Related Experiment Video
Updated: Dec 20, 2025
09:57
System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
9.0K
MmpL3 inhibitors as antituberculosis drugs
Min Shao1, Matthew McNeil2, Gregory M Cook2
1International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou, 510632, China.
European Journal of Medicinal Chemistry
|May 25, 2020
Summary
Mycobacterial membrane protein Large 3 (MmpL3) is a promising drug target. Inhibiting MmpL3 weakens the cell wall, leading to bacterial death, with various compounds identified as MmpL3 inhibitors.
Area of Science:
- Microbiology
- Drug Discovery
- Structural Biology
Background:
- Mycobacterial outer membrane integrity relies on trehalose-monomycolates and mycolic acids.
- The mycobacterial membrane protein Large 3 (MmpL3) is crucial for transporting these essential precursors.
- MmpL3 is a validated drug target due to its essential role in mycobacterial survival.
Purpose of the Study:
- To review the current development of MmpL3 inhibitors.
- To discuss the therapeutic potential of targeting MmpL3.
- To highlight challenges in developing MmpL3-targeting drugs.
Main Methods:
- High-throughput whole-cell screening.
- Whole genome sequencing of resistant mutants.
- Analysis of identified MmpL3 inhibitor classes.
Main Results:
- Numerous compound classes targeting MmpL3 have been identified through screening and resistance studies.
- Inhibition of MmpL3 effectively weakens the mycobacterial cell wall.
- MmpL3 inhibition leads to cell death in both in vitro and in vivo models.
Conclusions:
- MmpL3 is a validated and therapeutically relevant drug target for mycobacterial infections.
- Ongoing research is identifying diverse MmpL3 inhibitors with therapeutic potential.
- Challenges in MmpL3 inhibitor development require further investigation.
Related Concept Videos
01:28Pulmonary Tuberculosis V
465
Medical management of tuberculosis (TB) patients involves a comprehensive approach that includes diagnosis, treatment, and monitoring. The specific strategies can vary depending on the type of tuberculosis (latent or active), the patient's overall health status, and other considerations.
Latent tuberculosis infection occurs when TB bacteria are present in a person's body, but are not causing illness or symptoms. It is not contagious, and preventive treatment is crucial to avoid the...
Latent tuberculosis infection occurs when TB bacteria are present in a person's body, but are not causing illness or symptoms. It is not contagious, and preventive treatment is crucial to avoid the...
465
01:31Pulmonary Tuberculosis III
795
Tuberculosis (TB) is a contagious infection primarily affecting the lung parenchyma but which can also affect other body parts. TB can be classified based on disease development, presentation, and the affected anatomical site.
The first classification is based on the development of the disease, and it includes the following categories:
The first classification is based on the development of the disease, and it includes the following categories:
795
01:26Pulmonary Tuberculosis IV
423
Tuberculosis, more commonly referred to as TB, is an infectious disease stemming from Mycobacterium tuberculosis. While it primarily impacts the lungs, TB can also affect other body areas. Given its severity and global impact, timely and accurate diagnosis is crucial for controlling its spread and improving patient outcomes.
Several diagnostic approaches are used to detect TB. The conventional method is the Tuberculin Skin Test (TST), also known as the Mantoux test. However, this method has...
Several diagnostic approaches are used to detect TB. The conventional method is the Tuberculin Skin Test (TST), also known as the Mantoux test. However, this method has...
423
01:29Pulmonary Tuberculosis I
741
Tuberculosis, often called TB, is a contagious illness primarily caused by Mycobacterium tuberculosis. It mainly affects the lung parenchyma but can also impact other body parts.
Causative Organism
The primary infectious agent causing tuberculosis is Mycobacterium tuberculosis, a slow-growing, acid-fast, aerobic rod that exhibits sensitivity to heat and ultraviolet light. Instances of Mycobacterium bovis and Mycobacterium avium contributing to the development of TB infection are rare.
Mode of...
Causative Organism
The primary infectious agent causing tuberculosis is Mycobacterium tuberculosis, a slow-growing, acid-fast, aerobic rod that exhibits sensitivity to heat and ultraviolet light. Instances of Mycobacterium bovis and Mycobacterium avium contributing to the development of TB infection are rare.
Mode of...
741
01:28Pulmonary Tuberculosis II
1.2K
Tuberculosis, or TB, is a bacterial infectious disease caused by Mycobacterium tuberculosis. While its primary impact is on the lungs, leading to pulmonary tuberculosis, it can also affect various other organs, a condition referred to as extrapulmonary tuberculosis.
Here is a detailed explanation of its pathophysiology:
Transmission: The process begins when a person inhales droplet nuclei containing M. tuberculosis. These are typically released into the air when an individual with pulmonary or...
Here is a detailed explanation of its pathophysiology:
Transmission: The process begins when a person inhales droplet nuclei containing M. tuberculosis. These are typically released into the air when an individual with pulmonary or...
1.2K
01:15Drugs that Stabilize Microtubules
2.5K
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...
2.5K