Target-based approach to inhibitors of histone arginine methyltransferases.

  title={Target-based approach to inhibitors of histone arginine methyltransferases.},
  author={Astrid Spannhoff and Ralf Heinke and Ingo Bauer and Patrick Trojer and Eric Metzger and Ronald Gust and Roland Sch{\"u}le and Gerald Brosch and Wolfgang Sippl and Manfred Jung},
  journal={Journal of medicinal chemistry},
  volume={50 10},
Lysine and arginine methyltransferases participate in the post-translational modification of histones and regulate key cellular functions. So far only one arginine methyltransferase inhibitor discovered by random screening was available. We present the first target-based approach to protein arginine methyltransferase (PRMT) inhibitors. Homology models of human and Aspergillus nidulans PRMT1 were generated from available X-ray structures of rat PRMTs. The NCI diversity set was filtered by a… CONTINUE READING

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