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

The retinoid receptors

S M Pemrick1, D A Lucas, J F Grippo

  • 1Department of Toxicology and Pathology, Hoffman-La Roche, Nutley, NJ 07110.

Leukemia
|November 1, 1994
PubMed
Summary
This summary is machine-generated.

Retinoid receptors are crucial for gene regulation and have therapeutic uses in dermatology and oncology. However, resistance can develop due to mutations or pharmacokinetic issues, posing challenges for drug discovery.

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

A phase I, randomized, open-label study of the multiple-dose pharmacokinetics of vemurafenib in patients with BRAF V600E mutation-positive metastatic melanoma.

Cancer chemotherapy and pharmacology·2013
Same author

Safety, tolerability, and pharmacokinetics of ribavirin in hepatitis C virus-infected patients with various degrees of renal impairment.

Antimicrobial agents and chemotherapy·2013
Same author

The pharmacokinetics of peginterferon alfa-2a and ribavirin in African American, Hispanic and Caucasian patients with chronic hepatitis C.

Alimentary pharmacology & therapeutics·2012
Same author

Pharmacokinetically guided phase 1 trial of the IGF-1 receptor antagonist RG1507 in children with recurrent or refractory solid tumors.

Clinical cancer research : an official journal of the American Association for Cancer Research·2010
Same author

Glucokinase gene locus transgenic mice are resistant to the development of obesity-induced type 2 diabetes.

Diabetes·2001
Same author

Characterization of glucokinase regulatory protein-deficient mice.

The Journal of biological chemistry·2000

Area of Science:

  • Molecular Biology
  • Genetics
  • Pharmacology

Background:

  • Retinoid receptors are ligand-inducible transcription factors integral to cellular processes.
  • These receptors, including RAR and RXR, regulate gene expression and are vital for growth and differentiation.
  • Retinoids are clinically applied in dermatology and oncology, but resistance can emerge.

Purpose of the Study:

  • To explore the mechanisms of retinoid resistance.
  • To understand the role of mutated retinoic acid receptors (RAR) in dominant-negative activity.
  • To identify strategies for overcoming pharmacokinetic challenges in retinoid therapy.

Main Methods:

  • Analysis of nuclear receptor structure and function.
  • Investigation of gene pathways regulated by RAR and RXR.

Related Experiment Videos

  • Study of retinoid resistance in cell culture models (HL60R, RAC65).
  • Examination of dominant-negative activity of mutated RAR receptors.
  • Consideration of pharmacokinetic factors in clinical retinoid treatment.

    • Main Results:

    • Mutated RAR receptors can exhibit dominant-negative activity by binding DNA without activating transcription.
    • This dominant-negative effect may contribute to neoplastic diseases like acute promyelocytic leukemia (APL).
    • Clinical retinoid resistance is often linked to pharmacokinetic issues, such as decreasing plasma retinoic acid levels.

    Conclusions:

    • Understanding retinoid receptor mechanisms is key to developing effective cancer therapies.
    • Targeting dominant-negative receptor activity and improving drug pharmacokinetics are crucial for overcoming resistance.
    • Novel drug delivery systems or alternative retinoids may circumvent resistance mechanisms.