Phenotypic screening with target identification and validation in the discovery and development of E3 ligase modulators.
E3 ligase modulators
drug discovery
phenotypic screening
targeted protein degradation
Journal
Cell chemical biology
ISSN: 2451-9448
Titre abrégé: Cell Chem Biol
Pays: United States
ID NLM: 101676030
Informations de publication
Date de publication:
18 03 2021
18 03 2021
Historique:
received:
16
10
2020
revised:
17
12
2020
accepted:
12
02
2021
entrez:
19
3
2021
pubmed:
20
3
2021
medline:
2
9
2021
Statut:
ppublish
Résumé
The use of phenotypic screening was central to the discovery and development of novel thalidomide analogs, the IMiDs (immunomodulatory drugs) agents. With the discovery that these agents bind the E3 ligase, CRL4
Identifiants
pubmed: 33740433
pii: S2451-9456(21)00096-9
doi: 10.1016/j.chembiol.2021.02.011
pii:
doi:
Substances chimiques
Immunologic Factors
0
Ubiquitin-Protein Ligases
EC 2.3.2.27
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
283-299Subventions
Organisme : Cancer Research UK
ID : C309/A11566
Pays : United Kingdom
Organisme : Medical Research Council
Pays : United Kingdom
Informations de copyright
Copyright © 2021 Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of interests The authors declare no competing interests. R.C. is a former employee of Celgene Corporation and previously had commercial interest in IMiDs, and is also a founder of Monte Rosa Therapeutics.