Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five' chemical space: Recent progress and future challenges.
Absorption
Beyond rule-of-five
Degradation
Oral bioavailability
PROTACs
Proteolysis targeting chimeras
bRo5
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
01 07 2019
01 07 2019
Historique:
received:
13
02
2019
revised:
11
04
2019
accepted:
16
04
2019
pubmed:
3
5
2019
medline:
10
9
2020
entrez:
4
5
2019
Statut:
ppublish
Résumé
Proteolysis targeting chimeras (PROTACs) are heterobifunctional compounds with molecular weights and other properties that lie outside the classic 'rule-of-five' space. Consequently, PROTACs have unique challenges associated with their development as potential therapeutic agents. This review summarizes and analyzes a representative set of recent PROTACs and highlights some of the potential future challenges facing this promising modality.
Identifiants
pubmed: 31047748
pii: S0960-894X(19)30249-5
doi: 10.1016/j.bmcl.2019.04.030
pii:
doi:
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
1555-1564Informations de copyright
Copyright © 2019 Elsevier Ltd. All rights reserved.