Table 1 Clinical trials of metabolic diseases by targeting protein modifications
From: Targeting protein modifications in metabolic diseases: molecular mechanisms and targeted therapies
No. | Drug | Modification | Mechanism | Phase | NCT number |
|---|---|---|---|---|---|
1 | Atorvastatin | Prenylation | An HMG-CoA reductase inhibitor; Inhibits the posttranslational prenylation of small guanosine triphosphate binding proteins. | II | NCT02633956 |
2 | Curcumin | Phosphorylation Ubiquitination O-GlcNAcylation | An ACC inhibitor; Phosphorylates and inactivates ACC; Inhibits protein ubiquitination; Inhibits O-GlcNAcylation pathway. | IV | NCT01052025 |
3 | MK-4074 | Phosphorylation Ubiquitination O-GlcNAcylation | An ACC inhibitor; Phosphorylates and inactivates ACC; Inhibits protein ubiquitination; Inhibits O-GlcNAcylation pathway. | I | NCT01431521 |
4 | PF-05221304 | Phosphorylation Ubiquitination O-GlcNAcylation | An ACC inhibitor; Phosphorylates and inactivates ACC; Inhibits protein ubiquitination; Inhibits O-GlcNAcylation pathway. | I II | NCT03248882 NCT03776175 |
5 | Firsocostat | Phosphorylation Ubiquitination O-GlcNAcylation | An ACC inhibitor; Phosphorylates and inactivates ACC; Inhibits protein ubiquitination; Inhibits O-GlcNAcylation pathway. | II | NCT02856555 |
6 | Resveratrol | Acetylation | Decreases PGC-1α acetylation. | I | NCT02704494 |
7 | Selonsertib (GS-4997) | Phosphorylation | An ASK1 inhibitor; Phosphorylates p38/JNK. | II IIb N/A I II II III III | NCT02177786 NCT04026165 NCT02781584 NCT02509624 NCT02466516 NCT03449446 NCT03053063 NCT03053050 |
8 | BGP-15 | Phosphorylation | A PARP inhibitor; Phosphorylates Akt and GSK-3, prevents p38/JNK activation. | II | NCT01069965 |
9 | Tropifexor | Acetylation | A FXR agonist; Acetylates FXR; Blocks connection of FXR and the SUMO ligase PIASγ. | II II | NCT02855164 NCT02854605 |
10 | Cilofexor | Acetylation | A FXR agonist, acetylated FXR Blocks connection of FXR and the SUMO ligase PIASγ. | II II II | NCT02854605 NCT03449446 NCT03987074 |
11 | Emricasan | Phosphorylation Nitrosylation Ubiquitination SUMOylation Acetylation | A pan-Caspase inhibitor; Inhibits SUMOylation of the ligand-binding domain. | II II | NCT02686762 NCT03205345 |
12 | Dorzagliatin | SUMOylation Nitrosylation | A GK agonist; Promotes SUMOylation of pancreatic glucokinase. | II | NCT03141073 |
13 | MK-0941 | SUMOylation Nitrosylation | A GK agonist; Promotes SUMOylation of pancreatic glucokinase. | III | / |
14 | AZD1656 | SUMOylation Nitrosylation | A GK agonist; Promotes SUMOylation of pancreatic glucokinase. | II II | NCT01152385 NCT01020123 |
15 | Trodusquemine | Phosphorylation Nitrosylation Sumoylation | A PTP1B inhibitor; Inhibits phosphorylation, nitrosylation and SUMOylation at active site Cys215. | I I I I | NCT00509132 NCT00806338 NCT00606112 NCT02524951 |
16 | Sodium phenylbutyrate | Acetylation | A HDAC inhibitor; Inhibits histone deacetylase. | I | NTR7426 |
