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Development of 5N-Bicalutamide, a High-Affinity Reversible Covalent Antiandrogen.

Felipe de Jesus Cortez1, Phuong Nguyen2, Charles Truillet3

  • 1Department of Pharmaceutical Chemistry, University of California San Francisco , 600 16th Street, San Francisco, California 94158, United States.

ACS Chemical Biology
|October 6, 2017
PubMed
Summary

A new antiandrogen, 5N-bicalutamide, forms a covalent bond with a specific cysteine residue in the androgen receptor, significantly improving efficacy and potentially overcoming resistance in advanced prostate cancer treatment.

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