• Yasuo Tsutsumi.
• Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Osaka University, Suita 565-0871, Japan. ytsutsumi@nihs.go.jp
• Yakugaku Zasshi. 2004 Nov 1;124(11):769-80.

AbstractWith the success of the Human Genome Project, the focus of life science research has shifted to the functional and structural analyses of proteins, such as proteomics and structural genomics. These novel approaches to the analysis of proteins, including newly identified ones, are expected to help in the identification and development of protein therapies for various diseases. Thus pharmacoproteomic-based drug discovery currently has a very high profile. Nevertheless, the use of bioactive proteins in the clinical setting is not straightforward because in vivo these proteins have low stability and pleiotropic action. To promote pharmacoproteomic-based drug discovery and development, we have attempted to establish a system for creating functional mutant proteins (muteins) with the desired properties and to develop a site-specific bioconjugation system for further improving their therapeutic potency. These innovative protein-drug systems are discussed in this review.

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