Cover Picture: Design and Synthesis of a MAO‐B‐Selectively Activated Prodrug Based on MPTP: A Mitochondria‐Targeting Chemotherapeutic Agent for Treatment of Human Malignant Gliomas (ChemMedChem 4/2015)
Year: 2015
Type: article
Abstract: The front cover picture shows a monoamine oxidase B (MAO-B; purple)-activated prodrug (MP-MUS; orange) for treatment of glioblastoma (GBM), which selectively targets GBM mitochondrial DNA. MP-MUS has a nitrogen mustard warhead that alkylates DNA and an oxidizable N-methyl tetrahydropyridine that selectively binds to MAO-B (a mitochondrial enzyme highly upregulated in GBM). The ring is oxidized by MAO-B to a pyridimum ring, yielding the active compound P+-MUS, which accumulates at a ratio of 1000 : 1 inside mitochondria. P+-MUS selectively targets mitochondria of GBM with no toxicity to other cells and avoids chemotherapeutic resistance. It is the first reported selective mitochondrial chemotherapy in humans. For further details, see the Full Paper by David S. Baskin et al. on p. 621 ff.
Source: ChemMedChem
Institutions: Houston Methodist, Cornell University, St. John's School
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: bronze
OpenAlex ID: W2135446748