Androgen receptor: Difference between revisions
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====Side effects of SARMs==== | ====Side effects of SARMs==== | ||
Despite the consistent effect demonstrated by SARMs on lean body mass accrual, reductions in high-density lipoprotein (HDL) seem to be an important concern with these compounds, though it occurs to a lesser extent compared to testosterone <ref name="clinical trials">PMID: 32476495</ref>. | Despite the consistent effect demonstrated by SARMs on lean body mass accrual, reductions in high-density lipoprotein (HDL) seem to be an important concern with these compounds, though it occurs to a lesser extent compared to testosterone <ref name="clinical trials">PMID: 32476495</ref>. | ||
SARMs administration has also been related to hepatotoxicity and some compounds have shown liver enzymes alterations. The most common adverse events are an increase in alanine transaminase and aspartate transaminase <ref name="clinical trials" />. | SARMs administration has also been related to hepatotoxicity and some compounds have shown liver enzymes alterations. The most common adverse events are an increase in alanine transaminase and aspartate transaminase <ref name="clinical trials" />. | ||
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===Antagonist=== | ===Antagonist=== | ||
'''[[Image:Non-steroideal anti-androgens.jpeg | thumb | right ]]''' | '''[[Image:Non-steroideal anti-androgens.jpeg | thumb | right | Reproduced from Helsen et al. <ref name="ARA prostate" />]]''' | ||
These kinds of drugs were developed with the objective to avoid the secondary effects associated with cross reactivity of steroidal ARA, increasing the selectivity and the affinity to the androgen receptor, limiting the association with other steroids nuclear receptors <ref name="bicalutamide" />. Also, their non-steroidal structure improved oral bioavailability being another advantage in comparison with steroidal ARA <ref name="bicalutamide" />. Some examples are flutamide, bicalutamide <ref name="ARA prostate" /><ref name="bicalutamide" /><ref name="nonsteroidal" /><ref name="Bicalutamide functions">PMID: 12015321</ref><ref name="Unexpected">PMID: 21506597</ref><ref name="Role of AR">PMID: 30209899</ref> or apalutamide (ARN-509) <ref name="ARA prostate" /><ref name="Role of AR" />. | These kinds of drugs were developed with the objective to avoid the secondary effects associated with cross reactivity of steroidal ARA, increasing the selectivity and the affinity to the androgen receptor, limiting the association with other steroids nuclear receptors <ref name="bicalutamide" />. Also, their non-steroidal structure improved oral bioavailability being another advantage in comparison with steroidal ARA <ref name="bicalutamide" />. Some examples are flutamide, bicalutamide <ref name="ARA prostate" /><ref name="bicalutamide" /><ref name="nonsteroidal" /><ref name="Bicalutamide functions">PMID: 12015321</ref><ref name="Unexpected">PMID: 21506597</ref><ref name="Role of AR">PMID: 30209899</ref> or apalutamide (ARN-509) <ref name="ARA prostate" /><ref name="Role of AR" />. | ||
====Bicalutamide==== | ====Bicalutamide==== | ||