title: Androgen receptor antagonists for prostate cancer therapy.
abstract: Androgen deprivation is the mainstay therapy for metastatic prostate cancer (PCa). Another way of suppressing androgen receptor (AR) signaling is via AR antagonists or antiandrogens. Despite being frequently prescribed in clinical practice, there is conflicting evidence concerning the role of AR antagonists in the management of PCa. In the castration-resistant settings of PCa, docetaxel has been the only treatment option for decades. With recent evidence that castration-resistant PCa is far from AR-independent, there has been an increasing interest in developing new AR antagonists. This review gives a concise overview of the clinically available antiandrogens and the experimental AR antagonists that tackle androgen action with a different approach.
authors.affiliation: Laboratory of Molecular EndocrinologyDepartment of Cellular and Molecular Medicine, Katholieke Universiteit Leuven, Herestraat 49, B-3000 Leuven, BelgiumUrologyDepartment of Development and Regeneration, University Hospitals Leuven, Herestraat 49, 3000 Leuven, BelgiumLaboratory for Structural BioinformaticsCenter for Life Science Technologies, RIKEN, Yokohama, Japan.
authors.forename: Christine
authors.initials: C
authors.lastname: Helsen
authors.affiliation: Laboratory of Molecular EndocrinologyDepartment of Cellular and Molecular Medicine, Katholieke Universiteit Leuven, Herestraat 49, B-3000 Leuven, BelgiumUrologyDepartment of Development and Regeneration, University Hospitals Leuven, Herestraat 49, 3000 Leuven, BelgiumLaboratory for Structural BioinformaticsCenter for Life Science Technologies, RIKEN, Yokohama, JapanLaboratory of Molecular EndocrinologyDepartment of Cellular and Molecular Medicine, Katholieke Universiteit Leuven, Herestraat 49, B-3000 Leuven, BelgiumUrologyDepartment of Development and Regeneration, University Hospitals Leuven, Herestraat 49, 3000 Leuven, BelgiumLaboratory for Structural BioinformaticsCenter for Life Science Technologies, RIKEN, Yokohama, Japan.
authors.forename: Thomas
authors.initials: T
authors.lastname: Van den Broeck
authors.affiliation: Laboratory of Molecular EndocrinologyDepartment of Cellular and Molecular Medicine, Katholieke Universiteit Leuven, Herestraat 49, B-3000 Leuven, BelgiumUrologyDepartment of Development and Regeneration, University Hospitals Leuven, Herestraat 49, 3000 Leuven, BelgiumLaboratory for Structural BioinformaticsCenter for Life Science Technologies, RIKEN, Yokohama, Japan.
authors.forename: Arnout
authors.initials: A
authors.lastname: Voet
authors.affiliation: Laboratory of Molecular EndocrinologyDepartment of Cellular and Molecular Medicine, Katholieke Universiteit Leuven, Herestraat 49, B-3000 Leuven, BelgiumUrologyDepartment of Development and Regeneration, University Hospitals Leuven, Herestraat 49, 3000 Leuven, BelgiumLaboratory for Structural BioinformaticsCenter for Life Science Technologies, RIKEN, Yokohama, Japan.
authors.forename: Stefan
authors.initials: S
authors.lastname: Prekovic
authors.affiliation: Laboratory of Molecular EndocrinologyDepartment of Cellular and Molecular Medicine, Katholieke Universiteit Leuven, Herestraat 49, B-3000 Leuven, BelgiumUrologyDepartment of Development and Regeneration, University Hospitals Leuven, Herestraat 49, 3000 Leuven, BelgiumLaboratory for Structural BioinformaticsCenter for Life Science Technologies, RIKEN, Yokohama, Japan.
authors.forename: Hendrik
authors.initials: H
authors.lastname: Van Poppel
authors.affiliation: Laboratory of Molecular EndocrinologyDepartment of Cellular and Molecular Medicine, Katholieke Universiteit Leuven, Herestraat 49, B-3000 Leuven, BelgiumUrologyDepartment of Development and Regeneration, University Hospitals Leuven, Herestraat 49, 3000 Leuven, BelgiumLaboratory for Structural BioinformaticsCenter for Life Science Technologies, RIKEN, Yokohama, Japan.
authors.forename: Steven
authors.initials: S
authors.lastname: Joniau
authors.affiliation: Laboratory of Molecular EndocrinologyDepartment of Cellular and Molecular Medicine, Katholieke Universiteit Leuven, Herestraat 49, B-3000 Leuven, BelgiumUrologyDepartment of Development and Regeneration, University Hospitals Leuven, Herestraat 49, 3000 Leuven, BelgiumLaboratory for Structural BioinformaticsCenter for Life Science Technologies, RIKEN, Yokohama, Japan frank.claessens@med.kuleuven.be.
authors.forename: Frank
authors.initials: F
authors.lastname: Claessens
mesh_terms: D059002:Androgen Receptor Antagonists / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D002369:Castration; D006801:Humans; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D011944:Receptors, Androgen / Q000378:metabolism
chemical_list: D059002:Androgen Receptor Antagonists; D000970:Antineoplastic Agents; D011944:Receptors, Androgen
keywords: abiraterone; androgen receptor antagonist; antiandrogen; bicalutamide; enzalutamide; prostate cancer