Medicinal-Pharmaceutical Chemistry Commons^™

Small Molecule Tyrosine Kinase Inhibitors Of Erbb2/Her2/Neu In The Treatment Of Aggressive Breast Cancer., Richard L. Schroeder, Cheryl L. Stevens, Jayalakshmi Sridhar

Faculty and Staff Publications

he human epidermal growth factor receptor 2 (HER2) is a member of the erbB class of tyrosine kinase receptors. These proteins are normally expressed at the surface of healthy cells and play critical roles in the signal transduction cascade in a myriad of biochemical pathways responsible for cell growth and differentiation. However, it is widely known that amplification and subsequent overexpression of the HER2 encoding oncogene results in unregulated cell proliferation in an aggressive form of breast cancer known as HER2-positive breast cancer. Existing therapies such as trastuzumab (Herceptin^®) and lapatinib (Tyverb/Tykerb^®), a monoclonal antibody inhibitor …