New targeted anti CDK4/6 peptide MM-D37K.

Боженко, В К; Кулинич, Т М; Kudinova, Elena Aleksandrovna; Boldyrev, Andrey; Solodkij, Vladimir Alekseevich

doi:10.1200/jco.2013.31.15_suppl.e13545

Cited by 10 publications

(5 citation statements)

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“…Its structure is derived from the endogenous CDK4/6 inhibitor p16 INK4a coupled to a cell penetrating sequence. MMD37K has shown a promising cytotoxic, cytostatic and antitumor effect in vitro and in vivo [81]. Another new CDK4/6 inhibitor, trilaciclib, prevents chemotherapy-induced myelosuppression.…”

Section: Resistance To Cdk4/6 Inhibitorsmentioning

confidence: 99%

CDK4/6 and MAPK—Crosstalk as Opportunity for Cancer Treatment

2020

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Despite the development of targeted therapies and novel inhibitors, cancer remains an undefeated disease. Resistance mechanisms arise quickly and alternative treatment options are urgently required, which may be partially met by drug combinations. Protein kinases as signaling switchboards are frequently deregulated in cancer and signify vulnerable nodes and potential therapeutic targets. We here focus on the cell cycle kinase CDK6 and on the MAPK pathway and on their interplay. We also provide an overview on clinical studies examining the effects of combinational treatments currently explored for several cancer types.

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Section: Resistance To Cdk4/6 Inhibitorsmentioning

confidence: 99%

CDK4/6 and MAPK—Crosstalk as Opportunity for Cancer Treatment

2020

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“…It is a non-ATP-competitive CDK4/6 inhibitor that is in Phase-II-stage clinical research. The merit of MM-D37K over the existing ATP-competitive CDK inhibitors will be explored, benefiting the development of next-generation CDK inhibitors [113].…”

Section: Cdk4/6 Inhibitors In Clinical Researchmentioning

confidence: 99%

Recent Progress in CDK4/6 Inhibitors and PROTACs

Wang,

Ba,

Kang

et al. 2023

Molecules

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Cell division in eukaryotes is a highly regulated process that is critical to the life of a cell. Dysregulated cell proliferation, often driven by anomalies in cell Cyclin-dependent kinase (CDK) activation, is a key pathological mechanism in cancer. Recently, selective CDK4/6 inhibitors have shown clinical success, particularly in treating advanced-stage estrogen receptor (ER)-positive and human epidermal growth factor receptor 2 (HER2)-negative breast cancer. This review provides an in-depth analysis of the action mechanism and recent advancements in CDK4/6 inhibitors, categorizing them based on their structural characteristics and origins. Furthermore, it explores proteolysis targeting chimers (PROTACs) targeting CDK4/6. We hope that this review could be of benefit for further research on CDK4/6 inhibitors and PROTACs.

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“…265 Other CDK4/6 inhibitors that are being studied in phase I clinical trial includes XZP-3287 (birociclib), 266 BEBT-209, 267 TY-302, 268 PF-06842874, 269 CS3002, 270 and MM-D37K. 271…”

Section: Cdk4/6 Inhibitorsmentioning

confidence: 99%

“…FCN‐437c is another orally bioavailable CDK4/6 inhibitor, which is being studied in a phase I trial in patients with advanced solid tumors by Fochon Pharmaceuticals 265 . Other CDK4/6 inhibitors that are being studied in phase I clinical trial includes XZP‐3287 (birociclib), 266 BEBT‐209, 267 TY‐302, 268 PF‐06842874, 269 CS3002, 270 and MM‐D37K 271 …”

Section: Selective Cdk Inhibitorsmentioning

confidence: 99%

Analyzing the scaffold diversity of cyclin‐dependent kinase inhibitors and revisiting the clinical and preclinical pipeline

Bhurta

Bharate

2021

Medicinal Research Reviews

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Kinases have gained an important place in the list of vital therapeutic targets because of their overwhelming clinical success in the last two decades. Among various clinically validated kinases, the cyclin‐dependent kinases (CDK) are one of the extensively studied drug targets for clinical development. Food and Drug Administration has approved three CDK inhibitors for therapeutic use, and at least 27 inhibitors are under active clinical development. In the last decade, research and development in this area took a rapid pace, and thus the analysis of scaffold diversity is essential for future drug design. Available reviews lack the systematic study and discussion on the scaffold diversity of CDK inhibitors. Herein we have reviewed and critically analyzed the chemical diversity present in the preclinical and clinical pipeline of CDK inhibitors. Our analysis has shown that although several scaffolds represent CDK inhibitors, only the amino‐pyrimidine is a well‐represented scaffold. The three‐nitrogen framework of amino‐pyrimidine is a fundamental hinge‐binding unit. Further, we have discussed the selectivity aspects among CDKs, the clinical trial dose‐limiting toxicities, and highlighted the most advanced clinical candidates. We also discuss the changing paradigm towards selective inhibitors and an overview of ATP‐binding pockets of all druggable CDKs. We carefully analyzed the clinical pipeline to unravel the candidates that are currently under active clinical development. In addition to the plenty of dual CDK4/6 inhibitors, there are many selective CDK7, CDK9, and CDK8/19 inhibitors in the clinical pipeline.

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New targeted anti CDK4/6 peptide MM-D37K.

Cited by 10 publications

References 0 publications

CDK4/6 and MAPK—Crosstalk as Opportunity for Cancer Treatment

CDK4/6 and MAPK—Crosstalk as Opportunity for Cancer Treatment

Recent Progress in CDK4/6 Inhibitors and PROTACs

Analyzing the scaffold diversity of cyclin‐dependent kinase inhibitors and revisiting the clinical and preclinical pipeline

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