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The Gordon Research Seminar on Proteolytic Enzymes and Their Inhibitors is a unique forum for graduate students, post-docs, and other scientists with comparable levels of experience and education to present and exchange new data and cutting edge ideas. The focus of this meeting is to highlight recent developments on the role of proteolytic enzymes and inhibitors in health and disease. Proteases are important mediators of signaling pathways crucial for normal physiology, and their activity is tightly controlled. Dysregulation results in a broad range of human pathologies, including cancer, atherosclerosis, stroke, and inflammatory diseases such as pancreatitis and colitis. Understanding how proteases are normally regulated, identifying their substrates, and defining their mechanistic contributions to disease are all essential requisites to developing efficacious therapies.