Reactome | AR binds AR antagonists

AR binds AR antagonists

Stable Identifier

R-HSA-9706837

Type

Reaction [binding]

Species

Homo sapiens

Compartment

cytosol

ReviewStatus

5/5

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The actions of androgens on the androgen receptors(AR) can potentiate the growth and survival of prostate cancer cells. AR antagonist drugs can competitively inhibit androgens from binding to AR, inhibit AR nuclear translocation, as well as AR-mediated transcription which can all result in a decrease in prostate cancer cell proliferation and tumour size (Furr & Tucker 1996, Hodgson et al. 2007, Tran et al. 2009, Fizazi et al. 2018, Fizazi et al. 2015, Clegg et al. 2012). Androgens can also contribute to the development of androgen-dependent conditions such as acne and alopecia. Clascoterone blocks the effects of androgens that bind AR to treat these conditions (Rosette et al. 2019 , Herbert et al. 2020).

Literature References

PubMed ID	Title	Journal	Year
26313416	ODM-201: a new-generation androgen receptor inhibitor in castration-resistant prostate cancer Loriot, Y, Massard, C, Fizazi, K, Albiges, L	Expert Rev Anticancer Ther	2015
8560673	The preclinical development of bicalutamide: pharmacodynamics and mechanism of action Tucker, H, Furr, BJ	Urology	1996
32320027	Efficacy and Safety of Topical Clascoterone Cream, 1%, for Treatment in Patients With Facial Acne: Two Phase 3 Randomized Clinical Trials Thiboutot, D, Gerloni, M, Stein Gold, L, Hebert, A, Fragasso, E, Cartwright, M, Mazzetti, A	JAMA Dermatol	2020
17804755	Activity of androgen receptor antagonist bicalutamide in prostate cancer cells is independent of NCoR and SMRT corepressors Balk, SP, Hodgson, MC, Astapova, I, Hollenberg, AN	Cancer Res	2007
30197098	Clinical Development of Darolutamide: A Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer Fizazi, K, Tombal, B, Smith, MR	Clin Genitourin Cancer	2018
31141847	Cortexolone 17α-propionate (Clascoterone) Is a Novel Androgen Receptor Antagonist that Inhibits Production of Lipids and Inflammatory Cytokines from Sebocytes In Vitro Agan, FJ, Gerloni, M, Moro, L, Mazzetti, A, Rosette, C	J Drugs Dermatol	2019
19359544	Development of a second-generation antiandrogen for treatment of advanced prostate cancer Tran, C, Ouk, S, Wasielewska, T, Sawyers, CL, Scher, HI, Arora, V, Kwon, A, Jung, ME, Welsbie, D, Smith-Jones, PM, Wongvipat, J, Chen, CD, Higano, CS, Beer, TM, Chen, Y, Yoo, D, Watson, PA, Clegg, NJ, Hung, DT	Science	2009
22266222	ARN-509: a novel antiandrogen for prostate cancer treatment Tran, C, Klang, M, Wu, N, Wasielewska, T, Joseph, JD, Grillot, K, Sawyers, CL, Darimont, B, Jung, ME, Smith, ND, Bonnefous, C, Cai, L, Zhao, H, Chen, Y, Ouerfelli, O, Smith-Jones, P, Dorow, S, Sensintaffar, J, Ouk, S, Rix, PJ, Hager, JH, Bischoff, ED, Scher, HI, Arora, V, Cao, C, Qian, J, Shao, G, Dilhas, A, Wongvipat, J, Yang, G, Herbert, MR, Heyman, RA, Aparicio, A, Clegg, NJ, de Stanchina, E	Cancer Res	2012