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

Peptide hydroxamic acids inhibit skin collagenase.

W M Moore, C A Spilburg

    Biochemical and Biophysical Research Communications
    |April 14, 1986
    PubMed
    Summary

    Researchers developed peptide hydroxamic acids as inhibitors for human skin collagenase. The most effective compound, Z-Pro-Leu-Gly-NHOH, highlights the crucial role of the hydroxamate group in inhibiting this enzyme.

    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

    Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase.

    Bioorganic & medicinal chemistry letters·2001
    Same author

    A comparison of chronic combat-related posttraumatic stress disorder (PTSD) patients with and without a history of suicide attempt.

    The Journal of nervous and mental disease·2000
    Same author

    Attention to infants in the first year.

    Child: care, health and development·2000
    Same author

    Sitostanol administered in lecithin micelles potently reduces cholesterol absorption in humans.

    The American journal of clinical nutrition·1999
    Same author

    All parents should be given leaflet outlining full details of antenatal screening.

    BMJ (Clinical research ed.)·1999
    Same author

    2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase.

    Journal of medicinal chemistry·1998

    Area of Science:

    • Biochemistry
    • Medicinal Chemistry

    Background:

    • Human skin collagenase is a key enzyme involved in extracellular matrix remodeling.
    • Inhibitors of collagenase are sought for therapeutic applications, particularly in dermatological conditions.
    • Peptide-based inhibitors offer specificity and potential for targeted drug design.

    Purpose of the Study:

    • To synthesize and evaluate peptide hydroxamic acids as potential inhibitors of human skin collagenase.
    • To determine the structure-activity relationship, focusing on the C-terminal functional group.
    • To assess the potential of substrate analogs as collagenase inhibitors.

    Main Methods:

    • Synthesis of various peptide hydroxamic acids.
    • Enzyme inhibition assays to determine IC50 values.
    • Comparison of inhibition activity with peptides having different C-terminal groups (amide, carboxylate, aldehyde).

    Main Results:

    • Several peptide hydroxamic acids demonstrated inhibitory activity against human skin collagenase.
    • Z-Pro-Leu-Gly-NHOH exhibited significant inhibition with an IC50 value of 4 x 10(-5)M.
    • Peptides with amide, carboxylate, or aldehyde C-termini showed minimal to no inhibitory effect, underscoring the importance of the hydroxamate group.
    • The effective inhibitor's sequence mimicked the collagen cleavage site.

    Conclusions:

    • Peptide hydroxamic acids are effective inhibitors of human skin collagenase.
    • The hydroxamate functional group is critical for potent collagenase inhibition.
    • Substrate analogs containing metal-coordinating groups, like hydroxamates, are promising candidates for developing human collagenase inhibitors.

    Related Experiment Videos