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Published on: January 12, 2016
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.
Background:
The cancer is still a major cause of death worldwide. Among different targets to design anticancer agents, caspase-3 is an important target as its cleavage and activation lead to apoptosis and finally, cancer cell death. Apart from some naturally occurring molecules, many small molecules have been reported as caspase-3 activators.
Objectives:
In view of the above, the objective has been to review the published work on small molecules reported as caspase-3 activators and their anticancer activity to get some novel lead molecules for designing novel molecules of improved cancer therapeutic.
Methods:
Literature search has been carried out using different search engines like google, Elsevier, Science direct, RSC, etc. for the publications of small molecules as caspase-3 activators inducing apoptosis in cancer cells.
Results:
In this review, the small molecules showing caspase-3 cleavage and activation have been discussed under different broad chemical classes so as to provide some insight into the structural features responsible for caspase-3 activation leading to anticancer activity. The review also encompasses the established drugs, novel organometallics showing caspase-3 activation and anticancer activity.
Conclusion:
A large number of small molecules including some established drugs and organometallics have shown cleavage and activation of caspase-3 leading to apoptosis and anticancer activity. Many reported potent molecules of different chemical classes may be useful as lead molecules for optimization of anticancer activity as well as they may provide an insight of structural features which may be useful in designing novel caspase-3 activators as anticancer agents for drug development.
Insights
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.
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.
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