CDK9 a potential target for drug development (2008)
- Authors:
- Autor USP: CANDURI, FERNANDA - IQSC
- Unidade: IQSC
- Subjects: FÁRMACOS; MODELAGEM MOLECULAR; CÉLULAS; PROTEÍNAS
- Language: Inglês
- Abstract: The family of Cyclin-Dependent Kinases (CDKs) can be subdivided into two major functional groups based on their roles in cell cycle and/or transcriptional control. CDK9 is the catalytic subunit of positive transcription elongation factor b (P-TEFb). CDK9 is the kinase of the TAK complex (Tat-associated kinase complex), and binds to Tat protein of HIV, suggesting a possible role for CDK9 in AIDS progression. CDK9 complexed with its regulatory partner cyclin T1, serves as a cellular mediator of the transactivation function of the HIV Tat protein. P-TEFb is responsible for the phosphorylation of the carboxyl-terminal domain of RNA Pol II, resulting in stimulation of transcription. Furthermore, the complexes containing CDK9 induce the differentiation in distinct tissue. The CDK9/cyclin T1 complex is expressed at higher level in more differentiated primary neuroectodermal and neuroblastoma tumors, showing a correlation between the kinase expression and tumor differentiation grade. This may have clinical and therapeutical implications for these tumor types. Among the CDK inhibitors two have shown to be effective against CDK9: Roscovitine and Flavopiridol. These two inhibitors prevented the replication of human immunodeficiency virus (HIV) type 1 by blocking Tat transactivation of the HIV type 1 promoter. These compounds inhibit CDKs by binding to the catalytic domain in place of ATP, preventing transfer of a phosphate group to the substrate. More sensitivetherapeutic agents of CDK9 can be designed, and structural studies can add information in the understanding of this kinase. The major features related to CDK9 inhibition will be reviewed in this article
- Imprenta:
- Source:
- Título: Medicinal Chemistry
- ISSN: 1573-4064
- Volume/Número/Paginação/Ano: v. 4, n. 3, p. 210-218, 2008
-
ABNT
CANDURI, Fernanda et al. CDK9 a potential target for drug development. Medicinal Chemistry, v. 4, n. 3, p. 210-218, 2008Tradução . . Acesso em: 10 jan. 2026. -
APA
Canduri, F., Peres, P. C., Caceres, R. A., & Azevedo Junior, W. F. (2008). CDK9 a potential target for drug development. Medicinal Chemistry, 4( 3), 210-218. -
NLM
Canduri F, Peres PC, Caceres RA, Azevedo Junior WF. CDK9 a potential target for drug development. Medicinal Chemistry. 2008 ; 4( 3): 210-218.[citado 2026 jan. 10 ] -
Vancouver
Canduri F, Peres PC, Caceres RA, Azevedo Junior WF. CDK9 a potential target for drug development. Medicinal Chemistry. 2008 ; 4( 3): 210-218.[citado 2026 jan. 10 ] - Biochemical characterization of seminal plasma contents from rams and bucks
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