PROTACs bearing piperazine-containing linkers: what effect on their protonation state?
Journal
RSC advances
ISSN: 2046-2069
Titre abrégé: RSC Adv
Pays: England
ID NLM: 101581657
Informations de publication
Date de publication:
04 Aug 2022
04 Aug 2022
Historique:
received:
18
06
2022
accepted:
20
07
2022
entrez:
31
8
2022
pubmed:
1
9
2022
medline:
1
9
2022
Statut:
epublish
Résumé
Proteolysis targeting chimeras (PROTACs) represent an emerging class of compounds for innovative therapeutic application. Their bifunctional nature induces the formation of a ternary complex (target protein/PROTAC/E3 ligase) which allows target protein ubiquitination and subsequent proteasomal-dependent degradation. To date, despite great efforts being made to improve their biological efficacy PROTACs rational design still represents a challenging task, above all for the modulation of their physicochemical and pharmacokinetics properties. Considering the pivotal role played by the linker moiety, recently the insertion of a piperazine moiety into the PROTAC linker has been widely used, as this ring can in principle improve rigidity and increase solubility upon protonation. Nevertheless, the p
Identifiants
pubmed: 36043064
doi: 10.1039/d2ra03761k
pii: d2ra03761k
pmc: PMC9361468
doi:
Types de publication
Journal Article
Langues
eng
Pagination
21968-21977Informations de copyright
This journal is © The Royal Society of Chemistry.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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