Retinol binding protein 4 antagonists and protein synthesis inhibitors: Potential for therapeutic development.
Direct antagonists
Fenretinide
Protein synthesis inhibitors
Retinol-binding protein 4
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Dec 2021
15 Dec 2021
Historique:
received:
07
06
2021
revised:
07
09
2021
accepted:
13
09
2021
pubmed:
22
9
2021
medline:
27
1
2022
entrez:
21
9
2021
Statut:
ppublish
Résumé
Retinol-binding protein 4 (RBP4) is a serum protein that transports Vitamin A. RBP4 is correlated with numerous diseases and metabolic syndromes, including insulin resistance in type 2 diabetes, cardiovascular diseases, obesity, and macular degeneration. Recently, RBP4 antagonists and protein synthesis inhibitors are under development to regulate the effect of RBP4. Several RBP4 antagonists, especially BPN-14136, have demonstrated promising safety profiles and potential therapeutic benefits in animal studies. Two RBP4 antagonists, specifically tinlarebant (Belite Bio) and STG-001 (Stargazer) are currently undergoing clinical trials. Some antidiabetic drugs and nutraceuticals have been reported to reduce RBP4 expression, but more clinical data is needed to evaluate their therapeutical benefits. As regulating RBP4 levels or its activities would benefit a wide range of patients, further research is highly recommended to develop clinically useful RBP4 antagonists or protein synthesis inhibitors.
Identifiants
pubmed: 34547506
pii: S0223-5234(21)00705-4
doi: 10.1016/j.ejmech.2021.113856
pii:
doi:
Substances chimiques
BPN-14136
0
Carboxylic Acids
0
Protein Synthesis Inhibitors
0
Pyrimidines
0
Pyrroles
0
RBP4 protein, human
0
Retinol-Binding Proteins, Plasma
0
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
113856Informations de copyright
Copyright © 2021 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.