CDK

Proteomic and Phosphoproteomic Profiling Reveals the Oncogenic Role of Protein Kinase D Family Kinases in Cholangiocarcinoma

94 views | Feb 15 2024

The comprehensive analysis of protein and phosphorylation signatures in cholangiocarcinoma revealed the PRKD family's pivotal role, highlighting their potential as novel treatment targets validated by the inhibitory effects of 1-naphthyl PP1 on CCA cell proliferation, migration, and invasion. [Read the Full Post]

Targeting CDK9 with selective inhibitors or degraders in tumor therapy: an overview of recent developments

0 views | Dec 30 2023

Research into selective CDK9 inhibitors and PROTAC degraders shows promise in targeting specific tumor genotypes, with VIP152 demonstrating efficacy in advanced high-grade lymphoma and solid tumors, highlighting the potential for precision cancer therapy. [Read the Full Post]

CCT251545 enhances drug delivery and potentiates chemotherapy in multidrug-resistant cancers by Rac1-mediated macropinocytosis

57 views | Dec 30 2023

The study's findings suggest that CCT251545 in combination with chemotherapy demonstrates a potent synergistic effect by enhancing drug uptake through Rac1-dependent macropinocytosis and elevating NAD levels, providing a promising avenue for managing multidrug-resistant cancers. [Read the Full Post]

Degradation of Cyclin-Dependent Kinase 9/Cyclin T1 by Optimized Microtubule-Associated Protein 1 Light Chain 3 Beta-Recruiting Coumarin Analogs

53 views | Dec 24 2023

Researchers systematically optimized coumarin analogs linked with the CDK9 inhibitor SNS-032, potentially enabling simultaneous binding to CDK9 and LC3B, initiating selective autophagic degradation and demonstrating potential for treating diseases associated with intracellular pathogenic proteins. [Read the Full Post]

AZD5438 a GSK-3a/b and CDK inhibitor is antiapoptotic modulates mitochondrial activity and protects human neurons from mitochondrial toxins

0 views | Dec 23 2023

AZD5438, inhibiting CDKs and GSK-3a/b, emerges as a promising compound, showcasing potent neuroprotective effects by preventing mitochondrial dysfunction and neuronal damage induced by rotenone in human neurons, suggesting its potential therapeutic significance. [Read the Full Post]

Drug repurposing and structure-based discovery of new PDE4 and PDE5 inhibitors

44 views | Dec 17 2023

The study utilized high-throughput drug repurposing screening and structure-based drug design to identify novel PDE4 inhibitors, leading to the unexpected discovery of a dual PDE4/PDE5 inhibitor (CVT-313) and the subsequent development of a highly selective PDE5 inhibitor (compound 2), exemplifying the efficiency of this integrated approach in drug discovery. [Read the Full Post]

Cyclin-dependent kinase 6 (CDK6) as a potent regulator of the ovarian primordial-to-primary follicle transition

26 views | Dec 11 2023

The study reveals that CDK6 inhibition using BSJ disrupts the primordial-to-primary follicle transition, emphasizing the crucial role of precise cell cycle regulation in ovarian follicle development and suggesting potential implications for fertility-related interventions. [Read the Full Post]

Straightforward Access to a New Class of Dual DYRK1A/CLK1 Inhibitors Possessing a Simple Dihydroquinoline Core

17 views | Dec 10 2023

In this study, a novel class of dihydroquinolines was developed, exhibiting potent inhibitory activities in the nanomolar range against DYRK1A and CLK1, two kinases implicated in Alzheimer's disease and Down syndrome, with the most potent inhibitor also demonstrating antioxidant and radical scavenging properties. [Read the Full Post]

A live-cell image-based machine learning strategy for reducing variability in PSC differentiation systems

20 views | Dec 09 2023

Harnessing live-cell bright-field imaging and machine learning, this study enables real-time recognition of diverse cell types, predictive assessment of differentiation efficiency, and iterative optimization of pluripotent stem cell differentiation, ensuring consistent high efficiency across cell lines and batches for biomedical applications. [Read the Full Post]

Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor

16 views | Dec 02 2023

Compound 40 (JSH-150) is a highly selective CDK9 kinase inhibitor with an IC50 of 1 nM, demonstrating potent antiproliferative effects across multiple cancer cell lines, robust in vivo efficacy, and a promising pharmacological tool and drug candidate for leukemia and other cancers. [Read the Full Post]