Table 4 Inhibitors of acylation readers entering the clinical trials
From: Protein acylation: mechanisms, biological functions and therapeutic targets
Inhibitor | Target | Mechanism | Clinical stage | Indications |
|---|---|---|---|---|
PLX51107 | BRD3, BRD4 | Blocking some of the enzymes needed for cell growth. | Phase I | Acute myeloid leukemia |
Phase I, II | Acute graft versus host disease, steroid-refractory graft versus host disease | |||
OTX015/Birabresib | BRD3, BRD4 | Inhibiting the binding of BRD3 and BRD4 to AcH4 and downregulate c-Myc expression. | Phase I | Acute myeloid leukemia |
BI 894999 | BRD4 (BD1), BRD3 (BD2) | Inhibiting the binding of BRD4 and BRD3 with acetylated histone proteins. | Phase I | Neoplasms, NUT carcinoma |
Apabetalone | BRD4 (BD2) | Displacing BET proteins from chromatin | Phase I, II | Pulmonary arterial hypertension |
Phase II, III | COVID-19 | |||
Phase I, II | Dyslipidemia, atherosclerosis | |||
Phase III | Diabetes mellitus, type 2 |
