Histone Acetlytransferase and the Androgen Receptor

[LinuxCavalier]

In doing some google research into Androgen Receptor corepressors and coactivators I've come across some things that were interesting to me (some of which I can't find any mention of already on this board) Specifically relating to Histone Acetlytransferase (HAT)...

Intriguingly, most co-activators and co-repressors share the capacity to influence transcriptional potential of the receptor by regulating the acetylation status of androgen responsive genes and/or the AR itself, via their respective histone acetyltransferase (HAT) or histone deacetylase (HDAC) activities. Indeed, we and others have demonstrated that the co-activators Tip60 (12), p300 and PCAF (13) enhance the inherent transcriptional activity of the AR by direct receptor acetylation and up-regulate transcriptional rate by histone acetylation of AR target genes. Conversely, AR activity has been shown to be down-regulated by histone deacetylase 1 (HDAC1) in a deacetylase-dependent manner (12,14), suggesting that reversal of HAT activity is important for abrogating AR function.

http://www.pubmedcentral.nih.gov/articl ... tid=546130

So this lead me thinking that clinical research into inhibiting HAT could perhaps be of some use. After further googling:

Two natural products, anacardic acid and garcinol (a polyprenylated benzophenone), are reported to inhibit both p300/CBP and PCAF in a 5-10 mM range in vitro (1, 2). In contrast, curcumin displays activity against p300/CBP, but not PCAF (3). Subsequent studies suggest that anacardic acid may be a broad-spectrum HAT inhibitor, as it also interferes with the MYST HAT Tip60 (13).

http://www.thesynapticleap.org/node/139

so perhaps this is the method of action for curcumin? It seemed to me that anacardic acid might have good possibilities, so I looked into that some...

Turns out that, unfortunately, wikipedia believes Anacardic acid can cause a skin reaction similar to that of poison ivy, so I don't think we should be putting this on our heads. I do find it notable that Anacardic acid is known to work well against Acne (although most believe this is because it kills the acne bacteria.) I also found it interesting that Anacardic acid, when being used to kill bacteria, works synergistically with anethole from the seed of anise (Umbelliferae) and linalool from green tea.

I'm not advocating anyone go out and find HAT inhibitors and try and use them (it would likely be a very bad idea), especially since HAT effects many things other than andorgen receptors. But the possibility of research in this area intrigues me. Seeing known anti-androgens like green tea and curcumin mentioned in the same sentence as known HAT inhibitors is potentially important.

 

[harold]

Curcumin doesnt seeem to have much effect by itself but something like that could be the reason why curcumin analogues like ASC-whatever inhibit androgen receptor expression. Interesting post. I dont think anybody here has any expertise in any of this stuff and so these things tend to slip by.
hh

 

[purecontrol]

Major anti-oxidants ie SOD act to reduce androgen receptor expression, and as an anti-estrogen.

 

[Bryan]

Major anti-oxidants ie SOD act to reduce androgen receptor expression, and as an anti-estrogen.

Do you still think estrogen is bad for hair, or have you finally gotten past that?

 

[purecontrol]

Major anti-oxidants ie SOD act to reduce androgen receptor expression, and as an anti-estrogen.

Do you still think estrogen is bad for hair, or have you finally gotten past that?

Time and time again we see that not all estrogens are equal just as not all androgens are equal.

And yes too much estrogen will indeed cause more problems ie overexpression of the AR, cancer, etc

It is just too hard for you to choke down those studies?


Oh and further as stated before polyphenols ie resveratrol which REGROW hair act as an estrogen antagonist when estorgen effects are too high and an agonist when estrogen effects are too low

SOD and other AO act in this manner as well.

Here is another one for you, vit E (known to help regrow hair) also acts as estrogen atagonist and reduce inflamation. http://raypeat.com/articles/articles/vitamin-e.shtml

Free Radicals and Inflamation time and time again are markers for hair loss

 

[Bryan]

Time and time again we see that not all estrogens are equal just as not all androgens are equal.

Oh, so now you're saying that _some_ estrogens are beneficial for hair, and others are harmful?

And yes too much estrogen will indeed cause more problems ie overexpression of the AR...

Reference or citation, please.

Oh and further as stated before polyphenols ie resveratrol which REGROW hair act as an estrogen antagonist when estorgen effects are too high and an agonist when estrogen effects are too low

Hey, what do you think about that new study showing that fulvestrant (the same anti-estrogen that was used by Smart to grow hair in that famous mouse experiment several years ago) was recently tested in HUMANS, and found to have no effect on hair growth?