Table 3

Epigenetic clinical trials for aging-related degenerative diseasesa

Drugs

Epigenetic effect

Description

Clinical trials

References


Azacitidine

DNMT inhibitors

5-azacytidine; a chemical analogue of cytidine that affects DNA methylation as a false substrate

Phases I, II and III: myelodysplastic syndromes such as leukemia

[60]

Decitabine

DNMT inhibitors

5-aza-2'-deoxycytidine, a chemical analogue of cytidine that affects DNA methylation as a false substrate

Phases I, II and III: myelodysplastic syndromes such as leukemia, cervical, and non-small-cell lung cancer

[60]

Depsipeptide

HDAC inhibitors

Cyclic tetrapeptide

Phases I and II: hematological tumors such as leukemia and lymphoma

[78,79]

Phenylbutyrate

HDAC inhibitors

Aliphatic acid

Phases I and II: hematological tumors such as leukemia and lymphoma and colorectal cancer

[78,79]

Valproic acid

HDAC inhibitors

Aliphatic acid

Phase I: hematological tumors such as leukemia and lymphoma

[78,79]

Suberoylanilide hydroxamic acid

HDAC inhibitors

Hydroxamic acid

Phases I and II: hematological tumors, such as leukemia and lymphoma, solid tumors

[78,79]

Resveratrol

SIRT1 activator

A natural compound enriched in grapes and red wine

Phase I and II: diabetes, obesity, Alzheimer's disease and cancers

[118,119]

Genistein

Inhibitor of both DNMTs and HDACs

Active epigenetic diet found in soybean products

Preclinical: diabetes and cancer

[61,63,122,123]

EGCG

Inhibitor of both DNMTs and HDACs

Active epigenetic dietary compound enriched in green tea

Phase I: diabetes, cardiovascular disease and cancer

[61,62,124,125]

Sulforaphane

HDAC inhibitor

Active epigenetic dietary compound enriched in broccoli sprouts

Preclinical

[80,121]


aDNMT, DNA methyltransferase; HDAC, histone deacetylase; SIRT1, Sirtuin (silent mating type information regulation 2 homolog) 1; EGCG, epigallocatechin gallate.

Li et al. BMC Medicine 2011 9:98   doi:10.1186/1741-7015-9-98

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