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 …

Targeting cyclin-dependent kinases in human cancers: from small molecules to peptide inhibitors

M Peyressatre, C Prével, M Pellerano, MC Morris - Cancers, 2015 - mdpi.com
Cyclin-dependent kinases (CDK/Cyclins) form a family of heterodimeric kinases that play
central roles in regulation of cell cycle progression, transcription and other major biological …

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 …

Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs

R Roskoski Jr - Pharmacological research, 2016 - Elsevier
Cyclins and cyclin-dependent protein kinases (CDKs) are important regulatory components
that are required for cell cycle progression. The levels of the cell cycle CDKs are generally …

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 …

Selective degradation of CDK6 by a palbociclib based PROTAC

S Rana, M Bendjennat, S Kour, HM King… - Bioorganic & medicinal …, 2019 - Elsevier
Abstract Development of selective kinase inhibitors that target the ATP binding site
continues to be a challenge largely due to similar binding pockets. Palbociclib is a cyclin …

Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity

J Bian, J Ren, Y Li, J Wang, X Xu, Y Feng, H Tang… - Bioorganic …, 2018 - Elsevier
Wogonin is a natural product isolated from the Scutellaria baicalensis and has been proved
to be a potent and selective inhibitor of CDK9. Using this scaffold, we designed and …

CDK9 inhibitors in acute myeloid leukemia

S Boffo, A Damato, L Alfano, A Giordano - Journal of Experimental & …, 2018 - Springer
Current treatment for acute myeloid leukemia (AML) is less than optimal, but increased
understanding of disease pathobiology and genomics has led to clinical investigation of …

The Yin and Yang of P-TEFb regulation: implications for human immunodeficiency virus gene expression and global control of cell growth and differentiation

Q Zhou, JHN Yik - Microbiology and Molecular Biology Reviews, 2006 - Am Soc Microbiol
The positive transcription elongation factor b (P-TEFb) stimulates transcriptional elongation
by phosphorylating the carboxy-terminal domain of RNA polymerase II and antagonizing the …

CDK9: A key player in cancer and other diseases

LC Franco, F Morales, S Boffo… - Journal of Cellular …, 2018 - Wiley Online Library
Abstract Cyclin‐Dependent Kinase 9 (CDK9) is part of a functional diverse group of
enzymes responsible for cell cycle control and progression. It associates mainly with Cyclin …