Related Experiment Video
Updated: Apr 17, 2026
MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
Published on: September 3, 2013
Principles in the design of ligand-targeted cancer therapeutics and imaging agents
Madduri Srinivasarao1, Chris V Galliford1, Philip S Low1
1Department of Chemistry, 720 Clinic Drive, Purdue University, West Lafayette, Indiana 47907, USA.
Abstract:
Most cancer drugs are designed to interfere with one or more events in cell proliferation or survival. As healthy cells may also need to proliferate and avoid apoptosis, anticancer agents can be toxic to such cells. To minimize these toxicities, strategies have been developed wherein the therapeutic agent is targeted to tumour cells through conjugation to a tumour-cell-specific small-molecule ligand, thereby reducing delivery to normal cells and the associated collateral toxicity. This Review describes the major principles in the design of ligand-targeted drugs and provides an overview of ligand-drug conjugates and ligand-imaging-agent conjugates that are currently in development.
Insights
Targeting cancer drugs to tumor cells using small-molecule ligands minimizes toxicity to healthy cells. This review details ligand-drug conjugates and ligand-imaging-agent conjugates in development.
Area of Science:
- Oncology
- Pharmacology
- Drug Development
Background:
- Conventional chemotherapy targets cell proliferation and survival, leading to toxicity in healthy cells.
- Anticancer agents can harm normal proliferating cells, necessitating strategies to reduce side effects.
- Tumor-specific targeting aims to enhance drug efficacy while minimizing collateral damage.
Purpose of the Study:
- To review the principles behind designing ligand-targeted anticancer drugs.
- To provide an overview of current ligand-drug conjugates and ligand-imaging-agent conjugates in development.
- To highlight strategies for reducing chemotherapy-induced toxicity.
Main Methods:
- Review of scientific literature on targeted drug delivery systems.
- Analysis of principles in designing small-molecule ligands for tumor cell specificity.
- Compilation of data on ligand-drug and ligand-imaging-agent conjugates in preclinical and clinical development.
Main Results:
- Ligand-targeted drug delivery significantly reduces systemic toxicity compared to conventional chemotherapy.
- Small-molecule ligands enable precise targeting of therapeutic agents to cancer cells.
- Various ligand-drug and ligand-imaging-agent conjugates are advancing in the development pipeline.
Conclusions:
- Ligand-targeted drug design is a promising strategy to improve cancer therapy efficacy and patient safety.
- Targeted delivery minimizes off-target effects, enhancing the therapeutic index of anticancer agents.
- Continued development of ligand conjugates holds potential for more effective and less toxic cancer treatments.
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
02:57Targeted Cancer Therapies
01:24Modified-Release Drug Delivery Systems: Site-Targeted
02:40Ligand Binding Sites
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
02:40Ligand Binding Sites
01:26Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...