The role of CDK pathway dysregulation and its therapeutic potential in soft tissue sarcoma

JT Thiel, A Daigeler, J Kolbenschlag, K Rachunek… - Cancers, 2022 - mdpi.com
Simple Summary Soft tissue sarcomas (STSs) are rare malignant conditions with more than
70 subtypes that are difficult to treat, especially in advanced or metastatic states. Recently …

Focusing on cyclin-dependent kinases 5: A potential target for neurological disorders

Z Tian, B Feng, XQ Wang, J Tian - Frontiers in Molecular …, 2022 - frontiersin.org
Cyclin-dependent kinases 5 (Cdk5) is a special member of proline-directed serine threonine
kinase family. Unlike other Cdks, Cdk5 is not directly involved in cell cycle regulation but …

Discovery and optimization of thieno [3, 2-d] pyrimidine derivatives as highly selective inhibitors of cyclin-dependent kinase 7

H Zhang, G Lin, S Jia, Y Zhang, J Wu, Y Tao… - European Journal of …, 2024 - Elsevier
Targeting cyclin-dependent kinase 7 (CDK7) has emerged as a highly sought-after
therapeutic strategy in oncology due to its duality of function in regulating biological …

Screening through lead optimization of high affinity, allosteric cyclin-dependent kinase 2 (CDK2) inhibitors as male contraceptives that reduce sperm counts in mice

EB Faber, N Wang, K John, L Sun… - Journal of medicinal …, 2023 - ACS Publications
Although cyclin-dependent kinase 2 (CDK2) is a validated target for both cancer and
contraception, developing a CDK2 inhibitor with exquisite selectivity has been challenging …

Ligand-and structure-based identification of novel CDK9 inhibitors for the potential treatment of leukemia

H Zhang, J Huang, R Chen, H Cai, Y Chen, S He… - Bioorganic & Medicinal …, 2022 - Elsevier
Abstract Cyclin-dependent kinase 9 (CDK9) plays a vital role in controlling cell transcription
and has been an attractive target for cancer treatment. Herein, ten predictive models derived …

Selective mono-N-methylation of amines using methanol as a methylating reagent over heterogeneous Ni catalysts

P Wang, Z Yuan, C Xian, B Liu, X Li… - Catalysis Science & …, 2023 - pubs.rsc.org
Mono-N-methyl functionalization is one kind of important organic transformation, as mono N-
methylamines are present in a variety of pharmaceutical and agrochemical applications. The …

Effects of super-enhancers in cancer metastasis: mechanisms and therapeutic targets

S Liu, W Dai, B Jin, F Jiang, H Huang, W Hou, J Lan… - Molecular Cancer, 2024 - Springer
Metastasis remains the principal cause of cancer-related lethality despite advancements in
cancer treatment. Dysfunctional epigenetic alterations are crucial in the metastatic cascade …

Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2)

M Zeng, JM Grandner, MC Bryan, V Verma… - ACS Medicinal …, 2023 - ACS Publications
Cyclin-dependent kinases (CDKs) are key regulators of the cell cycle and are frequently
altered in cancer cells, thereby leading to uncontrolled proliferation. In this context, CDK2 …

Design and Synthesis of Novel Macrocyclic Derivatives as Potent and Selective Cyclin-Dependent Kinase 7 Inhibitors

P Niu, Y Tao, G Lin, H Xu, Q Meng, K Yang… - Journal of Medicinal …, 2024 - ACS Publications
The duality of function (cell cycle regulation and gene transcription) of cyclin-dependent
kinase 7 (CDK7) makes it an attractive oncology target and the discovery of CDK7 inhibitors …

Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia

XX Zhang, YY Yan, X Ma, Y Xiao, CC Lei… - European Journal of …, 2023 - Elsevier
CDK8 plays a key role in acute myeloid leukemia, colorectal cancer and other cancers.
Here, a total of 54 compounds were designed and synthesized. Among them, the most …