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 …

Kinase inhibitors: the road ahead

FM Ferguson, NS Gray - Nature reviews Drug discovery, 2018 - nature.com
Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …

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 …

Developments of CRBN-based PROTACs as potential therapeutic agents

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 …

CDK9: a comprehensive review of its biology, and its role as a potential target for anti-cancer agents

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 …

Strategies for designing proteolysis targeting chimaeras (PROTACs)

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 …

Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)

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 …

Targeting CDK9 for anti-cancer therapeutics

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 …

Lessons learned from past cyclin-dependent kinase drug discovery efforts

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 …

Discovery of AZD4573, a potent and selective inhibitor of CDK9 that enables short duration of target engagement for the treatment of hematological malignancies

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 …