verucopeptin

Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.

[1] Aya Yoshimura, et al.Structure Elucidation of Verucopeptin, a HIF-1 Inhibitory Polyketide-Hexapeptide Hybrid Metabolite from an Actinomycete. Org Lett. 2015 Nov 6;17(21):5364-7. DOI:10.1021/acs.orglett.5b02718
[2] Nobuaki Takahashi, et al. Total synthesis of verucopeptin, an inhibitor of hypoxia-inducible factor 1 (HIF-1). Chem Commun (Camb). 2019 Oct 1;55(79):11956-11959. DOI:10.1039/c9cc06169j
[3] Yuezhou Wang, et al. Pharmacological Targeting of Vacuolar H +-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Jun 30;S2451-9456(20)30234-8. DOI:10.1016/j.chembiol.2020.06.011