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Editor-in-Chief: Natalia Ortúzar
Impact Factor: 2.968
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Online ISSN: 1860-7187
January 15, 2010
VIP: Upgrading a Natural Product: Inhibition of Human β-Tryptase by Cyclotheonamide Analogues
Norbert Schaschke* and Christian P. Sommerhoff
Although current asthma treatments have reached a high level of efficacy, there remains a need for new therapeutic strategies to help combat this serious health issue, which affects hundreds of millions of people globally. In this Communication, Schaschke and Sommerhoff describe their work with cyclotheonamide E4-based inhibitors of the β-tryptase, a promising new anti-inflammatory drug target. By implementing information derived from substrate specificity screening onto the cyclotheonamide E4 scaffold, highly potent and selective β-tryptase inhibitors were obtained.
Received November 24, 2009; published online January 13, 2010, DOI: 10.1002/cmdc.200900484.