Nonpeptidic propargylamines as inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity.

@article{Schmitt2013NonpeptidicPA,
  title={Nonpeptidic propargylamines as inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity.},
  author={Martin L Schmitt and Alexander-Thomas Hauser and Luca Carlino and Martin Pippel and Johannes Schulz-Fincke and Eric Metzger and Dominica Willmann and Teresa T. Yiu and Michelle Barton and Roland Sch{\"u}le and Wolfgang Sippl and Manfred Jung},
  journal={Journal of medicinal chemistry},
  year={2013},
  volume={56 18},
  pages={7334-42}
}
Lysine demethylases play an important role in epigenetic regulation and thus in the development of diseases like cancer or neurodegenerative disorders. As the lysine specific demethylase 1 (LSD1/KDM1) has been strongly connected to androgen and estrogen dependent gene expression, it serves as a promising target for the therapy of hormone dependent cancer. Here, we report on the discovery of new small molecule inhibitors of LSD1 containing a propargylamine warhead, starting out from lysine… CONTINUE READING