligands to bind cell surface receptors on tumor cells, delivering cytotoxic or imaging agents.
- This strategy has been explored for over two decades, necessitating an evaluation of its progress and future potential.
Purpose of the Study:
- To review extensively studied receptor-ligand combinations in active targeting for cancer therapy.
- To determine if the field of active targeting is yielding diminishing returns or if its potential is largely untapped.
Main Methods:
- Literature review of active targeting strategies in cancer research.
- Analysis of receptor-ligand pairs used for targeted delivery of therapeutic or imaging agents.
- Assessment of naturally occurring versus synthetic ligands in active targeting campaigns.
Main Results:
- Identified key receptor-ligand combinations that have been extensively studied in active targeting.
- Evaluated the types of ligands employed, distinguishing between naturally occurring molecules and synthetic compounds.
- Assessed the overall progress and return on investment in active targeting research.
Conclusions:
- The review provides insights into the efficacy and limitations of current active targeting strategies.
- Determines whether active targeting research is approaching saturation or offers significant future promise.
- Informs future research directions by highlighting successful and less fruitful receptor-ligand pairings.
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