Related Experiment Video
Updated: Apr 13, 2026
14:20
Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
Published on: June 13, 2014
17.2K
Novel harmine derivatives for tumor targeted therapy
Siwen Li1, Aqin Wang1, Fan Gu1
1Department of Biomedical Engineering, State Key Laboratory of Natural Medicines, School of Life Science and Technology, China Pharmaceutical University, Arlington, TX, USA.
Oncotarget
|May 6, 2015
Summary
Researchers modified harmine, a natural compound, into targeted cancer therapies. New derivatives, 2DG-Har-01 and MET-Har-02, show improved efficacy and reduced toxicity for potential cancer treatment.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Oncology
Background:
- Harmine, a beta-carboline alkaloid from Peganum Harmala, has historical use as an anticancer folk medicine.
- Clinical use of harmine is hindered by low efficacy and significant neurotoxicity.
Purpose of the Study:
- To synthesize novel harmine derivatives with enhanced therapeutic efficacy and reduced systemic toxicity.
- To develop tumor-targeting agents for improved cancer therapy.
Main Methods:
- Synthesized two harmine derivatives, 2DG-Har-01 and MET-Har-02, by conjugating harmine with 2-amino-2-deoxy-D-glucose (2DG) and Methionine (Met) targeting groups.
- Evaluated the in vitro and in vivo therapeutic efficacy and toxicity of the synthesized compounds.
Main Results:
- Both 2DG-Har-01 and MET-Har-02 demonstrated significantly higher therapeutic effects compared to unmodified harmine.
- MET-Har-02 exhibited superior potency over 2DG-Har-01.
Conclusions:
- The novel harmine derivatives show promise for targeted cancer therapy.
- MET-Har-02 represents a potent candidate for further development in cancer treatment strategies.
Related Concept Videos
02:57Targeted Cancer Therapies
9.2K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
9.2K
02:57Targeted Cancer Therapies
1.8K
1.8K
02:50Combination Therapies and Personalized Medicine
6.4K
Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
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...
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...
6.4K
01:10Drugs that Destabilize Microtubules
4.3K
Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
4.3K
02:49Cancer Therapies
10.7K
Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
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...
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...
10.7K
01:26Targets for Drug Action: Overview
11.9K
Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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...
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...
11.9K