Related Experiment Video

Updated: Apr 12, 2026

Ookluc: A Plasmodium berghei Line for Identifying Transmission-blocking Compounds
07:14

Ookluc: A Plasmodium berghei Line for Identifying Transmission-blocking Compounds

Published on: July 11, 2025

631

The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents

Yan Shen, Shengsheng Qiang, Shutao Ma1

  • 1Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, China. mashutao@sdu.edu.cn.

Mini Reviews in Medicinal Chemistry
|May 13, 2015
PubMed

Insights

Farnesyltransferase (FTase) inhibitors show promise for treating cancer and malaria by targeting cell growth and parasitic infections. This review highlights their enzyme inhibitory activity, stability, and selectivity for future drug design.

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Parasitology

Background:

  • Cancer and malaria pose significant global health challenges, characterized by uncontrolled cell division and parasitic infection, respectively.
  • Farnesyltransferase (FTase), an isoprenyltransferase, plays a crucial role in Ras-processing, making it a viable therapeutic target for both diseases.
  • Despite extensive research, effective treatments for cancer and malaria remain a critical unmet medical need.

Purpose of the Study:

  • To review farnesyltransferase (FTase) inhibitors as potential anticancer and antimalarial agents.
  • To analyze the enzyme inhibitory activity, stability, and selectivity of reported FTase inhibitors.
  • To highlight promising novel FTase inhibitors and discuss design inspirations.

Main Methods:

  • Literature review of scientific publications on FTase inhibitors.
  • Analysis of reported data on enzyme inhibitory activity, stability, and selectivity.
  • Focus on inhibitors with demonstrated anticancer or antimalarial effects.

Main Results:

  • Numerous FTase inhibitors with anticancer and antimalarial activities have been identified.
  • Some FTase inhibitors are progressing through clinical development.
  • Key properties such as enzyme inhibitory activity, stability, and selectivity are crucial for therapeutic efficacy.

Conclusions:

  • FTase inhibitors represent a promising class of therapeutic agents for both cancer and malaria.
  • Further research into novel FTase inhibitors, focusing on design principles, is warranted.
  • Optimizing enzyme inhibitory activity, stability, and selectivity will be key to developing effective treatments.

More Related Videos

Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells13:38

Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells

Published on: January 18, 2017

12.8K
Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors10:29

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

2.7K

Related Concept Videos

Anthelminthic Agents01:15

Anthelminthic Agents

Anthelmintic drugs differ significantly from antiparasitic therapies targeting protozoa, primarily due to differences in parasite biology. Whereas most protozoal treatments act on proliferating cells, anthelmintics are typically directed against mature, nonproliferative helminths. The therapeutic approach considers the helminth's reliance on neuromuscular coordination, glucose metabolism, and microtubular integrity for survival, reproduction, and localization within the host. Most anthelmintics...
82
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
69
Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

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
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
2.9K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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...
9.2K
Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase01:27

Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase

Phase II biotransformation reactions are essential for detoxifying and eliminating xenobiotics, including many pharmaceutical compounds. These reactions typically involve conjugation, the covalent attachment of polar endogenous groups such as glucuronic acid, sulfate, methyl, or acetyl moieties to functional groups introduced during Phase I metabolism. The resulting conjugates are more water-soluble, enabling efficient renal or biliary excretion.The major classes of Phase II enzymes include...
74