2. Academic Validation
  3. Boholamide A, an APD-Class, Hypoxia-Selective Cyclodepsipeptide

Boholamide A, an APD-Class, Hypoxia-Selective Cyclodepsipeptide

  • J Nat Prod. 2020 Apr 24;83(4):1249-1257. doi: 10.1021/acs.jnatprod.0c00038.
Joshua P Torres 1,  Zhenjian Lin 1,  David S Fenton 1,  Lee U Leavitt 2,  Changshan Niu 1,  Pui-Ying Lam 3,  Jose Miguel Robes 4,  Randall T Peterson 3,  Gisela P Concepcion 4,  Margo G Haygood 1,  Baldomero M Olivera 2,  Eric W Schmidt 1 2
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, University of Utah, Salt Lake City, Utah 84112, United States.
  • 2 School of Biological Sciences, University of Utah, Salt Lake City, Utah 84112, United States.
  • 3 Department of Pharmacology and Toxicology, University of Utah, Salt Lake City, Utah 84112, United States.
  • 4 The Marine Science Institute, University of the Philippines, Diliman, Quezon City 1101, Philippines.
PMID: 32186874 DOI: 10.1021/acs.jnatprod.0c00038
Abstract

Calcium homeostasis is implicated in some cancers, leading to the possibility that selective control of calcium might lead to new Cancer drugs. On the basis of this idea, we designed an assay using a glioblastoma cell line and screened a collection of 1000 unique Bacterial extracts. Isolation of the active compound from a hit extract led to the identification of boholamide A (1), a 4-amido-2,4-pentadieneoate (APD)-class peptide. Boholamide A (1) applied in the nanomolar range induces an immediate influx of CA2+ in glioblastoma and neuronal cells. APD-class Natural Products are hypoxia-selective cytotoxins that primarily target mitochondria. Like Other APD-containing compounds, 1 is hypoxia selective. Since APD Natural Products have received significant interest as potential chemotherapeutic agents, 1 provides a novel APD scaffold for the development of new Anticancer compounds.

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