Re: Anacetrapib Officially Bites the Dust
posted on
Oct 26, 2017 03:22PM
Golfyeti,
You are incorrectly using the term epigenetics. I would refer to a small molecule like a CETP inhibitor that inhibits a single enzyme as a laser focused scalpel. I would refer to a drug like apabetalone, which is an inhibitor of the epigenetic reader BET proteins as more of a sledgehammer. CETP inhibitors have nothing to do with epigenetics.
The bromodomains of BET proteins recognize acetylated lysines on histones. Just to borrow some concise description from Wikipedia: "The acetylation of lysine residues is an important mechanism of epigenetics. It functions by regulating the binding of histones to DNA in nucleosomes and thereby controlling the expression of genes on that DNA.........Bromodomains, as the "readers" of lysine acetylation, are responsible in transducing the signal carried by acetylated lysine residues and translating it into various normal or abnormal phenotypes."
So a drug that affects BET proteins is going to have a much more widespread (sledgehammer) effect on gene expression and the number of affected pathways as opposed to a focused (scalpel) drug that inhibits an enzyme like CEPT that has no effect on mRNA transcription or epigenetics.
BearDownAZ