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

N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists.

M A Dechantsreiter1, E Planker, B Mathä

  • 1Institut für Organische Chemie und Biochemie, Technische Universität München, Lichtenbergstrasse 4, D-85747 Garching, Germany.

Journal of Medicinal Chemistry
|August 17, 1999
PubMed
Summary

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

Bridging the gap: a systematic literature review and meta-analysis on the management of rectal wall defect after transanal excision.

Techniques in coloproctology·2026
Same author

Scrotal abscesses in perianal Crohn's disease: a retrospective cohort study of clinical presentation, management, and outcomes.

Techniques in coloproctology·2026
Same author

Pedicled omental flap construction: A useful adjunct to completion proctectomy or pouch excision for inflammatory bowel disease.

Techniques in coloproctology·2026
Same author

Total neoadjuvant therapy in early-onset versus average-onset locally advanced rectal cancer: patient characteristics and tolerance of therapy.

ESMO gastrointestinal oncology·2026
Same author

Endocannabinoid and N-acylethanolamine concentrations in hair of female patients with posttraumatic stress disorder - associations with clinical symptoms and outcomes following multimodal trauma-focused inpatient treatment.

Translational psychiatry·2025
Same author

Surgical and oncological outcomes in transverse colon carcinoma: does tumor sublocation make a difference?

Langenbeck's archives of surgery·2025

N-methylation of the alpha(V)beta(3) integrin antagonist cyclo(RGDfV) created a more potent compound, cyclo(RGDf-N(Me)V-). This discovery offers a promising new avenue for targeting tumor metastasis and angiogenesis.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • The alpha(V)beta(3) integrin receptor is crucial in human tumor metastasis and angiogenesis.
  • Inhibiting this receptor with antibodies or RGD-containing peptides shows therapeutic potential.

Purpose of the Study:

  • To investigate the impact of N-methylation on the biological activity of the alpha(V)beta(3) antagonist cyclo(RGDfV).
  • To identify more potent and selective inhibitors for targeting alpha(V)beta(3) integrin-mediated diseases.

Main Methods:

  • Synthesis and biological evaluation of N-methylated cyclo(RGDfV) analogs.
  • Nuclear Magnetic Resonance (NMR) spectroscopy for structural determination.
  • Distance geometry and molecular dynamics calculations for 3D structure analysis in water.

Related Experiment Videos

Main Results:

  • Cyclo(RGDf-N(Me)V-) (P5) demonstrated enhanced activity compared to the parent compound cyclo(RGDfV) (L1).
  • P5 is identified as a highly active and selective inhibitor of vitronectin binding to alpha(V)beta(3) integrin.
  • The study elucidated the high-resolution 3D structure of P5 in water.

Conclusions:

  • N-methylation of cyclo(RGDfV) significantly enhances its biological activity and selectivity as an alpha(V)beta(3) integrin antagonist.
  • The detailed structural insights contribute to understanding structure-activity relationships for developing novel anti-cancer therapeutics.
  • This research provides a foundation for future drug development targeting alpha(V)beta(3) integrin in cancer therapy.