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.