Article
The Effect of F877L and T878A Mutations on Androgen Receptor Response to Enzalutamide.
Molecular cancer therapeutics - 1 Jul 2016
Prekovic Stefan, van Royen Martin E, Voet Arnout R D, Geverts Bart, Houtman Rene, Melchers Diana, Zhang Kam Y J, Van den Broeck Thomas, Smeets Elien, Spans Lien, Houtsmuller Adriaan B, Joniau Steven, Claessens Frank, Helsen Christine
Abstract excerpt
Treatment-induced mutations in the ligand-binding domain of the androgen receptor (AR) are known to change antagonists into agonists. Recently, the F877L mutation has been described to convert enzalutamide into an agonist. This mutation was seen to co-occur in the endogenous AR allele of LNCaP cells, next to the T878A mutation. Here, we studied the effects of enzalutamide on the F877L and T878A mutants, as well...
Topics
- Amino Acid Substitution
- Androgen Antagonists
- Antineoplastic Agents
- Benzamides
- Cell Line, Tumor
- Cluster Analysis
- Codon
- Drug Resistance, Neoplasm
- Gene Expression Profiling
- Gene Expression Regulation, Neoplastic
- Humans
- Ligands