Applications of activatable probes in molecular imaging

Abstract

Most new drug candidates generated during in vitro screenings turn out to be invalid after time-consuming and costly testing in animal models. Therefore, development of noninvasive, real-time, sensitive, and cost-effective tools with higher throughput for monitoring and early detection of drug efficacy in vivo is urgently needed. Of such techniques, optical molecular imaging provides many advantages over other imaging modalities, including the use of non-radioactive materials, high sensitivity, and safe detection using readily available instruments at moderate cost. Performance of in vivo optical imaging is solely dependent on the development of sophisticated imaging probes that exhibit high sensitivity and low background noise. Among diverse applications, peptide-based molecular beacons, so called protease activatable optical probes, have enabled in vivo imaging of proteases activity and demonstrated promising results in the field of protease research and protease-targeted drug development. Matrix metalloproteinases (MMPs) are a family of Zn2+ dependent endopeptidase. It is highly expressed in most cancers, cardiovascular diseases and other diseases. Herein, we are using MMPs as targets to develop an ultra-sensitive activatable probe for throughput drug discovery application.