Scripps VIVO scripps research logo

  • Index
  • Log in
  • Home
  • People
  • Organizations
  • Research
  • Events
Search form

Anti-tumor promoting effects of palmitoyl: protein thioesterase inhibitors against a human neurotumor cell line

Academic Article
uri icon
  • Overview
  • Research
  • Identity
  • Additional Document Info
  • View All
scroll to property group menus

Overview

authors

  • Dawson, G.
  • Dawson, S. A.
  • Marinzi, C.
  • Dawson, Philip

publication date

  • 2002

journal

  • Cancer Letters  Journal

abstract

  • Inhibiting the depalmitoylation of proteins disrupts cell survival signaling in tumor cells and leads to increased cell death. We chemically synthesized a non-hydrolyzable analog of the palmitoyl-cysteine thioester linkage (AcG-alpha-ketoamido-palmitoyl diamino propionate-VKIKK) (DAPKA) and showed that it inhibits palmitoyl:protein thioesterase (PPT1) in an in vitro assay using a specific fluorescent-based (4-methylumbelliferyl-beta-gluco-6-thiopalmitate) assay. We then showed that it killed cultured tumor cells and enhanced the killing of neurotumor cells by chemotherapeutic drugs such as etoposide and adriamycin. Overexpression of PPT1 protected against apoptosis induced by etoposide and the ketoamide and the inhibitory effect of the two was additive.

subject areas

  • Antibiotics, Antineoplastic
  • Antineoplastic Agents
  • Doxorubicin
  • Enzyme Inhibitors
  • Etoposide
  • Humans
  • Neuroblastoma
  • Thiolester Hydrolases
  • Tumor Cells, Cultured
scroll to property group menus

Research

keywords

  • apoptosis
  • ketoamide
  • neurotumor cell line
  • protein palmitoylation
  • thioesterase inhibitor
scroll to property group menus

Identity

International Standard Serial Number (ISSN)

  • 0304-3835

Digital Object Identifier (DOI)

  • 10.1016/s0304-3835(02)00403-2

PubMed ID

  • 12359364
scroll to property group menus

Additional Document Info

start page

  • 163

end page

  • 168

volume

  • 187

issue

  • 1-2

©2019 The Scripps Research Institute | Terms of Use | Powered by VIVO

  • About
  • Contact Us
  • Support