Cyclin-dependent kinase 2 inhibitors in cancer therapy: an update

S Tadesse, EC Caldon, W Tilley… - Journal of medicinal …, 2018 - ACS Publications
Cyclin-dependent kinase 2 (CDK2) drives the progression of cells into the S-and M-phases
of the cell cycle. CDK2 activity is largely dispensable for normal development, but it is …

Overview of CDK9 as a target in cancer research

F Morales, A Giordano - Cell cycle, 2016 - Taylor & Francis
ABSTRACT CDK9 is a protein in constant development in cancer therapy. Herein we
present an overview of the enzyme as a target for cancer therapy. We provide data on its …

Targeting CDK9 reactivates epigenetically silenced genes in cancer

H Zhang, S Pandey, M Travers, H Sun, G Morton… - Cell, 2018 - cell.com
Summary Cyclin-dependent kinase 9 (CDK9) promotes transcriptional elongation through
RNAPII pause release. We now report that CDK9 is also essential for maintaining gene …

CDK1 structures reveal conserved and unique features of the essential cell cycle CDK

NR Brown, S Korolchuk, MP Martin, WA Stanley… - Nature …, 2015 - nature.com
CDK1 is the only essential cell cycle CDK in human cells and is required for successful
completion of M-phase. It is the founding member of the CDK family and is conserved across …

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 …

Differences in the conformational energy landscape of CDK1 and CDK2 suggest a mechanism for achieving selective CDK inhibition

DJ Wood, S Korolchuk, NJ Tatum, LZ Wang… - Cell chemical …, 2019 - cell.com
Dysregulation of the cell cycle characterizes many cancer subtypes, providing a rationale for
develo** cyclin-dependent kinase (CDK) inhibitors. Potent CDK2 inhibitors might target …

Cyclin dependent kinase 9 inhibitors for cancer therapy: miniperspective

YA Sonawane, MA Taylor, JV Napoleon… - Journal of medicinal …, 2016 - ACS Publications
Cyclin dependent kinase (CDK) inhibitors have been the topic of intense research for nearly
2 decades due to their widely varied and critical functions within the cell. Recently CDK9 has …

Recent developments in the biology and medicinal chemistry of CDK9 inhibitors: an update

T Wu, Z Qin, Y Tian, J Wang, C Xu, Z Li… - Journal of medicinal …, 2020 - ACS Publications
Cyclin-dependent kinase 9 (CDK9), which regulates transcriptional elongation, is an
attractive therapeutic target for many cancers, especially for cancers driven by transcriptional …

Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures

W Cheng, Z Yang, S Wang, Y Li, H Wei, X Tian… - European journal of …, 2019 - Elsevier
The cyclin-dependent protein kinases (CDKs) are protein-serine/threonine kinases that
display crucial effects in regulation of cell cycle and transcription. While the excessive …

The XChemExplorer graphical workflow tool for routine or large-scale protein–ligand structure determination

T Krojer, R Talon, N Pearce, P Collins… - Biological …, 2017 - journals.iucr.org
XChemExplorer (XCE) is a data-management and workflow tool to support large-scale
simultaneous analysis of protein–ligand complexes during structure-based ligand discovery …