A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity.

@article{Qiu2002ACR,
  title={A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity.},
  author={Wei Qiu and Robert L. Campbell and Anne Gangloff and Philippe Dupuis and Roch P Boivin and Martin R Tremblay and Donald Poirier and S Lin},
  journal={FASEB journal : official publication of the Federation of American Societies for Experimental Biology},
  year={2002},
  volume={16 13},
  pages={1829-31}
}
Human estrogenic 17beta-hydroxysteroid dehydrogenase (17beta-HSD type 1) catalyzes the final step in the synthesis of active estrogens that stimulate the proliferation of breast cancer cells. Based on the initial premise to make use of the binding energies of both the substrate and cofactor sites, and molecular modeling starting from the enzyme structure, several estradiol-adenosine hybrids were designed and synthesized. Among these hybrids, EM-1745 with a linker of 8-CH2 groups is proved to be… CONTINUE READING