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During the last few decades, many methods have been developed in order to facilitate the drug design and discovery phases. Most of these methods were devoted to find new chemical entities that provide the most meaningful interaction with the desired receptors or enzymes with the potential to have minimal unwanted interaction. However, this strategy is time consuming, costly and requires screening of thousands of molecules for biological activity of which only one might enter the drug market. One of the most attractive and promising method is the prodrug approach, in which the active drug molecule is masked by a promoiety to alter its undesired properties.It is concluded that These FR-targeted technologies can also pave the way for inspiring further sophisticated drug conjugates, especially as this receptor is being targeted by use of several complementary technologies: small molecule, nanoparticle and protein-based thus providing broad and distinct knowledge in the area.