title: [New generation of androgen receptor antagonist in castration resistant prostate cancer].
abstract: Androgen ablation therapy is performed for prostate cancer patients especially with advanced stage. Nevertheless, outgrowth of hormone independent cancer cells occurs within several years and leads to a lethal condition, so-called castration resistant prostate cancer (CRPC). Even in CRPC cells under low levels of serum androgens, androgen receptor (AR) signaling still functions and is engaged in the establishment of CRPC. Recently, novel AR antagonists have been developed such as enzalutamide or ARN-509. This review focuses on these AR antagonists that have some features including high affinity to AR compared with bicalutamide, preventing nuclear translocation and DNA binding. These new hormonal agents have changed the landscape of CRPC treatment with a promising outcome.
authors.forename: Hiroji
authors.initials: H
authors.lastname: Uemura
mesh_terms: D059002:Androgen Receptor Antagonists / Q000627:therapeutic use*; D004247:DNA / Q000378:metabolism; D006801:Humans; D008297:Male; D058990:Molecular Targeted Therapy; D064129:Prostatic Neoplasms, Castration-Resistant / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism; D011944:Receptors, Androgen / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects
chemical_list: C410798:AR protein, human; D059002:Androgen Receptor Antagonists; D011944:Receptors, Androgen; D004247:DNA