scholarly journals Potential of Cyclin-Dependent Kinase Inhibitors as Cancer Therapy

2021 ◽  
Vol 12 (2) ◽  
pp. 182-184
Author(s):  
Ahmed F. Abdel-Magid
Keyword(s):  
Cancer Therapy ◽  
Kinase Inhibitors ◽  
Cyclin Dependent Kinase

Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 – 2014)

2015 ◽  
Vol 25 (9) ◽  
pp. 953-970 ◽  
Author(s):  
Veronika Malínková ◽  
Jakub Vylíčil ◽  
Vladimír Kryštof
Keyword(s):  
Cancer Therapy ◽  
Kinase Inhibitors ◽  
Cyclin Dependent Kinase ◽  
Patent Review

Anti-cancer therapy with cyclin-dependent kinase inhibitors: impact and challenges

2021 ◽  
Vol 23 ◽  
Author(s):  
Marika A. V. Reinius ◽  
Elizabeth Smyth
Keyword(s):  
Breast Cancer ◽  
Cancer Therapy ◽  
Kinase Inhibitors ◽  
Metastatic Breast ◽  
Treatment Resistance ◽  
Current Status ◽  
Cyclin Dependent Kinase ◽  
Cancer Management ◽  
Potential Biomarker ◽  
Anti Cancer

Abstract The introduction of cyclin-dependent kinase 4/6 inhibitors (CKIs) has marked a major development in the standard treatment of advanced breast cancer. Extensive preclinical, translational and clinical research efforts into CKI agents are ongoing, and clinical application of this class of systemic anti-cancer therapy is anticipated to expand beyond metastatic breast cancer treatment. Emerging evidence indicates that mechanisms by which CKI agents exert their therapeutic effect transcend their initially expected impacts on cell cycle control into the realms of cancer immunology and metabolism. The recent expansion in our understanding of the multifaceted impact of CKIs on tumour biology has the potential to improve clinical study design, therapeutic strategies and ultimately patient outcomes. This review contextualises the current status of CKI therapy by providing an overview of the original and emerging insights into mechanisms of action and the evidence behind their current routine use in breast cancer management. Recent preclinical and clinical studies into CKIs across tumour types are discussed, including a synthesis of the more than 300 clinical trials of CKI-combination treatments registered as of November 2020. Key challenges and opportunities anticipated in the 2020s are explored, including treatment resistance, combination therapy strategies and potential biomarker development.

Aurora Kinase Inhibitors in Head and Neck Cancer

2018 ◽  
Vol 18 (3) ◽  
pp. 199-213
Author(s):  
Guangying Qi ◽  
Jing Liu ◽  
Sisi Mi ◽  
Takaaki Tsunematsu ◽  
Shengjian Jin ◽  
...  
Keyword(s):  
Head And Neck Cancer ◽  
Cancer Therapy ◽  
Kinase Inhibitors ◽  
Biological Function ◽  
Aurora Kinase ◽  
Aurora Kinases ◽  
Related Research ◽  
Chemotherapy Drugs ◽  
Aurora Kinase Inhibitors

Aurora kinases are a group of serine/threonine kinases responsible for the regulation of mitosis. In recent years, with the increase in Aurora kinase-related research, the important role of Aurora kinases in tumorigenesis has been gradually recognized. Aurora kinases have been regarded as a new target for cancer therapy, resulting in the development of Aurora kinase inhibitors. The study and application of these small-molecule inhibitors, especially in combination with chemotherapy drugs, represent a new direction in cancer treatment. This paper reviews studies on Aurora kinases from recent years, including studies of their biological function, their relationship with tumor progression, and their inhibitors.

Mini-Review: Bmx Kinase Inhibitors for Cancer Therapy

2013 ◽  
Vol 8 (3) ◽  
pp. 228-238 ◽  
Author(s):  
John Jarboe ◽  
Shilpa Dutta ◽  
Sadanandan Velu ◽  
Christopher Willey
Keyword(s):  
Cancer Therapy ◽  
Kinase Inhibitors

scholarly journals The Individual Effects of Cyclin-Dependent Kinase Inhibitors on Head and Neck Cancer Cells—A Systematic Analysis

Cancers ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 2396
Author(s):  
Nina Schoenwaelder ◽  
Inken Salewski ◽  
Nadja Engel ◽  
Mareike Krause ◽  
Björn Schneider ◽  
...  
Keyword(s):  
Combination Therapy ◽  
Head And Neck ◽  
Kinase Inhibitors ◽  
In Vivo Studies ◽  
Specific Response ◽  
Cyclin Dependent Kinase ◽  
Systematic Analysis ◽  
Mhc I ◽  
Oncological Treatment

Cyclin-dependent kinase inhibitors (CDKi´s) display cytotoxic activity against different malignancies, including head and neck squamous cell carcinomas (HNSCC). By coordinating the DNA damage response, these substances may be combined with cytostatics to enhance cytotoxicity. Here, we investigated the influence of different CDKi´s (palbociclib, dinaciclib, THZ1) on two HNSCC cell lines in monotherapy and combination therapy with clinically-approved drugs (5-FU, Cisplatin, cetuximab). Apoptosis/necrosis, cell cycle, invasiveness, senescence, radiation-induced γ-H2AX DNA double-strand breaks, and effects on the actin filament were studied. Furthermore, the potential to increase tumor immunogenicity was assessed by analyzing Calreticulin translocation and immune relevant surface markers. Finally, an in vivo mouse model was used to analyze the effect of dinaciclib and Cisplatin combination therapy. Dinaciclib, palbociclib, and THZ1 displayed anti-neoplastic activity after low-dose treatment, while the two latter substances slightly enhanced radiosensitivity. Dinaciclib decelerated wound healing, decreased invasiveness, and induced MHC-I, accompanied by high amounts of surface-bound Calreticulin. Numbers of early and late apoptotic cells increased initially (24 h), while necrosis dominated afterward. Antitumoral effects of the selective CDKi palbociclib were weaker, but combinations with 5-FU potentiated effects of the monotherapy. Additionally, CDKi and CDKi/chemotherapy combinations induced MHC I, indicative of enhanced immunogenicity. The in vivo studies revealed a cell line-specific response with best tumor growth control in the combination approach. Global acting CDKi’s should be further investigated as targeting agents for HNSCC, either individually or in combination with selected drugs. The ability of dinaciclib to increase the immunogenicity of tumor cells renders this substance a particularly interesting candidate for immune-based oncological treatment regimens.

Cyclin-Dependent Kinase 4/6 (Cdk4/6) Inhibitors: Perspectives in Cancer Therapy and Imaging

2010 ◽  
Vol 10 (6) ◽  
pp. 527-539 ◽  
Author(s):  
F. Graf ◽  
B. Mosch ◽  
L. Koehler ◽  
R. Bergmann ◽  
F. Wuest ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Cyclin Dependent Kinase

Expression and mutational analysis of Cip/Kip family in early glottic cancer

2015 ◽  
Vol 129 (2) ◽  
pp. 168-173 ◽  
Author(s):  
D-K Kim ◽  
J H Lee ◽  
O J Lee ◽  
C H Park
Keyword(s):  
Dna Methylation ◽  
Polymerase Chain Reaction ◽  
Kinase Inhibitors ◽  
Mutational Analysis ◽  
Glottic Cancer ◽  
Cyclin Dependent Kinase ◽  
Chain Reaction ◽  
Single Strand Conformational Polymorphism ◽  
Early Glottic Cancer ◽  
Polymerase Chain

AbstractBackground:Genetic alteration of cyclin-dependent kinase inhibitors has been associated with carcinogenesis mechanisms in various organs.Objective:This study aimed to evaluate the expression and mutational analysis of Cip/Kip family cyclin-dependent kinase inhibitors (p21CIP1/WAF1, p27KIP1 and p57KIP2) in early glottic cancer.Methods:Expressions of Cip/Kip family and p53 were determined by quantitative reverse transcription polymerase chain reaction and densitometry. For the analysis of p21 inactivation, sequence alteration was assessed using single-strand conformational polymorphism polymerase chain reaction. Additionally, the inactivation mechanism of p27 and p57 were investigated using DNA methylation analysis.Results:Reduced expression of p27 and p57 were detected in all samples, whereas the expression of p21 was incompletely down-regulated in 6 of 11 samples. Additionally, single-strand conformational polymorphism polymerase chain reaction analysis showed the p53 mutation at exon 6. Methylation of p27 and p57 was detected by DNA methylation assay.Conclusion:Our results suggest that the Cip/Kip family may have a role as a molecular mechanism of carcinogenesis in early glottic cancer.

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