Cancer Therapeutics

Research into cancer signalling has paved the way for the development of numerous , which act at different stages/sites in the cell-cycle to arrest/suppress signalling in cancer cells and induce cell death. Molecularly targeted drugs based on rational drug design have been developed to target and inhibit isolated genes or pathways crucial to the disease mechanism. Many of the earlier targeted therapeutics utilised cancer vaccines, siRNA and antisense oligonucleotides, however, novel therapies now employ monoclonal antibodies (MoAbs) and small-molecule protein-kinase inhibitors (SMPKIs), and have been more successful. MoAbs are bulky and target membrane-bound receptors and act through interfering with ligand-receptor interactions, complement-mediated cytotoxicity, immune modulation and antibody-dependent cellular toxicity. SMPKIs are dual specific and target both membrane-bound and internal targets via binding catalytic domains, allosteric binders, inactive kinase binding ligands, and ATP analogues. Because of the structural homology shared by many protein kinases, a single SMPKI can inhibit multiple protein kinases, which is quite advantageous in anticancer therapy.

Molecularly targeted drugs can be placed into several categories based on their mode of action and the specific disease mechanism targeted. Some of the major categories include (i) Aromatase inhibitors, block aromatase in oestrogen-sensitive breast cancer (Drugs: Anastrozole/Arimidex

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