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During the last three decades or so, many efforts have been made to study the protein cleavage sites by some disease-causing enzyme, such as HIV (Human Immunodeficiency Virus) protease and SARS (Severe Acute Respiratory Syndrome) coronavirus main proteinase. It has become increasingly clear via this mini-review that the motivation driving the aforementioned studies is quite wise, and that the results acquired through these studies are very rewarding, particularly for developing peptide drugs.