This week in therapeutics

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Cancer

Cancer

Discoidin domain receptor tyrosine kinase 1 (DDR1)

Rat and in vitro studies identified inhibitors of DDR1 that could help treat cancer. In in vitro assays, compounds from a class of 3-(2-(pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides inhibited DDR1 with low nanomolar potency. In a panel of human cancer cell lines with high DDR1 expression, the lead molecules inhibited cell growth. In rats, the inhibitors showed high oral bioavailability and good pharmacokinetics. Next steps include studying the molecules in animal models of cancer.

SciBX 6(14); doi:10.1038/scibx.2013.333
Published online April 11, 2013

Patent application filed; available for licensing

Ding, K. et al. J. Med. Chem.; published online March 22, 2013;
doi:10.1021/jm301824k
Contact: Yong Xu, Chinese Academy of Sciences, Guangzhou, China
e-mail:
tu_zhengchao@gibh.ac.cn

Contact: Ke Ding, same affiliation as above
e-mail:
ding_ke@gibh.ac.cn