Related Experiment Video

Updated: Apr 25, 2026

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
07:04

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology

Published on: May 2, 2025

1.3K

Small molecule Mcl-1 inhibitors for the treatment of cancer

Johannes Belmar1, Stephen W Fesik1

  • 1Department of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, TN 37232-0146, United States.

Pharmacology & Therapeutics
|August 31, 2014
PubMed

Insights

Myeloid cell leukemia 1 (Mcl-1) protein overexpression drives cancer growth and chemoresistance. This review details progress in developing small molecule inhibitors targeting Mcl-1 as a cancer therapy.

Area of Science:

  • Molecular Biology
  • Cancer Biology
  • Drug Discovery

Background:

  • The Bcl-2 protein family regulates apoptosis.
  • Myeloid cell leukemia 1 (Mcl-1) is a pro-survival protein.
  • Mcl-1 overexpression and gene amplification occur in numerous cancers, conferring resistance to chemotherapy.

Purpose of the Study:

  • To review the current advancements in the discovery of small molecule inhibitors targeting Mcl-1.
  • To highlight Mcl-1 as a significant therapeutic target in oncology.

Main Methods:

  • Literature review of scientific publications.
  • Analysis of preclinical and clinical studies on Mcl-1 inhibitors.

Main Results:

  • Mcl-1 is a validated cancer target due to its role in tumor survival and drug resistance.
  • Several classes of small molecule Mcl-1 inhibitors are under investigation.
  • Targeting Mcl-1 shows promise for overcoming therapeutic resistance.

Conclusions:

  • Small molecule inhibitors of Mcl-1 represent a promising strategy for cancer treatment.
  • Further development of Mcl-1 inhibitors is crucial for clinical application.
  • Targeting Mcl-1 could enhance the efficacy of existing chemotherapeutic agents.
Keywords:
BH3-mimeticInhibitorsMcl-1Myeloid cell leukemia-1Small molecule

More Related Videos

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics06:00

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics

Published on: May 14, 2016

10.8K
Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer06:51

Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer

Published on: July 21, 2018

18.9K

Related Concept Videos

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...
7.0K
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
4.8K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

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...
4.9K
Abnormal Proliferation02:23

Abnormal Proliferation

Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the...
4.0K
The Intrinsic Apoptotic Pathway01:31

The Intrinsic Apoptotic Pathway

Internal cellular stress, such as cellular injury or hypoxia, triggers intrinsic apoptosis. The B-cell lymphoma 2 (Bcl-2) family of proteins are the primary regulators of the intrinsic apoptotic pathway. For example, during DNA damage, checkpoint proteins, such as Ataxia Telangiectasia Mutated (ATM protein) and Checkpoints Factor-2 (Chk2) proteins, are activated. These proteins phosphorylate p53 which further activates pro-apoptotic proteins, such as Bax, Bak, PUMA, and Noxa, and inhibits...
6.1K
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...
2.2K