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Updated: Feb 17, 2026

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo
Published on: February 6, 2015
Overview on Anticancer Drug Design and Development
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Biruni University, Istanbul, Turkey.
Background:
Many impediments of current anti-cancer therapies have urged scientists to discover new agents. As a result of growing spectrums of new targets and strategies and recent biological and biotechnological progresses, many anti-cancer agents such as monoclonal antibodies, small molecule tyrosine kinase inhibitors and epigenetic drugs have been reached to clinical trials.
Objectives:
This review helps to understand the rationale for the development of inhibitors against major targets such as cell growth, proliferation, survival, angiogenesis and recent targets such as proteasome, heat shock proteins, and epigenetics.
Methods:
Recent approaches of the target-based anti-cancer drug developments were highlighted to giving some examples from approved agents. Many factors, such as metabolic change, hypoxia, cancer precursors and cancer resistant cells, and their effect on drug resistance mechanisms were discussed. The impacts of advanced computational techniques to identify targets of cancer and designing more selective inhibitors were explained.
Results:
Contributions of recent techniques such as a network analysis, the precise modes of action and computational methodologies especially simulation of bio-molecular processes to clarify targets, mechanism actions and reasons of lack of efficacy of anti-cancer drugs have been explained. The relationship between the several mechanisms and molecular design strategies has been discussed.
Conclusion:
This review provides an overview of important targets and design strategies of anti-cancer drugs, advantages and disadvantages of these methods and evaluation of some currently used anticancer targets in clinical studies.
Insights
Scientists are developing new anti-cancer drugs targeting key cellular processes and exploring novel strategies like epigenetics. This review examines current targets, drug design, and computational methods to overcome treatment challenges and improve efficacy.
Area of Science:
- Oncology
- Pharmacology
- Biotechnology
Background:
- Current anti-cancer therapies face significant challenges, driving the need for novel therapeutic agents.
- Advances in understanding cancer biology have led to new targets and strategies, including monoclonal antibodies, tyrosine kinase inhibitors, and epigenetic drugs entering clinical trials.
Purpose of the Study:
- To review the rationale behind developing inhibitors for major cancer targets (cell growth, proliferation, survival, angiogenesis) and emerging targets (proteasome, heat shock proteins, epigenetics).
- To discuss factors influencing drug resistance, such as metabolic changes, hypoxia, and cancer precursors.
- To explain the role of computational techniques in identifying cancer targets and designing selective inhibitors.
Main Methods:
- Highlighting recent target-based anti-cancer drug development approaches with examples of approved agents.
- Discussing factors contributing to drug resistance and their impact.
- Explaining the application of advanced computational techniques in target identification and inhibitor design.
Main Results:
- Recent techniques like network analysis and biomolecular simulations aid in clarifying targets, mechanisms of action, and reasons for drug inefficacy.
- The interplay between various anti-cancer mechanisms and molecular design strategies is explored.
- Computational methodologies are crucial for understanding drug efficacy and resistance.
Conclusions:
- This review summarizes key targets and design strategies for anti-cancer drugs.
- It evaluates the advantages and disadvantages of current anti-cancer methods and targets used in clinical studies.
- The findings provide insights into optimizing anti-cancer drug development and clinical application.
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