Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
J Med Chem
; 59(19): 8667-8684, 2016 10 13.
Article
em En
| MEDLINE
| ID: mdl-27171036
ABSTRACT
Cyclin dependent kinase (CDK) inhibitors have been the topic of intense research for nearly 2 decades due to their widely varied and critical functions within the cell. Recently CDK9 has emerged as a druggable target for the development of cancer therapeutics. CDK9 plays a crucial role in transcription regulation; specifically, CDK9 mediated transcriptional regulation of short-lived antiapoptotic proteins is critical for the survival of transformed cells. Focused chemical libraries based on a plethora of scaffolds have resulted in mixed success with regard to the development of selective CDK9 inhibitors. Here we review the regulation of CDK9, its cellular functions, and common core structures used to target CDK9, along with their selectivity profile and efficacy in vitro and in vivo.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quinase 9 Dependente de Ciclina
/
Inibidores de Proteínas Quinases
/
Descoberta de Drogas
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article