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. 2020 May 8;25(9):2197. doi: 10.3390/molecules25092197

Table 1.

Summary of pharmacological studies on largazole (1).

Disease/Target Significant Biological Activity Reference
Angiogenesis-associated diseases
  • Topical application of the compound attenuated alkali-induced corneal neovascularization in mouse model.

  • Down-regulated the expression of the pro-angiogenic factors and up-regulated the expression of the anti-angiogenic factors in vivo.

[31]
Lung cancer
  • Potently inhibits the proliferation and clonogenic activity in lung cancer cells.

  • Arrests cell cycle at G1 phase and up-regulates the expression of cyclin-dependent kinase inhibitor p21 in lung cancer cells.

  • An E2F1-targeting cell cycle inhibitor, which is overexpressed in lung cancer tumor.

[32]
Rheumatoid arthritis
  • Activates p38 and Akt pathways and increase expression of HDAC6 by more than 200% in rheumatoid arthritis synovial fibroblasts.

  • Increases HDAC6 expression, which led to enhancement of the detrimental effects of TNF-α in RA synovial fibroblasts.

[33]
Liver fibrosis
  • Reduces liver fibrosis and angiogenesis by inhibition of transforming growth factor-b as well as vascular endothelial growth factor signalling.

[34]
Breast cancer
  • Cooperates with dexamethasone to induce localization of E-cadherin to the plasma membrane in breast cancers as well as to suppress in vitro cellular invasion of cancer cells.

[35]
Protein ubiquitination
  • Largazole and its ester and ketone analogs selectively inhibit ubiquitin conjugation to p27Kip1 and TRF1 in vitro.

[36]
Epstein-Barr virus (EBV)-associated lymphomas
  • Induces expression of EBV lytic-phase gene and sensitize lymphoma cells to nucleoside antiviral drugs.

[37]
Bone-related disorders
  • Exhibits in vitro and in vivo osteogenic activity via increased expression of Runx2 (runt-related transcription factor 2) and BMPs (bone morphogenetic proteins).

  • Induces expression of alkaline phosphatase (ALP) and osteopontin (OPN).

[38]
Colon cancer
  • Strongly stimulated histone hyperacetylation in tumor in vivo by using a human HCT116 xenograft mouse model.

  • Efficacy in inhibiting tumor growth and induced apoptosis in the tumor.

  • Regulates transcription of genes involved in the induction of cell cycle arrest and apoptosis.

[39]
Oncogenic super-enhancers
  • Decreases RNA polymerase II accumulation at super-enhancers (SEs) and preferentially suppresses SE-driven transcripts associated with oncogenic activities in transformed cells.

[40]
Antiretroviral therapy
  • Combination of largazole and bryostatin analogues are potent activators of latent HIV without global T-cell activation within resting CD4+ T-cells.

[41]