Recent developments in antiandrogens and selective androgen receptor modulators

The effects of visceral obesity and androgens on bone: trenbolone protects against loss of femoral bone mineral density and structural strength in viscerally obese and testosterone-deficient male rats

“…However, unlike TREN [38], supraphysiological TEST is prone to aromatisation to estradiol in adipose tissue [39]. In the present study, the reductions in VAT mass induced by TREN were likely mediated by the unique androgen receptor affinity and endocrine metabolism of 17-betahydroxylated steroids, described elsewhere [40,41].…”

“…In the present study, the reductions in VAT mass induced by TREN were likely mediated by the unique androgen receptor affinity and endocrine metabolism of 17-betahydroxylated steroids, described elsewhere [40,41]. Briefly, TREN does not undergo the enzymatic bioconversions typical of testosterone, and TREN treatment is therefore highly selective of the androgen receptor [38,41]. In a model of late-onset testosterone deficiency, Abdelhamed et al [42] described the role of the androgen receptor in reducing visceral adipose cell size in aged male rats.…”

Twenty-five Years of Nuclear Receptor Structure Analysis: From the Laboratory to the Clinic

“…However, the growth promoting action of androgens on the prostate is of real concern with androgen replacement therapies. To date a number of non-steroidal molecules have been designed and tested as 'androgen selective modulators' (SARMs), in the laboratory and more recently in clinical trials for indicators such as sarcopenia and osteoporosis (reviewed in (Haendler and Cleve 2012;McEwan 2013;Narayanan et al 2008) Crystal structures are available for the wild-type AR-LBD bound with the SARMs andarine , LGD2226 (Wang et al 2006) and BMS-564929 (Ostrowski et al 2007). The canonical agonist bound LBD structure (see Fig.…”

Mammalian Cells Engineered to Produce Novel Steroids

“…Steroid hormone analogs take advantage of the wideranging effects of their endogenous counterparts, such as immunosuppression and increased bone density, and thus are used to treat conditions ranging from arthritis to anemia. Unfortunately, the global responses steroids alter result in side effects, such as diabetes and osteoporosis for glucocorticoids, or masculinizing effects for androgens [1][2][3] . They are active at bloodstream concentrations in the nanomolar range and readily cross cell membranes 4,5 .…”