CDK1: Occupies an important site of signal transduction, clinically refers to pancreatic cancer & glioma!

Cyclin-dependent kinase (CDK) is one of the important members of the protein kinase family; among them, CDK1 plays a key role in cell cycle regulation, checkpoint activation, and DNA damage repair

Important cell signaling site

Tumor cells are characterized by continuous division and uncontrolled proliferation.

There are many studies on whether the functions of CDKs are dependent and replaceable, especially CDK1 vs CDK2

In addition, CDK1 can completely compensate for the loss of CDK2 in terms of cell cycle regulation.

Disease location: pancreatic cancer & glioma

At present, the development of clinical indications for CDK1 inhibitors is mainly focused on pancreatic cancer and glioma, especially pancreatic cancer

Pancreatic cancer is known as the "king of cancer".

The treatment of pancreatic cancer mainly includes surgical treatment, radiotherapy and chemotherapy

　　Up to now, through database query, no drugs developed for CDK1 have been marketed, and the highest clinical progress is clinical phase III, such as Rigosertib (Phase III), BEY-1107 (Phase II), Zotiraciclib (Phase II), etc.

　　 First of all, this is a pan-target inhibitor, which is composed of oDeveloped by nconova Therapeutics for the treatment of first-line high-risk myelodysplastic syndrome (MDS) in combination with azacitidine

　　 BEY-1107 (Phase II)

　　The development company is Beyondbio, which is a CDK1 inhibitor and is clinically used in the treatment of pancreatic cancer

　　 Zotiraciclib (Phase II)

　　The development company is Adastra Pharmaceuticals, an oral brain-penetrating multikinase inhibitor, and also a multi-target inhibitor, especially targeting CDK1/2/5/7/9, which is clinically directed towards glioblastoma and interstitial Treatment of degenerative astrocyte tumors

　　Patent applications in China

　　Through domestic patent inquiries, the CDK1 inhibitor-related patents applied in China are related to tumors.

　　Shandong University applied for the invention patent "Cyclin-dependent kinase 1 inhibitor and its use" in 2011.

　　The Chinese Academy of Medical Sciences Peking Union Medical College Hospital, applied for the invention patent "Cyclin-dependent kinase 1 inhibitor and its use" in 2019.

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Research on the mechanism of cyclin-dependent kinase 1 promoting DNA synthesis and mediating tumor cell chemotherapy resistance.
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CN102019000441888C

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CN102011000146236C

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Cyclin-dependent kinases-based synthetic lethality: Evidence, concept, and strategy.
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Cyclin-dependent protein serine/threonine kinase inhibitors as anticancer drugs.
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Cell cycle regulators in cancer cell metabolism.
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Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.
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