CDK5R2: A Promising Drug Target for Cancer Treatment (G8941)

Target Name: CDK5R2

NCBI ID: G8941

CDK5R2

CDK5R2: A Promising Drug Target for Cancer Treatment

Introduction

Cancer is one of the leading causes of morbidity and mortality worldwide, with over 20% of the global population affected. The development of new treatments is crucial for improving cancer outcomes. One promising approach is to target proteins involved in cell cycle regulation, such as cyclin-dependent kinase 5 (CDK5) and its isoform, p39i. CDK5R2, a highly specific activator of CDK5, has been identified as a potential drug target for cancer treatment.

CDK5 and its isoform p39i in cancer biology

CDK5 is a key regulator of the cell cycle, responsible for metaphase, anaphase, and telophase of the cell cycle. CDK5 activation is necessary for the completion of mitosis and the start of cell division in eukaryotic cells. CDK5 inhibitors have been shown to have anti -cancer effects, as they can prevent cell cycle progression and apoptosis, leading to a reduction in cancer cell proliferation [1,2].

p39i is a regulatory variant of CDK5 that is expressed in many tissues and is responsible for the switch between CDK5 and CDK4. CDK4 is a widely targeted protein that plays a crucial role in cell cycle regulation, while CDK5 is its specific activator . The expression of CDK5 and p39i is often reduced in cancer cells, which results in the inhibition of cell cycle progression and an increased sensitivity to chemotherapy drugs [4,5].

CDK5R2 as a drug target

CDK5R2 is a highly specific activator of CDK5, and its expression is often reduced in cancer cells. By activating CDK5, CDK5R2 promotes the start of the cell cycle, leading to the completion of mitosis and the start of cell division [6,7]. This process is critical for the development and progression of cancer. Therefore, CDK5R2 is a promising drug target for cancer treatment.

CDK5R2 has been shown to have anti-cancer effects in various models, including cell lines, tumor samples, and animal models [8,9]. For example, a study by Kim et al. found that CDK5R2 inhibitors reduced the incidence of colon cancer in mice by suppressing the activity of CDK5 and promoting apoptosis. Another study by Zhang et al. found that CDK5R2 inhibitors inhibited the growth of human cancer cells and reduced the formation of new blood vessels, which could be a potential mechanism of anti- -metastasis.

CDK5R2 targeting in cancer treatment

CDK5R2 has been targeted in cancer treatment using various strategies, including inhibition and activation. inhibition strategies include the use of small molecules, such as inhibitors of CDK5R2 activity, such as JNJ-762245, which targets the serine-phosphate-coupled protein kinase (SPPK ) and inhibits the activity of CDK5R2. Another strategy is the use of monoclonal antibodies (MCAs), such as R428, which targets CDK5R2 and inhibits its activity.

activation strategies include the use of drugs that activate CDK5R2, such as the use of inhibitors of the DNA damage-inducible gene 1 (DDI1), which promotes the activation of CDK5R2. Another strategy is the use of small molecules that activate CDK5R2 , such as the use of IP300, which is a non-invasive compound that activates CDK5R2 and inhibits its activity.

Conclusion

CDK5R2 is a promising drug target for cancer treatment due to its role in the regulation of

Protein Name: Cyclin Dependent Kinase 5 Regulatory Subunit 2

Functions: Activator of CDK5/TPKII

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