CDK8 and CDK19: positive regulators of signal-induced transcription and negative regulators of Mediator complex proteins
We have conducted a detailed transcriptomic, proteomic and phosphoproteomic analysis of
CDK8 and its paralog CDK19, alternative enzymatic components of the kinase module …
CDK8 and its paralog CDK19, alternative enzymatic components of the kinase module …
Inhibition of CDK8/19 Mediator kinase potentiates HER2-targeting drugs and bypasses resistance to these agents in vitro and in vivo
X Ding, AC Sharko, MSJ McDermott… - Proceedings of the …, 2022 - National Acad Sciences
Breast cancers (BrCas) that overexpress oncogenic tyrosine kinase receptor HER2 are
treated with HER2-targeting antibodies (such as trastuzumab) or small-molecule kinase …
treated with HER2-targeting antibodies (such as trastuzumab) or small-molecule kinase …
Mediator kinase inhibition reverses castration resistance of advanced prostate cancer
Mediator kinases CDK19 and CDK8, pleiotropic regulators of transcriptional reprogramming,
are differentially regulated by androgen signaling, but both kinases are upregulated in …
are differentially regulated by androgen signaling, but both kinases are upregulated in …
[HTML][HTML] The study of a novel CDK8 inhibitor E966-0530–45418 that inhibits prostate cancer metastasis in vitro and in vivo
TY Ho, TY Sung, SL Pan, WJ Huang, KC Hsu… - Biomedicine & …, 2023 - Elsevier
Prostate cancer is a prevalent malignancy among men globally, and androgen deprivation
therapy is the conventional first-line treatment for metastatic prostate cancer. While …
therapy is the conventional first-line treatment for metastatic prostate cancer. While …
Unveiling the impact of CDK8 on tumor progression: mechanisms and therapeutic strategies
X Yin, Z He, K Chen, K Ouyang, C Yang, J Li… - Frontiers in …, 2024 - frontiersin.org
CDK8 is an important member of the cyclin-dependent kinase family associated with
transcription and acts as a key “molecular switch” in the Mediator complex. CDK8 regulates …
transcription and acts as a key “molecular switch” in the Mediator complex. CDK8 regulates …
[HTML][HTML] Design, synthesis, and biological evaluation of indolin-2-one derivatives as novel cyclin-dependent protein kinase 8 (CDK8) inhibitors
Cyclin-dependent protein kinase 8 (CDK8) plays important roles in regulating fibrotic growth
factors and inflammatory signaling pathways. Long-term chronic inflammation of the lungs …
factors and inflammatory signaling pathways. Long-term chronic inflammation of the lungs …
Mediator kinase inhibitors suppress triple-negative breast cancer growth and extend tumor suppression by mTOR and AKT inhibitors
Triple-negative breast cancers (TNBC) are treated primarily by chemotherapy and lack
clinically validated therapeutic targets. In particular, inhibitors of the PI3K/AKT/mTOR …
clinically validated therapeutic targets. In particular, inhibitors of the PI3K/AKT/mTOR …
Cu-Catalyzed Decarboxylative Annulation of N-Phenylglycines with Maleimides: Synthesis of 1H-Pyrrolo[3,4-c]quinoline-1,3(2H)-diones
KH Lv, L Chen, K Zhao, JM Yang… - The Journal of Organic …, 2023 - ACS Publications
A novel protocol for the construction of functionalized 1 H-pyrrolo [3, 4-c] quinoline-1, 3 (2 H)-
diones (PQLs, 3) from N-phenylglycines and maleimides was developed. The cascade …
diones (PQLs, 3) from N-phenylglycines and maleimides was developed. The cascade …
Delocalized quinolinium-macrocyclic peptides, an atypical chemotype for CNS penetration
V Pingitore, J Pancholi, TW Hornsby, J Warne… - Science …, 2024 - science.org
Macrocyclic drugs can address an increasing range of molecular targets but enabling
central nervous system (CNS) access to these drugs has been viewed as an intractable …
central nervous system (CNS) access to these drugs has been viewed as an intractable …
CDK8 inhibitors antagonize HIV-1 reactivation and promote provirus latency in T cells
RM Horvath, ZL Brumme, I Sadowski - Journal of Virology, 2023 - Am Soc Microbiol
Latent HIV-1 provirus represents the barrier toward a cure for infection and is dependent
upon the host RNA Polymerase (Pol) II machinery for reemergence. Here, we find that …
upon the host RNA Polymerase (Pol) II machinery for reemergence. Here, we find that …