Minoxidil binds to the androgen receptor in a previously unreported groove

I am bringing attention to this part of a study on Minoxidil. Minoxidil causes PFS for many and this study is the most comprehensive on the antiandrogenic drug, and perhaps the most in-depth look into what antiandrogens are doing to us on a transcriptional level. So comprehensive the study, that they discovered a new groove in the androgen receptor where minoxidil binds and prevents AR [Androgen Receptor] related functions.

I have PFS from Minoxidil, and it would be interesting to see if other AR-binding, PFS-causing drugs like Finasteride or Isotretinoin also occupy this previously undiscovered grove.


Interestingly, our structural studies demonstrated that minoxidil is chelated at a novel, previously unreported groove in the AR… Moreover, the groove is also located opposite to and at a distance from AF-2 and BF-3 sites…accordingly, it may represent a new candidate site for the interaction of AR coregulators. In our model, variations in this region resulted in steric clashes or changes in secondary structure. By occupying this grove, minoxidil may hinder the physical association of interacting proteins, thereby disrupting downstream regulation of AR transactivation. Taken together with mutagenesis data, our structural findings suggest that this groove may be important for binding of AR-interacting proteins during transactivation.