Biology and medicinal chemistry approaches towards various apoptosis inducers

Vivek K Vyas1, Chetan Chintha, Mitul R Pandya

  • 1Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, S.G. Highway, Charodi, Ahmedabad 382 481, Gujarat, India. vicky_1744@yahoo.com

Insights

Apoptosis, a programmed cell death, is crucial for normal development and cancer control. Inducing apoptosis in cancer cells offers a promising therapeutic strategy.

Area of Science:

  • Cell Biology
  • Oncology

Background:

  • Apoptosis is a regulated cellular process essential for development and tissue homeostasis.
  • Dysregulation of apoptosis contributes to cancer development and progression.
  • Cancer cells often exhibit resistance to apoptosis, a key hallmark of malignancy.

Purpose of the Study:

  • To review the current understanding of apoptosis induction by various chemical agents.
  • To highlight the role of apoptosis-inducing agents as potential cancer therapeutics.

Main Methods:

  • Review of scientific literature on apoptosis and cancer therapy.
  • Discussion of chemical compounds and therapeutic approaches targeting apoptosis.

Main Results:

  • Apoptosis induction effectively controls tumor size and cell number.
  • Various therapeutic strategies, including small molecules and gene therapy, aim to induce apoptosis.
  • Resistance to apoptosis is a significant challenge in cancer treatment.

Conclusions:

  • Apoptosis-inducing agents represent a vital component in cancer treatment strategies.
  • Targeting key apoptosis regulatory mechanisms offers emerging opportunities for effective cancer therapy.

Related Concept Videos

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...
Apoptosis01:30

Apoptosis

Apoptosis is a combination of two Greek words, 'apo' and 'ptosis,' meaning separation and falling off, respectively. Hippocrates used this word to describe gangrene, which was caused due to bandaging of fractured bones. Apoptosis was distinguished from necrosis in 1970 when John Kerr reported observations of morphological changes occurring during apoptosis. During one experiment, he observed that the disruption of blood supply to the liver tissue resulted in a size reduction of the tissue.
The Extrinsic Apoptotic Pathway01:17

The Extrinsic Apoptotic Pathway

The extrinsic apoptotic pathway is initiated when extracellular death-inducing signals, such as specific cytokines, activate the death receptors expressed on the cell surface. The immune cells involved in this pathway are natural killer cells (NK cells) and cytotoxic T-lymphocytes. NK cells are critical in innate immune response, while cytotoxic T-lymphocytes are associated with adaptive immune response. These cells recognize specific receptors expressed on the altered cells and activate...
Cellular Injury V: Apoptosis and Autophagy01:22

Cellular Injury V: Apoptosis and Autophagy

Cells respond to damage and stress through highly coordinated processes that decide whether they survive or undergo controlled self-destruction. Two major pathways involved in this regulation are apoptosis, a type of programmed cell death, and autophagy, a survival mechanism that helps cells adapt to adverse conditions.ApoptosisApoptosis removes aged or injured cells to maintain tissue balance. During this process, the cell shrinks, chromatin condenses and fragments, and membrane-bound...
Caspases01:24

Caspases

Caspase, a family of cysteine proteases, serve as effectors in apoptosis. The ced3 gene in C.elegans was first identified to be involved in apoptosis. This gene encodes the ced-3 caspase that is similar to the interleukin-1-beta converting enzyme or ICE in mammals. In addition to apoptosis, caspases also function in the inflammatory response. Inflammatory caspases are essential in activating pro-inflammatory cytokines that recruit immune cells and block the replication of pathogens inside cells.
Overview of Cell Death01:30

Overview of Cell Death

Cell death is an essential process where the body gets rid of old or damaged cells. Cell proliferation and death need to be balanced, as an imbalance between the two may lead to cancer or autoimmune diseases.
Cell death was observed in the early 19th century, but there was no experimental evidence to prove it. In 1842, Carl Vogt first discovered cell death in a metamorphic toad; however, it was not termed ‘cell death.’ Scientists discovered different cell death pathways only in the 20th century...