Drug name: Valproic Acid


Related CSCTT Targets

GSK3-β [ref.1]P49841

Valproic Acid, Valproate

Cas.no PubChem ID
99-66-1 3121
Known Target
Histone deacetylase 9Q9UKV0
4-aminobutyrate aminotransferase, mitochondrialP80404
Short/branched chain specific acyl-CoA dehydrogenase, mitochondrialP45954
2-oxoglutarate dehydrogenase, mitochondrialQ02218
Succinate-semialdehyde dehydrogenase, mitochondrialP51649
Histone deacetylase 2Q92769
Introduction
Valproic Acid dissociates to the valproate ion in the gastrointestinal tract and then binds to and inhibits GABA transaminase. The drug's anticonvulsant activity may be related to increased brain concentrations of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter in the CNS, by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. Valproic Acid may also work by suppressing repetitive neuronal firing through inhibition of voltage-sensitive sodium channels. It is also a histone deacetylase inhibitor. Valproic acid has also been shown to be an inhibitor of an enzyme called histone deacetylase 1 (HDAC1). HDAC1 is needed for HIV to remain in infected cells. A study published in August 2005 revealed that patients treated with valproic acid in addition to highly active antiretroviral therapy (HAART) showed a 75% reduction in latent HIV infection.

Valproic Acid, Valproate-Structure

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Reference

  • [1] Histone deacetylase inhibitors stimulate dedifferentiation of human breast cancer cells through WNT/β-catenin signaling. Debeb, B. G., et al. (2012).Stem Cells. 30(11):2366-77.
    22961641. [ 22961641 ]

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