PROTACs: great opportunities for academia and industry

X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …

Inhibitors of cyclin-dependent kinases as cancer therapeutics

SR Whittaker, A Mallinger, P Workman… - Pharmacology & …, 2017 - Elsevier
Over the past two decades there has been a great deal of interest in the development of
inhibitors of the cyclin-dependent kinases (CDKs). This attention initially stemmed from …

The mediator complex: at the nexus of RNA polymerase II transcription

C Jeronimo, F Robert - Trends in Cell Biology, 2017 - cell.com
Mediator is an essential, large, multisubunit, transcriptional co-activator highly conserved
across eukaryotes. Mediator interacts with gene-specific transcription factors at enhancers …

Progress in targeted therapeutic drugs for oral squamous cell carcinoma

L Liu, J Chen, X Cai, Z Yao, J Huang - Surgical oncology, 2019 - Elsevier
With the rapid development of biomedicine, people have a deeper understanding with the
biological characteristics of malignant tumors, and begin to notice that in most tumors, there …

[HTML][HTML] Inhibition of CDK8 mediator kinase suppresses estrogen dependent transcription and the growth of estrogen receptor positive breast cancer

MSJ McDermott, AA Chumanevich, C Lim, J Liang… - Oncotarget, 2017 - ncbi.nlm.nih.gov
Hormone therapy targeting estrogen receptor (ER) is the principal treatment for ER-positive
breast cancers. However, many cancers develop resistance to hormone therapy while …

Therapeutic targeting of transcriptional cyclin-dependent kinases

MD Galbraith, H Bender, JM Espinosa - Transcription, 2019 - Taylor & Francis
The fact that many cancer types display transcriptional addiction driven by dysregulation of
oncogenic enhancers and transcription factors has led to increased interest in a group of …

Discovery of potent, selective, and orally bioavailable small-molecule modulators of the mediator complex-associated kinases CDK8 and CDK19

A Mallinger, K Schiemann, C Rink… - Journal of medicinal …, 2016 - ACS Publications
The Mediator complex-associated cyclin-dependent kinase CDK8 has been implicated in
human disease, particularly in colorectal cancer where it has been reported as a putative …

Inhibitors of cyclin-dependent kinases: types and their mechanism of action

P Łukasik, I Baranowska-Bosiacka… - International Journal of …, 2021 - mdpi.com
Recent studies on cyclin-dependent kinase (CDK) inhibitors have revealed that small
molecule drugs have become very attractive for the treatment of cancer and …

Structure-based optimization of potent, selective, and orally bioavailable CDK8 inhibitors discovered by high-throughput screening

P Czodrowski, A Mallinger, D Wienke… - Journal of medicinal …, 2016 - ACS Publications
The mediator complex-associated cyclin dependent kinase CDK8 regulates β-catenin-
dependent transcription following activation of WNT signaling. Multiple lines of evidence …

Development of highly potent and selective steroidal inhibitors and degraders of CDK8

JM Hatcher, ES Wang, L Johannessen… - ACS medicinal …, 2018 - ACS Publications
Cortistatin A is a natural product isolated from the marine sponge Corticium simplex and was
found to be a potent and selective inhibitor of CDK8. Many synthetic groups have reported …