Related Experiment Video

Updated: Jun 9, 2026

Examining BCL-2 Family Function with Large Unilamellar Vesicles
08:35

Examining BCL-2 Family Function with Large Unilamellar Vesicles

Published on: October 5, 2012

Emerging Bcl-2 inhibitors for the treatment of cancer

Asfar S Azmi1, Zhiwei Wang, Philip A Philip

  • 1Wayne State University School of Medicine, 740 Hudson Webber Cancer Research Center, Barbara Ann Karmanos Cancer Institute, Department of Pathology, 4100 John R, Detroit, MI 48201, USA.

Expert Opinion on Emerging Drugs
|September 4, 2010
PubMed
Abstract

Insights

Small molecule inhibitors (SMI) targeting B-cell lymphoma 2 (Bcl-2) family proteins show promise for cancer therapy by overcoming chemoresistance. Ongoing research focuses on developing next-generation inhibitors for improved treatment strategies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Bcl-2 family proteins are crucial anti-apoptotic factors overexpressed in malignancies, contributing to chemoresistance.
  • Targeting these pro-survival proteins is a key strategy in cancer therapy research.

Purpose of the Study:

  • To review advancements in the design and synthesis of small molecule inhibitors (SMI) targeting pro-survival Bcl-2 proteins.
  • To discuss the clinical status and future directions of Bcl-2 family protein inhibitors.

Main Methods:

  • Comprehensive review of research over the past two decades.
  • Analysis of clinical trial data for Bcl-2 family protein SMIs.
  • Discussion of emerging insights and future research avenues.

Main Results:

  • Significant progress in the development of SMIs targeting Bcl-2 family proteins.
  • Emergence of novel inhibitor classes in Phase I and II clinical trials.
  • Demonstrated potential of SMI strategies in overcoming cancer chemoresistance.

Conclusions:

  • Targeting Bcl-2 family proteins with SMIs is a rapidly advancing and promising cancer therapy approach.
  • Next-generation inhibitors, including those targeting Mcl-1 and other apoptotic molecules, are under development.
  • SMI strategies hold potential to become a mainstay in future cancer treatment regimens.

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 specific...
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 specific...
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...
Treatment Resistent Cancers02:56

Treatment Resistent Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
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...
Treatment Resistant Cancers02:56

Treatment Resistant Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...