In this presentation, Prof. Zhang will describe his recent biochemical and genetic studies of oncogenic PTPs that yield new insights into the molecular basis that underlies the phosphatase-mediated tumorigenesis. He will also discuss several novel approaches for the acquisition of highly potent and selective PTP inhibitors with efficacious in vivo activity. Potent and specific PTP inhibitors could significantly facilitate functional analysis of the PTPs in complex cellular signal transduction pathways and may constitute valuable therapeutics for many human diseases.