Cited by 517Retinoids in leukemia and cellular processesPeroxisome Proliferator-Activated ReceptorsPsoriasis: Treatment and Pathogenesis

RAR and RXR modulation in cancer and metabolic disease

Altucci, Lucia, Leibowitz, Mark D., Ogilvie, Kathleen M., de Lera, Angel R., Gronemeyer, Hinrich·2007·Nature Reviews Drug Discovery

Abstract

Retinoic acid receptors (RARs) are ligand-controlled transcription factors that function as heterodimers with retinoid X receptors (RXRs) to regulate cell growth and survival. The success of RAR modulation in the treatment of acute promyelocytic leukaemia (APL) has stimulated considerable interest in the development of RAR and RXR modulators. This has been aided by recent advances in the understanding of the biological role of RARs and RXRs and in the design of selective receptor modulators that might overcome the limitations of current drugs. Here, we discuss the challenges and opportunities for therapeutic strategies based on RXR and RAR modulators, with a focus on cancer and metabolic diseases such as diabetes and obesity.

Integrity signals

Registry

Crossref · 10.1038/nrd2397

Cites

184 of 184 references verified0 citation errors · 0 not checkable

Statistics

Recomputing p-values needs the paper’s full text.

Claims the paper makes

This paper’s full text isn’t openly available, so its claims and self-check weren’t run. The registry and citation checks still apply.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

  • Several semi-synthetic and synthetic retinoids have been developed to decrease the toxicity of natural retinoids and to increase their stability and selectivity against a specific RAR subtype.

    “To decrease the toxicity of the natural retinoids as well as to increase their stability and selectivity against a specific RAR subtype, several semi-synthetic and synthetic retinoids (including “atypical retinoids”) have been developed29,30.”
  • At least four molecules have reached phase 4 clinical trials: bexarotene, tazarotene, adapalene, and trifarotene.

    “At least four molecules have reached phase 4 clinical trials: bexarotene, tazarotene, adapalene, and trifarotene29–31.”
  • In most cases, RA-based monotherapies are less efficient in interfering with tumorigenesis and cancer progression than combination therapies.

    “In most cases, RA-based monotherapies are less efficient in interfering with tumorigenesis and cancer progression than combination therapies29.”

Cites

Flagged first, then by citations

Cited by

Sorted by citations

Authors
Altucci, L., Leibowitz, M. D., Ogilvie, K. M., de Lera, A. R., & Gronemeyer, H.
Affiliations
  • University of Campania "Luigi Vanvitelli" (IT)
  • Ligand Pharmaceuticals (United States) (US)
  • Exelixis (United States) (US)
  • Institut de génétique et de biologie moléculaire et cellulaire (FR)
Corresponding author
Gronemeyer, Hinrich
Venue
Nature Reviews Drug Discovery
Published
2007-10
Volume
6
Issue
10
Pages
793-810
ISSN
  • 1474-1776 (ISSN-L)
  • 1474-1784
OpenAlex
W2091007186
Cited by
517
References
184
Citations by year
2026: 9 · 2025: 24 · 2024: 13 · 2023: 14 · 2022: 23 · 2021: 16 · 2020: 20 · 2019: 35 · 2018: 25 · 2017: 21 · 2016: 22 · 2015: 24 · 2014: 32 · 2013: 36 · 2012: 43
FWCI
2.88
Type
journal article
Language
en
Open access
closed
Locations
  • Nature Reviews Drug Discovery (publishedVersion)
  • PubMed (publishedVersion)
  • HAL (submittedVersion)
  • Archivio Istituzionale della Ricerca - Università degli Studi della Campania "Luigi Vanvitelli" (submittedVersion)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Retinoids in leukemia and cellular processes
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Peroxisome Proliferator-Activated Receptors
  • Life Sciences › Immunology and Microbiology › Immunology › Psoriasis: Treatment and Pathogenesis
Keywords
retinoic acid receptor, retinoid X receptor, RAR/RXR heterodimers, acute promyelocytic leukemia, cancer therapy, metabolic disorders, diabetes mellitus, obesity, transcription factors, drug design
MeSH terms
Clinical Trials as Topic, Diabetes Mellitus, Humans, Ligands, Neoplasms, Obesity, Retinoids, Receptors, Retinoic Acid, Retinoid X Receptors

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review