Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …
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 …
C Wang, Y Zhang, Y Wu, D Xing - European journal of medicinal chemistry, 2021 - Elsevier
Protease-targeted chimeras (PROTACs) are a new technology that is receiving much attention in the treatment of diseases. The mechanism is to inhibit protein function by …
AT Anshabo, R Milne, S Wang, H Albrecht - Frontiers in oncology, 2021 - frontiersin.org
Cyclin-dependent kinases (CDKs) are proteins pivotal to a wide range of cellular functions, most importantly cell division and transcription, and their dysregulations have been …
S He, G Dong, J Cheng, Y Wu… - Medicinal Research …, 2022 - Wiley Online Library
Proteolysis targeting chimaeras (PROTACs) is a cutting edge and rapidly growing technique for new drug discovery and development. Currently, the largest challenge in the molecular …
CM Robb, JI Contreras, S Kour, MA Taylor… - Chemical …, 2017 - pubs.rsc.org
Cyclin-dependent kinase 9 (CDK9), a member of the cyclin-dependent protein kinase (CDK) family, is involved in transcriptional elongation of several target genes. CDK9 is ubiquitously …
R Mandal, S Becker, K Strebhardt - Cancers, 2021 - mdpi.com
Simple Summary CDK9, in combination with Cyclin T1, is one of the major regulators of RNA Polymerase II mediated productive transcription of critical genes in any cell. The activity of …
Z Xie, S Hou, X Yang, Y Duan, J Han… - Journal of Medicinal …, 2022 - ACS Publications
Inhibition of cyclin-dependent kinases (CDKs) has become an effective therapeutic strategy for treating various diseases, especially cancer. Over almost three decades, although great …
B Barlaam, R Casella, J Cidado, C Cook… - Journal of Medicinal …, 2020 - ACS Publications
A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the …