kunsel Lecture 22: Epigenetic Therapies-HDAC Inhibitors
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11 Terms
histone structural motifs for epigenetic signaling
protein methylation
acetylation
phosphorylation
CpG island shore & CpG island ~ methylation
lysine ~ acetylation
phosphorylation?
HATs
enzyme that puts acetyl groups onto histone & other proteins
HDACs
catalyze acetyl group removal from histones & other proteins
HDAC inhibitors
vorinostat
romidepsin
what drug
vorinostat (SAHA) strucuture
romidepsin (FK-228) structure
romidepsin prodrug mechanism
disulfide reduction
what makes romidepsin (FK-228) a prodrug?
disulfide bond → reduction activation
HDAC inhibitor structural motif
metal chelating ligand → reacts with Zn2+ on HDACi
why is epigenetic drug development so complicated?
HAT & HDAC proteins target other things besides histone proteins
tripartite motif of HDAC inhibitors
Note 
Flashcards (118)