P12 Chemical Biology for modulators targeting cancer microenvironment and cell membrane signaling
Monday, January 12, 2015
California Ballroom C and Santa Fe Room
Hideaki Kakeya1, Aya Yoshimura1, Ryosuke Sugiyama1, Shinji Kishimoto1, Shinichi Nishimura1, Akira Hattori1, Fumihiro Ishikawa1, Yusuke Yomoda1, Shan Lu1, Naohiro Katagiri1, Sayaka Shimada1, Eri Seto1, Hideaki Hayashi1, Nobuaki Takahashi1 and Hiroshi Harada2, (1)Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan, (2)Graduate School of Medicine, Kyoto University, Kyoto, Japan
Exploration of novel small molecules from natural sources such as microbial metabolites, medicinal plants, and marine invertebrates has contributed to the dicovery of not only lead molecules for drugs but also research tools on chemical biology. Chemial biology based on forward/reverse chemical genetics accerelates drug development and the functional analysis of genes and proteins. We have discovered several novel bioactive metabolites by both in vivo cell-based phenotypic screenings and in vitro target-oriented screenings, and investigated their modes of action using a chemical genetics or a chemical genomics approach.1)

In this conference, we present chemical genetics approaches for microbial metabolites targeting cancer microenvironmetnt and cell membrane signaling, as well as development of 5-SOxT probe for chemical tagging of a drug target using 5-sulfonyl tetrazole. 2)

1) URL:http://www.pharm.kyoto-u.ac.jp/sc-molsci/

2) a) Yoshimura, A. et al. J. Org. Chem. 79, 6858 (2014); b) Sugiyama, R. et al. J. Am. Chem. Soc. 136, 5209 (2014); c) Kishimoto, S. et al. Org. Lett. in press (2014); d) Ishikawa, F. et al. Bioorg. Med. Chem. Lett. 24, 865 (2014); e) Ostuki, S. et al. Bioorg. Med. Chem. Lett. 23, 1608 (2013).