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Related Concept Videos

Caspases01:24

Caspases

12.6K
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...
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The Intrinsic Apoptotic Pathway01:31

The Intrinsic Apoptotic Pathway

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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...
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The Extrinsic Apoptotic Pathway01:17

The Extrinsic Apoptotic Pathway

6.5K
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...
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Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

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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...
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Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

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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...
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Updated: Aug 8, 2025

Caspase-3 Activity in the Rat Amygdala Measured by Spectrofluorometry After Myocardial Infarction
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Caspase-3 Activity in the Rat Amygdala Measured by Spectrofluorometry After Myocardial Infarction

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Caspase-3 Activators as Anticancer Agents.

Nitin Srivastava1, Anil Kumar Saxena2

  • 1Department of Chemistry, Amity School of Applied Sciences, Amity University, Lucknow Campus, 226028, India.

Current Protein & Peptide Science
|February 27, 2023
PubMed
Summary
This summary is machine-generated.

Small molecules activating caspase-3 (a key protein in apoptosis) show promise as anticancer agents. This review highlights diverse chemical classes and structural features for developing novel cancer therapeutics.

Keywords:
BCRABL kinase.Caspase-3EGFRanticancer agentapoptosiscancer cellscaspase-3 activationcytochrome chemostasis

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Area of Science:

  • Medicinal Chemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • Cancer remains a leading global cause of mortality.
  • Caspase-3 activation is crucial for inducing apoptosis and cancer cell death.
  • Small molecules are being explored as potential caspase-3 activators for cancer therapy.

Approach:

  • Comprehensive literature search of scientific databases (Elsevier, Science Direct, RSC, Google).
  • Focus on small molecules reported as caspase-3 activators with demonstrated anticancer activity.
  • Categorization of molecules by chemical class to identify structure-activity relationships.

Key Points:

  • Numerous small molecules, including established drugs and novel organometallics, activate caspase-3.
  • These activators induce apoptosis, leading to anticancer effects.
  • Structural features contributing to caspase-3 activation and anticancer activity are discussed.

Conclusions:

  • A wide array of small molecules exhibit caspase-3 activation and anticancer properties.
  • These compounds serve as valuable lead molecules for developing improved cancer therapeutics.
  • Understanding structural features can guide the design of novel, potent caspase-3 activators.