Giovannetti E, Leon LG.
Curr Drug Targets. 2014;15(14):1261-2
Since 2005, improvements in our understanding of cancer biology have triggered the development of new class anti- cancer compounds targeting key pathways involved in tumor growth.
These new, rationally designed, drugs neutralize specific molecules or genes involved in the development of cancer, and have been appropriately called “targeted agents”. Most of these novel agents interact with receptors or signalling molecules, that play an essential role in cancer development and progression, and they can inhibit cancer cell growth, or induce apoptotic death. The development of these targeted agents responds to the fact that most currently used chemotherapy regimens for solid tumors reached an efficacy plateau, while causing severe toxic effects.
This issue describes the main pharmacological features of the most interesting compounds targeting specific signaling pathways ruled by the growth factor receptors EGFR and c-Met. These receptors are commonly expressed on tumor cells and are involved in the occurrence and spread of many tumor types through multiple effects on cell cycle, programmed cell death, and invasion. Remarkably, they use a highly overlapping repertoire of signaling adaptors and down- stream pathways, and are potential targets for different drugs.
Consequently, the present issue will provide the scientist working in basic research as well as clinicians a comprehensive overview of novel effective compounds interacting with EGFR and c-Met, with the aim of clarifying their development, pharmacology, resistance factors, and new strategies and applications, against major solid tumors.
Importantly, this pharmacological evaluation is accompanied by a deep description of the genetic heterogeneity of most cancer, as demonstrated using patient specimens before, during treatment or in the following disease stabilization or progression. With this information, these new therapeutic strategies are indeed expected to ameliorate the outcome of current anticancer treatments.