Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

A self-assembling protein kinase C inhibitor.

S A Rotenberg1, T Calogeropoulou, J S Jaworski

  • 1Columbia University, Institute of Cancer Research, New York, NY 10032.

Proceedings of the National Academy of Sciences of the United States of America
|March 15, 1991
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Targeted Delivery of Microneurotrophin BNN27 via Biomaterial Grafts Protects Retinal Ganglion Cells After Optic Nerve Injury.

Journal of biomedical materials research. Part B, Applied biomaterials·2025
Same author

The monitoring of DNA adducts as an approach to carcinogen detection.

Annual review of public health·2010
Same author

Stat3 orchestrates tumor development and progression: the Achilles' heel of head and neck cancers?

Current cancer drug targets·2010
Same author

Activated checkpoint kinase 2 expression and risk for oral squamous cell carcinoma.

Cancer epidemiology, biomarkers & prevention : a publication of the American Association for Cancer Research, cosponsored by the American Society of Preventive Oncology·2007
Same author

A 17beta-derivative of allopregnanolone is a neurosteroid antagonist at a cerebellar subpopulation of GABA A receptors with nanomolar affinity.

British journal of pharmacology·2007
Same author

Hint1 is a haplo-insufficient tumor suppressor in mice.

Oncogene·2005
Same journal

Chemotactic self-organization captures the dynamics of mammalian hair follicle patterning.

Proceedings of the National Academy of Sciences of the United States of America·2026
Same journal

Tomographic imaging of superconducting order using particle-hole interference.

Proceedings of the National Academy of Sciences of the United States of America·2026
Same journal

Inhibitory potential of autologous neutralizing antibodies sets quantitative limits on the rebound-competent HIV-1 reservoir.

Proceedings of the National Academy of Sciences of the United States of America·2026
Same journal

Inferring epidemiological parameters under an infectious phylogeography model with visitor dynamics.

Proceedings of the National Academy of Sciences of the United States of America·2026
Same journal

Analytical modeling for suction cup designs for skin-interfaced wearable devices.

Proceedings of the National Academy of Sciences of the United States of America·2026
Same journal

Improving cell-free metabolism through direct integration of artificial respiratory chains.

Proceedings of the National Academy of Sciences of the United States of America·2026
See all related articles

A novel dicationic anticancer agent, formed in situ from phosphonium salts, selectively inhibits protein kinase C (PKC) isoforms. This discovery offers new insights into targeted cancer therapy mechanisms.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Cancer Biology

Background:

  • Dicationic anticarcinoma agents can form in situ from monocationic phosphonium salts.
  • These agents exhibit synergistic inhibition of cell growth and selective cytotoxicity against cancer cells.

Purpose of the Study:

  • To investigate the in vitro inhibitory effects of a dicationic product on protein kinase C (PKC) isoforms.
  • To elucidate the mechanism by which monocationic precursors and their dicationic product affect PKC activity.

Main Methods:

  • In vitro enzyme inhibition assays using purified PKC alpha and beta 1 isoforms.
  • Kinetic studies using High-Performance Liquid Chromatography (HPLC) to monitor product formation and enzyme activity.
  • Dose-response analyses of monocationic precursors and the dicationic product.

Related Experiment Videos

Main Results:

  • The dicationic product is a potent inhibitor of PKC alpha (IC50 = 20.4 microM) and PKC beta 1 (IC50 = 35 microM).
  • Monocationic precursors are weak inhibitors of PKC (IC50 > 200 microM).
  • The rate of dicationic product formation correlates with the time-dependent decrease in PKC activity when precursors are combined.

Conclusions:

  • The dicationic product formed in situ acts as an effective inhibitor of PKC alpha and beta 1.
  • PKC inhibition is a potential mechanism underlying the antiproliferative effects of these dicationic agents against carcinoma cells.