CDK4 Antibodies

Structure of CDK4

CDK4 is a cyclin-dependent kinase with a molecular weight of approximately 33.8 kDa. Its molecular weight is highly conserved among different species, mainly due to its key cell cycle function.

This protein is encoded by the CDK4 gene, and its primary structure contains a typical serine/threonine protein kinase domain. The tertiary structure presents a billobar configuration shared by all kinases. The N-terminal lobe is mainly composed of β -folds and is responsible for ATP binding, while the C-terminal lobe is dominated by α -helixes, providing structural support and participating in substrate recognition. The key residues in its active center, such as phenylalanine (Phe93) located in the ATP-binding pocket and the αC helix associated with the binding of cyclin D, jointly regulate its kinase activity and control the cell's transition from the G1 phase to the S phase.

Fig. 1 Specific targets of CDK4/6 inhibitors.¹

Key structural properties of CDK4:

• Encoding Cyclin-dependent kinase 4
• With the cell cycle protein D (Cyclin D) to activate the forming complexes
• The blocking of the cell cycle by phosphorylating Rb protein is relieved
• The core regulatory element of the G1/S phase checkpoint in cells

Functions of CDK4

The main function of the CDK4 gene is to regulate the process of the cell cycle from the G1 phase to the S phase. However, it is also widely involved in a variety of pathophysiological processes, including tumorigenesis, cell senescence and abnormal proliferation.

The kinase activity of CDK4 is completely dependent on its binding to Cyclin D, which is different from some constitutive activated kinases, indicating that it is strictly regulated by upstream signaling and serves as a core checkpoint for cells to determine whether to divide.

Applications of CDK4 and CDK4 Antibody in Literature

1. Zhou, Fiona H., et al. "CDK4/6 inhibitor resistance in estrogen receptor positive breast cancer, a 2023 perspective." Frontiers in cell and developmental biology 11 (2023): 1148792. https://doi.org/10.3389/fcell.2023.1148792

The article indicates that CDK4/6 inhibitors are first-line treatment drugs for ER+/HER2- advanced breast cancer, but the problem of drug resistance is becoming increasingly prominent. This article reviews its mechanism of action and the causes of drug resistance, and explores potential therapeutic strategies after drug resistance.

2. Yang, Yilan, et al. "CDK4/6 inhibitors: a novel strategy for tumor radiosensitization." Journal of Experimental & Clinical Cancer Research 39.1 (2020): 188. https://doi.org/10.1186/s13046-020-01693-w

The article indicates that CDK4/6 inhibitors can enhance tumor radiosensitivity through mechanisms such as inducing G1 phase arrest, inhibiting DNA damage repair, and enhancing apoptosis. Preclinical and small-sample studies have shown that its combination with radiotherapy has good tolerance and significant effects, but there is still a lack of large-scale clinical evidence at present, and the best combination regimen remains to be explored.

3. She, Youjun, et al. "CDK4/6 inhibitors in drug-induced liver injury: a pharmacovigilance study of the FAERS database and analysis of the drug–gene interaction network." Frontiers in pharmacology 15 (2024): 1378090. https://doi.org/10.3389/fphar.2024.1378090

Based on the analysis of the FAERS database, it was found that among the CDK4/6 inhibitors, ribociclib and abemaciclib have the risk of drug-induced liver injury (DILI), with ribociclib having the highest risk and palbociclib being relatively safe. The mechanism involves genes such as STAT3 and HSP90AA1, as well as multiple pathways. It is recommended to monitor liver function during clinical medication.

4. Nabieva, Naiba, and Peter A. Fasching. "CDK4/6 inhibitors—overcoming endocrine resistance is the standard in patients with hormone receptor-positive breast cancer." Cancers 15.6 (2023): 1763. https://doi.org/10.3390/cancers15061763

The article indicates that CDK4/6 inhibitors significantly improve the progression-free survival of advanced breast cancer. Among them, abemaciclib and ribociclib can prolong overall survival, and abemaciclib can also reduce the recurrence risk of early-stage patients. This type of drug has reshaped the treatment standards for breast cancer, and its drug resistance mechanism and combination treatment regimens are still under exploration.

5. Andrikopoulou, Angeliki, et al. "Aromatase and CDK4/6 inhibitor-induced musculoskeletal symptoms: a systematic review." Cancers 13.3 (2021): 465. https://doi.org/10.3390/cancers13030465

The article indicates that CDK4/6 inhibitors may alleviate muscle and joint pain caused by aromatase inhibitors (AIs). Studies have shown that compared with AI monotherapy, the incidence of arthralgia, myalgia and ostealgia in patients treated with CDK4/6 inhibitors in combination has decreased, suggesting that it may have a protective effect on AIMSS, but further verification is still needed.

Creative Biolabs: CDK4 Antibodies for Research

Creative Biolabs specializes in the production of high-quality CDK4 antibodies for research and industrial applications. Our portfolio includes monoclonal antibodies tailored for ELISA, Flow Cytometry, Western blot, immunohistochemistry, and other diagnostic methodologies.

• Custom CDK4 Antibody Development: Tailor-made solutions to meet specific research requirements.
• Bulk Production: Large-scale antibody manufacturing for industry partners.
• Technical Support: Expert consultation for protocol optimization and troubleshooting.
• Aliquoting Services: Conveniently sized aliquots for long-term storage and consistent experimental outcomes.

For more details on our CDK4 antibodies, custom preparations, or technical support, contact us at email.