Reactome | AR binds AR agonists

AR binds AR agonists

Stable Identifier

R-HSA-9705926

Type

Reaction [binding]

Species

Homo sapiens

Compartment

cytosol

ReviewStatus

5/5

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Endogenous androgens such as testosterone and dihydrotestosterone are steroid hormones that regulate the development and maintenance of male characteristics in vertebrates through their binding to the androgen receptor (AR) (Tóth & Zakár 1982, Askew et al. 2007, Brinkmann 2011). They are synthesised from cholesterol in the testes, ovaries and the adrenal glands. Synthetic androgen agonists (AR agonists) are used in androgen replacement therapy to counter the effects of male hypogonadism (diminished functional activity of the gonads) (Rey & Grinspon 2020), to help with menopausal symptoms (Marina et al. 2020), in delayed puberty, the prophylactic treatment of hereditary angioedema (Bork 2018), the treatment of endometriosis (Simitsidellis et al. 2018, Gibson et al. 2020), muscle wasting (Woerdeman & de Ronde 2011, von Haehling 2017), erectile dysfunction (Morgunov et al. 2007, Aversa et al. 2019), osteoporosis (Chen et al. 2019) and to treat breast cancer in women (Kono et al. 2016, Kono et al. 2017, Chen et al. 2020, Basaria et al. 2001, Shahidi 2001).

Both natural and synthetic androgens can act as anabolic–androgenic steroids (AAS, commonly called anabolic steroids). AASs can contribute to increases in body weight, often as lean mass increases can see gains in muscular strength and performance enhancement. For these reasons, their use in sport has been banned because of the potential to gain unfair advantage in physical competitions (Sjöqvist et al. 2008, Kicman 2008).

Literature References

PubMed ID	Title	Journal	Year
18254226	[Safety of long-term replacement hormonal therapy in patients with erectile dysfunction and androgen deficiency] Morgunov, LIu, Vertkin, AL, Pushkar', DIu	Urologiia	2007
27663436	Impact of androgen receptor expression in fluoxymesterone-treated estrogen receptor-positive metastatic breast cancer refractory to contemporary hormonal therapy Gong, Y, Tripathy, D, Fujii, T, Ueno, NT, Karuturi, MS, Bassett, R, Lyons, GR, Huo, L, Kono, M	Breast Cancer Res Treat	2016
11701661	Clinical review 138: Anabolic-androgenic steroid therapy in the treatment of chronic diseases Basaria, S, Dobs, AS, Wahlstrom, JT	J Clin Endocrinol Metab	2001
28301631	Androgen Receptor Function and Androgen Receptor-Targeted Therapies in Breast Cancer: A Review Lim, B, Fujii, T, Ueno, NT, Karuturi, MS, Tripathy, D, Kono, M	JAMA Oncol	2017
32544881	Androgens, oestrogens and endometrium: a fine balance between perfection and pathology Saunders, PTK, Collins, F, Gibson, DA, Simitsidellis, I	J Endocrinol	2020
32448030	Androgen Treatment in Adolescent Males With Hypogonadism Grinspon, RP, Rey, RA	Am J Mens Health	2020
6891012	Relative binding affinities of testosterone, 19-nortestosterone and their 5 alpha-reduced derivatives to the androgen receptor and to other androgen-binding proteins: a suggested role of 5 alpha-reductive steroid metabolism in the dissociation of "myotropic" and "androgenic" activities of 19-nortestosterone Tóth, M, Zakár, T	J Steroid Biochem	1982
31731497	Androgens and Androgen Receptor Actions on Bone Health and Disease: From Androgen Deficiency to Androgen Therapy Lin, PW, Yang, YC, Tsai, YR, Kang, HY, Chen, JF	Cells	2019
31826031	Acquired and hereditary forms of recurrent angioedema: Update of treatment Bork, K	Allergol Select	2018
28755533	Wasting away: How to treat cachexia and muscle wasting in chronic disease? von Haehling, S	Br J Clin Pharmacol	2017
17591767	Modulation of androgen receptor activation function 2 by testosterone and dihydrotestosterone Askew, EB, Gampe, RT, Stanley, TB, Faggart, JL, Wilson, EM	J Biol Chem	2007
32982970	Androgen Receptor in Breast Cancer: From Bench to Bedside Huang, J, Chen, M, Li, L, Xu, K, Qiu, F, Yang, Y	Front Endocrinol (Lausanne)	2020
32016915	Hormonal profile of menopausal women receiving androgen replacement therapy: a meta-analysis Maseroli, E, Marina, L, Spaggiari, G, Santi, D, Pandurevic, S, Sojat, AS	J Endocrinol Invest	2020
21158691	Therapeutic effects of anabolic androgenic steroids on chronic diseases associated with muscle wasting de Ronde, W, Woerdeman, J	Expert Opin Investig Drugs	2011
28919297	Androgens and endometrium: New insights and new targets Saunders, PTK, Gibson, DA, Simitsidellis, I	Mol Cell Endocrinol	2018
31110491	Androgen Deficiency and Phosphodiesterase Type 5 Expression Changes in Aging Male: Therapeutic Implications Calogero, AE, Duca, Y, La Vignera, S, Condorelli, RA, Aversa, A	Front Endocrinol (Lausanne)	2019
11589254	A review of the chemistry, biological action, and clinical applications of anabolic-androgenic steroids Shahidi, NT	Clin Ther	2001
21796517	Molecular mechanisms of androgen action--a historical perspective Brinkmann, AO	Methods Mol Biol	2011