Table 1 The table summarizes the main non-enzymatic modifications discussed in the review. We reported for each modification, the eraser accountable for the removal of non-enzymatic mark, and the drugs that exhibit a specific inhibitory activity
From: Epigenetic meets metabolism: novel vulnerabilities to fight cancer
NECM | Eraser | Drugs targeting the eraser enzyme |
|---|---|---|
Crotonylation | Histone deacetylates, Sirtuin 3 (SIRT3) | • 4’-bromo-resveratrol (4′-BR) [104] • 8-mercapto-3,7-dihydro-1H-purine-2,6-dione scaffold. [105] • BZD9Q [106] • Cambinol [107] • NƐ-acyl-lysine analogues [108] • 2-methoxyestradiol (2-ME) [109] • Butyrate [110] • Albendazole, [111] • 3-O-chloroacetyl-gagamine (A671) [112] • EX-527 [113] • LC-0296 [114] |
Formylation | HDAC6 | • JBI-097 [121] |
Propionylation | SIRT2 | • Thioamide-containing sirtuin inhibitors [130] • Thiourea-containing sirtuin inhibitors [130] |
β-ydroxybutyrylation | HDAC1 HDAC2 | • Chidamide (CS055) [134] • Santacruzamate A, [135] • Thujaplicins, [136] |
Succinylation | SIRT5 | • Norharmane derivative [141] • 2- cyano- N- phenyl- 3- (5-phenylfuran- 2- yl)acrylamide, ty [143] |
Malonylation | SIRT5 | • Norharmane derivative and the [141] • 2- cyano- N- phenyl- 3- (5-phenylfuran- 2- yl)acrylamide, ty [143] |
Glutarylation | SIRT7 | • 2800Z [150] • 40569Z [150] |
Lactylation | GLO1 HDAC1 HDAC2 HDAC3 | • Inhibitors targeting HDAC1 [134, 135] • Inhibitors targeting HDAC2 [136] • Inhibitors targeting HDAC3 [22] |
Glycation | DJ-1 PAD4 | • Inhibitors targeting DJ-1 [168] • Inhibitors targeting PAD4 [169] |