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

Novel alpha-glucosidase inhibitors identified using multiple cyclic peptide combinatorial libraries

J Eichler1, A W Lucka, C Pinilla

  • 1Torrey Pines Institute for Molecular Studies, San Diego, CA 92121, USA.

Molecular Diversity
|August 1, 1996
PubMed
Summary

Researchers synthesized peptide libraries to find alpha-glucosidase inhibitors. A specific hexapeptide lactam library showed significant activity and was optimized to identify potent and selective inhibitors.

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

Long-term in vivo degradation of Mg-Zn-Ca elastic stable intramedullary nails and their influence on the physis of juvenile sheep.

Biomaterials advances·2023
Same author

["Legal highs" (new psychoactive substances) : What does the anesthesiologist need to know?]

Der Anaesthesist·2020
Same author

[Efficacy of biofeedback in patients with chronic low back pain : Impact on pain intensity, psychological factors and stress markers].

Schmerz (Berlin, Germany)·2019
Same author

Comparison of a resorbable magnesium implant in small and large growing-animal models.

Acta biomaterialia·2018
Same author

Chronic intrahypothalamic rather than subcutaneous liraglutide treatment reduces body weight gain and stimulates the melanocortin receptor system.

International journal of obesity (2005)·2017
Same author

Long-term in vivo degradation behavior and near-implant distribution of resorbed elements for magnesium alloys WZ21 and ZX50.

Acta biomaterialia·2016

Area of Science:

  • Medicinal Chemistry
  • Biochemistry
  • Peptide Synthesis

Background:

  • Cyclic peptides offer unique structural properties for drug discovery.
  • Alpha-glucosidase inhibitors are crucial for managing type 2 diabetes.

Purpose of the Study:

  • To develop novel cyclic peptide inhibitors of alpha-glucosidase.
  • To identify potent and selective alpha-glucosidase inhibitors through combinatorial library synthesis and screening.

Main Methods:

  • Synthesis of 26 cyclic peptide combinatorial libraries (disulfides and lactams) and linear analogs.
  • Screening of libraries for alpha-glucosidase inhibitory activity.
  • Iterative synthesis and screening to define key positions in active hexapeptide lactam library cyclo[xXxXxN].

Related Experiment Videos

Main Results:

  • One hexapeptide lactam library (cyclo[xXxXxN]) exhibited significant alpha-glucosidase inhibitory activity.
  • Iterative optimization successfully defined all five variable positions (x and X) within the active library.
  • Potent and selective alpha-glucosidase inhibitors were identified from the optimized library.

Conclusions:

  • Cyclic peptide combinatorial libraries are effective for discovering enzyme inhibitors.
  • The identified compounds represent promising leads for alpha-glucosidase inhibitor drug development.
  • This approach enables the discovery of potent and selective drug candidates.