Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis

CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

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 …

The cell cycle: a review of regulation, deregulation and therapeutic targets in cancer

K Vermeulen, DR Van Bockstaele… - Cell …, 2003 - Wiley Online Library
The cell cycle is controlled by numerous mechanisms ensuring correct cell division. This
review will focus on these mechanisms, ie regulation of cyclin‐dependent kinases (CDK) by …

Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts

DW Fry, PJ Harvey, PR Keller, WL Elliott… - Molecular cancer …, 2004 - AACR
PD 0332991 is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4)(IC50, 0.011
μmol/L) and Cdk6 (IC50, 0.016 μmol/L), having no activity against a panel of 36 additional …

Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer

KD Freeman-Cook, RL Hoffman… - Journal of medicinal …, 2021 - ACS Publications
Control of the cell cycle through selective pharmacological inhibition of CDK4/6 has proven
beneficial in the treatment of breast cancer. Extending this level of control to additional cell …

Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6

PL Toogood, PJ Harvey, JT Repine… - Journal of medicinal …, 2005 - ACS Publications
A pharmacological approach to inhibition of cyclin-dependent kinases 4 and 6 (Cdk4/6)
using highly selective small molecule inhibitors has the potential to provide novel cancer …

Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment …

PG Wyatt, AJ Woodhead, V Berdini… - Journal of medicinal …, 2008 - ACS Publications
The application of fragment-based screening techniques to cyclin dependent kinase 2
(CDK2) identified multiple (> 30) efficient, synthetically tractable small molecule hits for …

Pharmacological inhibitors of cyclin-dependent kinases

M Knockaert, P Greengard, L Meijer - Trends in pharmacological sciences, 2002 - cell.com
Cyclin-dependent kinases (CDKs) regulate the cell division cycle, apoptosis, transcription
and differentiation in addition to functions in the nervous system. Deregulation of CDKs in …

[HTML][HTML] Selective inhibition of CDK4/6: A safe and effective strategy for developing anticancer drugs

K Yuan, X Wang, H Dong, W Min, H Hao… - … Pharmaceutica Sinica B, 2021 - Elsevier
The sustained cell proliferation resulting from dysregulation of the cell cycle and activation of
cyclin-dependent kinases (CDKs) is a hallmark of cancer. The inhibition of CDKs is a highly …

Large-scale proteomics analysis of the human kinome

FS Oppermann, F Gnad, JV Olsen… - Molecular & Cellular …, 2009 - ASBMB
Members of the human protein kinase superfamily are the major regulatory enzymes
involved in the activity control of eukaryotic signal transduction pathways. As protein kinases …