Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
J Med Chem
; 64(16): 12200-12227, 2021 08 26.
Article
em En
| MEDLINE
| ID: mdl-34387088
ABSTRACT
The functions of the bromodomain and extra terminal (BET) family of proteins have been implicated in a wide range of diseases, particularly in the oncology and immuno-inflammatory areas, and several inhibitors are under investigation in the clinic. To mitigate the risk of attrition of these compounds due to structurally related toxicity findings, additional molecules from distinct chemical series were required. Here we describe the structure- and property-based optimization of the in vivo tool molecule I-BET151 toward I-BET282E, a molecule with properties suitable for progression into clinical studies.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Artrite
/
Quinolinas
/
Fatores de Transcrição
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Proteínas Nucleares
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Imidazóis
/
Anti-Inflamatórios
Limite:
Animals
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article