Discovery of novel co-degradation CK1&#945; and CDK7/9 PROTACs with p53 activation for treating acute myeloid leukemia.

Wang, Kai; Jiang, Meixu; Liu, Huimin; Meng, Chen; Li, Mengyuan; Lu, Haibin

Discovery of novel co-degradation CK1α and CDK7/9 PROTACs with p53 activation for treating acute myeloid leukemia.

Wang, Kai; Jiang, Meixu; Liu, Huimin; Meng, Chen; Li, Mengyuan; Lu, Haibin.

Affiliation

Wang K; College of Pharmacy, Jilin University, Changchun 130021, China.
Jiang M; College of Pharmacy, Jilin University, Changchun 130021, China.
Liu H; College of Pharmacy, Jilin University, Changchun 130021, China.
Meng C; College of Pharmacy, Jilin University, Changchun 130021, China.
Li M; College of Pharmacy, Jilin University, Changchun 130021, China.
Lu H; College of Pharmacy, Jilin University, Changchun 130021, China. Electronic address: luhaibin@jlu.edu.cn.

Bioorg Chem ; 147: 107319, 2024 Jun.

Article in En | MEDLINE | ID: mdl-38593529

Subject(s)

Antineoplastic Agents; Casein Kinase Ialpha; Cell Proliferation; Cyclin-Dependent Kinase 9; Cyclin-Dependent Kinases; Drug Screening Assays, Antitumor; Leukemia, Myeloid, Acute; Tumor Suppressor Protein p53; Humans; Tumor Suppressor Protein p53/metabolism; Leukemia, Myeloid, Acute/drug therapy; Leukemia, Myeloid, Acute/metabolism; Leukemia, Myeloid, Acute/pathology; Antineoplastic Agents/pharmacology; Antineoplastic Agents/chemistry; Antineoplastic Agents/chemical synthesis; Casein Kinase Ialpha/metabolism; Casein Kinase Ialpha/antagonists & inhibitors; Cell Proliferation/drug effects; Cyclin-Dependent Kinase 9/antagonists & inhibitors; Cyclin-Dependent Kinase 9/metabolism; Structure-Activity Relationship; Molecular Structure; Cyclin-Dependent Kinases/antagonists & inhibitors; Cyclin-Dependent Kinases/metabolism; Dose-Response Relationship, Drug; Apoptosis/drug effects; Drug Discovery; Cell Line, Tumor; Proteolysis/drug effects; Tumor Cells, Cultured; Proteolysis Targeting Chimera; Cyclin-Dependent Kinase-Activating Kinase

Key words

Acute myeloid leukemia; CDK7/9; CK1α; P53; PROTAC

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Drug Screening Assays, Antitumor / Leukemia, Myeloid, Acute / Tumor Suppressor Protein p53 / Cyclin-Dependent Kinases / Cyclin-Dependent Kinase 9 / Casein Kinase Ialpha / Cell Proliferation / Antineoplastic Agents Limits: Humans Language: En Journal: Bioorg Chem Year: 2024 Type: Article Affiliation country: China

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