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

Glucocorticoids: binding affinity and lipophilicity.

M Ponec, J Kempenaar, B Shroot

    Journal of Pharmaceutical Sciences
    |October 1, 1986
    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

    Comparison of human back versus arm skin region for its suitability to test weak irritants.

    Skin research and technology : official journal of International Society for Bioengineering and the Skin (ISBS) [and] International Society for Digital Imaging of Skin (ISDIS) [and] International Society for Skin Imaging (ISSI)·2016
    Same author

    The use of human keratinocytes and human skin models for predicting skin irritation.

    Alternatives to laboratory animals : ATLA·2014
    Same author

    The lipid organisation of the skin barrier: liquid and crystalline domains coexist in lamellar phases.

    Journal of biological physics·2013
    Same author

    Human skin equivalents are an excellent tool to study the effect of moisturizers on the water distribution in the stratum corneum.

    International journal of cosmetic science·2012
    Same author

    Reconstruction of human epidermis on de-epidermized dermis: Expression of differentiation-specific protein markers and lipid composition.

    Toxicology in vitro : an international journal published in association with BIBRA·2010
    Same author

    Use of human skin cell cultures for the estimation of potential skin irritants.

    Toxicology in vitro : an international journal published in association with BIBRA·2010
    Same journal

    Green, renewable, or low-carbon? A framework for informed solvent selection in pharmaceutical sciences.

    Journal of pharmaceutical sciences·2026
    Same journal

    Theranostic potential of ramucirumab functionalized magnetoliposomes for targeted delivery of sorafenib and MRI.

    Journal of pharmaceutical sciences·2026
    Same journal

    Intranasal mucoadhesive chitosan microspheres of ranolazine: Formulation, design, and pharmacokinetic evaluation.

    Journal of pharmaceutical sciences·2026
    Same journal

    Evolving landscape of drug development for pediatric rare diseases-from successes to strategies for addressing unmet needs.

    Journal of pharmaceutical sciences·2026
    Same journal

    A mathematical framework for predicting tablet weight variability from blend particle size distribution and tooling geometry.

    Journal of pharmaceutical sciences·2026
    Same journal

    Recrystallization can stop nitrosamine formation in ranitidine hydrochloride.

    Journal of pharmaceutical sciences·2026
    See all related articles

    Steroid modifications alter glucocorticoid receptor binding affinity and lipophilicity. Hydroxyl groups increase affinity, while acetate esters decrease it, impacting drug design for glucocorticoid receptor interactions.

    Area of Science:

    • Biochemistry
    • Molecular Pharmacology
    • Dermatology

    Background:

    • The glucocorticoid receptor (GR) plays a crucial role in cellular responses.
    • Understanding steroid-ligand interactions with GR is vital for therapeutic development.
    • Keratinocytes express functional GR, relevant for skin conditions.

    Purpose of the Study:

    • To determine the relative binding affinities of 35 steroids for the GR.
    • To correlate binding affinity with steroid lipophilicity.
    • To investigate how structural modifications affect GR binding and lipophilicity.

    Main Methods:

    • Competitive binding assays using radiolabeled dexamethasone or hydrocortisone.
    • Measurement of steroid lipophilicity via partition coefficients (1-octanol/aqueous buffer).

    Related Experiment Videos

  • Analysis of 35 different steroid structures and their GR binding characteristics.

    • Main Results:

    • Hydroxyl group substitutions (17 alpha-OH, 21-OH) decreased lipophilicity and increased GR affinity.
    • Acetate ester substitutions (17 alpha-OAc, 21-OAc) increased lipophilicity and decreased GR affinity.
    • Longer ester chains (valerate) increased both lipophilicity and affinity, but 21-esters had lower affinity than parent alcohols.

    Conclusions:

    • Steroid structure significantly influences both lipophilicity and GR binding affinity.
    • Specific substitutions can modulate GR interaction, offering potential for targeted drug design.
    • A correlation between binding affinity and lipophilicity was observed for 17 alpha- and 21-ester series.