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

Tissue transglutaminase inhibition.

Jeffrey W Keillor1

  • 1Départment de Chimie, Université de Montréal, Québec H3C 3J7, Canada.

Chemistry & Biology
|April 27, 2005
PubMed
Summary

Researchers synthesized novel peptidic dihydroisoxazole compounds that inhibit tissue transglutaminase (TG2). These compounds show promise for synergistic glioblastoma treatment due to their oral bioavailability and efficacy.

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

Trylons: Polyamide Surrogate Substrates Enable High-Throughput Screening of Nylon-Degrading Enzymes.

Chembiochem : a European journal of chemical biology·2026
Same author

Editor's Note: Transglutaminase Interaction with α6/β4-Integrin Stimulates YAP1-Dependent ΔNp63α Stabilization and Leads to Enhanced Cancer Stem Cell Survival and Tumor Formation.

Cancer research·2026
Same author

Diving into AA9-mediated transglutaminase 2 inhibition reveals ferroptosis as driver of anticancer effects.

Biochemical pharmacology·2026
Same author

Don't Lose Your (War)head: Structure-Activity Relationships of Covalent Warheads as Substrates for GST-Catalyzed Glutathione Conjugation.

Journal of medicinal chemistry·2026
Same author

Structure-activity relationships of hydrophobic small molecule irreversible inhibitors of tissue transglutaminase.

RSC medicinal chemistry·2025
Same author

Tissue transglutaminase inhibitors over the past decade.

Bioorganic & medicinal chemistry·2025

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Biochemistry

Background:

  • Glioblastoma multiforme (GBM) is an aggressive brain tumor with limited treatment options.
  • Tissue transglutaminase 2 (TG2) is implicated in GBM progression and chemoresistance.
  • Novel therapeutic strategies targeting TG2 are needed for improved GBM treatment.

Discussion:

  • This study details the synthesis of novel peptidic dihydroisoxazole derivatives.
  • In vitro evaluation demonstrated the inhibitory potential of these compounds against recombinant human TG2.
  • The compounds exhibited favorable oral bioavailability and efficacy in preclinical models.

Key Insights:

  • Peptidic dihydroisoxazoles are effective inhibitors of human TG2.
  • These novel inhibitors show potential for synergistic glioblastoma therapy.
  • Oral administration of these compounds is feasible and effective.

Outlook:

  • Further investigation into the mechanism of action and long-term effects is warranted.
  • Clinical translation of these TG2 inhibitors could offer a new therapeutic avenue for glioblastoma.
  • Combination therapies involving these compounds may enhance treatment outcomes for brain tumors.

Related Experiment Videos