Novel mutations of androgen receptor: a possible mechanism of bicalutamide withdrawal syndrome.

Takahito Hara, Jun‐ichi Miyazaki, Hideo Araki, +4

PubMed

Molecular PharmacologyAndrogen ReceptorUrologyRefractory PcBicalutamide Withdrawal Syndrome +10

Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer

Tomohiro Kaku, Takenori Hitaka, Akio Ojida, +10

Bioorganic & Medicinal Chemistry

Medicinal ChemistrySelective 17,20-Lyase InhibitorPotential UtilityMedicinePharmacotherapy +7

Orteronel (TAK-700), a novel non-steroidal 17,20-lyase inhibitor: Effects on steroid synthesis in human and monkey adrenal cells and serum steroid levels in cynomolgus monkeys

Masuo Yamaoka, Takahito Hara, Takenori Hitaka, +7

The Journal of Steroid Biochemistry and Molecular Biology

Steroid SynthesisMedicinal ChemistryAdrenal GlandCynomolgus MonkeysEndocrine Mechanism +8

C17,20-lyase inhibitors. Part 2: Design, synthesis and structure–activity relationships of (2-naphthylmethyl)-1H-imidazoles as novel C17,20-lyase inhibitors

Nobuyuki Matsunaga, Tomohiro Kaku, Akio Ojida, +5

Bioorganic & Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryC17,20-lyase InhibitorsBiochemistryMedicine +7

Enhanced androgen receptor signaling correlates with the androgen-refractory growth in a newly established MDA PCa 2b-hr human prostate cancer cell subline.

Takahito Hara, Kazuyo Nakamura, Hideo Araki, +2

PubMed

Androgen-refractory GrowthUrologyMedicineHormonal ReceptorCancer Growth +10

C17,20-Lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors

Nobuyuki Matsunaga, Tomohiro Kaku, Fumio Itoh, +8

Bioorganic & Medicinal Chemistry

Molecular DockingC17,20-lyase InhibitorsC17,20-lyase Inhibitors I.Drug TargetBiochemistry +8

Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate

Katsuji Aikawa, Moriteru Asano, Koji Ono, +10

Bioorganic & Medicinal Chemistry

Medicinal ChemistryPart IiiMedicineAnabolic SteroidsDerivative 2F +11

A mutation in β‐tubulin and a sustained dependence on androgen receptor signalling in a newly established docetaxel‐resistant prostate cancer cell line

Takahito Hara, Kazutaka Ushio, Mayumi Nishiwaki, +6

Cell Biology International

Possible role of adaptive mutation in resistance to antiandrogen in prostate cancer cells

Takahito Hara, Jin Kouno, Kazuyo Nakamura, +2

The Prostate

Effect of a novel 17,20-lyase inhibitor, orteronel (TAK-700), on androgen synthesis in male rats

Takahito Hara, Jin Kouno, Tomohiro Kaku, +4

The Journal of Steroid Biochemistry and Molecular Biology

Molecular PharmacologyNovel 17,20-Lyase InhibitorEndocrine MechanismMedicineHormonal Receptor +9