Related Experiment Video
Updated: Jul 9, 2026
Chemotherapy-induced Vascular Toxicity - Real-time In vivo Imaging of Vessel Impairment
Published on: January 7, 2015
Molecular targets on blood vessels for cancer therapies in clinical trials
Masanori Sato1, Wadih Arap, Renata Pasqualini
1Department of Genitourinary Medical Oncology, The University of Texas, M D Anderson Cancer Center, Houston, Texas, USA.
Abstract:
This review covers progress to date in the identification of molecular targets on blood vessels in cancers, as well as agents that act on those targets, with emphasis on those currently in clinical trials. Current vascular-targeting therapies comprise two general types--antiangiogenic therapy and antivascular therapy. Advances in antiangiogenic therapies, particularly inhibitors of vascular endothelial growth factors and their receptors, have clarified the capacity of these inhibitors to change tumor-associated vessel structure to a more normal state, thereby improving the ability of chemotherapeutics to access the tumors. The responses of other antiangiogenesis target molecules in humans are more complicated; for example, alphanubeta3 integrins are known to stimulate as well as inhibit angiogenesis, and cleavage of various extracellular proteins/proteoglycans by matrix metalloproteinases produces potent regulators of the angiogenic process. Antivascular therapies disrupt established blood vessels in solid tumors and often involve the use of ligand-based or small-molecule agents. Ligand-based agents, irrespective of the antiangiogenic capacity of the ligand, target antivascular effectors to molecules expressed specifically on blood vessels, such as aminopeptidase N, fibronectin extra-domain B, and prostate-specific membrane antigen. Small-molecule antivascular agents, which are not targeted to molecules on blood vessels, rely on physical differences between the vasculatures in tumors and those in normal tissues.
Insights
This review details molecular targets on tumor blood vessels and therapies, focusing on agents in clinical trials. Vascular-targeting strategies include antiangiogenic and antivascular therapies to improve cancer treatment.
Area of Science:
- Oncology
- Vascular Biology
- Pharmacology
Background:
- Cancer blood vessels present unique molecular targets for therapeutic intervention.
- Vascular-targeting therapies aim to disrupt tumor vasculature or normalize it to enhance drug delivery.
- Significant progress has been made in identifying molecular targets and developing agents for clinical use.
Purpose of the Study:
- To review current progress in identifying molecular targets on tumor blood vessels.
- To summarize agents targeting these molecular sites, with an emphasis on clinical trials.
- To discuss the mechanisms and clinical applications of antiangiogenic and antivascular therapies.
Main Methods:
- Review of scientific literature on molecular targets and agents for vascular targeting in cancer.
- Analysis of data from ongoing and completed clinical trials of vascular-targeting therapies.
- Categorization of therapies into antiangiogenic and antivascular approaches.
Main Results:
- Antiangiogenic therapies, such as vascular endothelial growth factor inhibitors, can normalize tumor vasculature, improving chemotherapy efficacy.
- Target molecules like alphanubeta3 integrins and matrix metalloproteinases have complex roles in angiogenesis.
- Antivascular therapies utilize ligand-based agents targeting specific molecules (e.g., aminopeptidase N) or small molecules exploiting vascular differences.
Conclusions:
- Vascular-targeting therapies offer promising strategies for cancer treatment by targeting tumor neovasculature.
- Further research is needed to optimize the use of antiangiogenic and antivascular agents.
- Clinical trials are crucial for evaluating the safety and efficacy of novel vascular-targeting drugs.
More Related Videos
08:52Intravital Microscopy of Tumor-associated Vasculature Using Advanced Dorsal Skinfold Window Chambers on Transgenic Fluorescent Mice
Published on: January 19, 2018
10:27Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
Published on: July 25, 2020
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against specific...
02:57Targeted Cancer Therapies
There are several types of targeted therapies against specific...
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...
02:49Cancer Therapies
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
02:49Cancer Therapies
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
02:50Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...