CDK7: A Promising Drug Target and Biomarker for the Treatment of Cancer

Target Name: CDK7

NCBI ID: G1022

CDK7: A Promising Drug Target and Biomarker for the Treatment of Cancer

CDK7 (Chromatin-remodeling complex subunit K homolog) is a gene that encodes a protein involved in the process of chromosomal remodeling, which is critical for the development and progression of cancer. The discovery of CDK7 as a potential drug target and biomarker has significant implications for the treatment of cancer. In this article, we will explore the biology of CDK7, its role in cancer progression, and the potential of CDK7 as a drug target and biomarker.

The biology of CDK7

CDK7 is a 21-kDa protein that is expressed in most tissues of the body, including muscle, liver, and bone. It is a key component of the chromatin remodeling complex (CRC), which is responsible for maintaining the structural integrity of chromosomes and for regulating gene expression. The CRC includes several subunits, including CDK7, which plays a critical role in the regulation of microRNA (miRNA) expression.

CDK7 functions as a negative regulator of the CRC, primarily by binding to the CRC's G-box, which prevents the CRC from binding to the nuclear protein p21 ( transforming growth factor-??1). CDK7 has been shown to physically interact with p21 and to inhibit its phosphorylation, which is a critical event in the CRC's regulation of miRNA expression.

The role of CDK7 in cancer progression

CDK7 has been implicated in the progression of several types of cancer, including breast, ovarian, and prostate cancers. Several studies have shown that CDK7 is overexpressed or hypermethylated in the tumors of cancer patients, which may contribute to their poor prognosis.

In addition to its role in cancer progression, CDK7 has also been implicated in the regulation of cell survival. Several studies have shown that CDK7 can inhibit the apoptosis (programmed cell death) of cancer cells, which may contribute to their survival and the development of cancer-induced resistance.

The potential of CDK7 as a drug target

The potential of CDK7 as a drug target is based on several factors. First, CDK7 is a protein that can be targeted by small molecules, making it an attractive target for drug development. Second, the CRC is a well-established drug discovery target, and the use of small molecules to target CDK7 may simplify the drug development process.

CDK7 has been shown to play a critical role in the regulation of cellular processes that are important for cancer progression, such as cell survival, angiogenesis (the formation of new blood vessels), and the regulation of the immune response. Several small molecules have been shown to interact with CDK7 and to inhibit its activity, including inhibitors of the CRC, such as veraclimab and tasimetan.

In addition to its potential as a drug target, CDK7 has also been shown to be a potential biomarker for cancer. The CRC is a well-established biomarker for several types of cancer, and the use of small molecules to target CDK7 may provide a new tool for the diagnosis and treatment of cancer.

The future of CDK7 research

CDK7 has the potential to be a valuable drug target and biomarker for cancer. Further research is needed to fully understand its role in cancer progression and to develop effective small molecules to target it.

In addition, there is a need for studies to determine the safety and efficacy of small molecules that target CDK7. Preclinical studies are needed to assess the efficacy of small molecules for the treatment of cancer in cell

Protein Name: Cyclin Dependent Kinase 7

Functions: Serine/threonine kinase involved in cell cycle control and in RNA polymerase II-mediated RNA transcription. Cyclin-dependent kinases (CDKs) are activated by the binding to a cyclin and mediate the progression through the cell cycle. Each different complex controls a specific transition between 2 subsequent phases in the cell cycle. Required for both activation and complex formation of CDK1/cyclin-B during G2-M transition, and for activation of CDK2/cyclins during G1-S transition (but not complex formation). CDK7 is the catalytic subunit of the CDK-activating kinase (CAK) complex. Phosphorylates SPT5/SUPT5H, SF1/NR5A1, POLR2A, p53/TP53, CDK1, CDK2, CDK4, CDK6 and CDK11B/CDK11. CAK activates the cyclin-associated kinases CDK1, CDK2, CDK4 and CDK6 by threonine phosphorylation, thus regulating cell cycle progression. CAK complexed to the core-TFIIH basal transcription factor activates RNA polymerase II by serine phosphorylation of the repetitive C-terminal domain (CTD) of its large subunit (POLR2A), allowing its escape from the promoter and elongation of the transcripts (PubMed:9852112). Phosphorylation of POLR2A in complex with DNA promotes transcription initiation by triggering dissociation from DNA. Its expression and activity are constant throughout the cell cycle. Upon DNA damage, triggers p53/TP53 activation by phosphorylation, but is inactivated in turn by p53/TP53; this feedback loop may lead to an arrest of the cell cycle and of the transcription, helping in cell recovery, or to apoptosis. Required for DNA-bound peptides-mediated transcription and cellular growth inhibition

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