A unified model for the G1/S cell cycle transition

S Hume, GL Dianov, K Ramadan - Nucleic acids research, 2020 - academic.oup.com
Efficient S phase entry is essential for development, tissue repair, and immune defences.
However, hyperactive or expedited S phase entry causes replication stress, DNA damage …

Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015–2019)

C Sánchez-Martínez, MJ Lallena… - Bioorganic & medicinal …, 2019 - Elsevier
Sustained proliferative capacity and gene dysregulation are hallmarks of cancer. In
mammalian cells, cyclin-dependent kinases (CDKs) control critical cell cycle checkpoints …

Rapid adaptation to CDK2 inhibition exposes intrinsic cell-cycle plasticity

M Arora, J Moser, TE Hoffman, LP Watts, M Min… - Cell, 2023 - cell.com
CDK2 is a core cell-cycle kinase that phosphorylates many substrates to drive progression
through the cell cycle. CDK2 is hyperactivated in multiple cancers and is therefore an …

Structure of the human Mediator–RNA polymerase II pre-initiation complex

S Rengachari, S Schilbach, S Aibara, C Dienemann… - Nature, 2021 - nature.com
Mediator is a conserved coactivator complex that enables the regulated initiation of
transcription at eukaryotic genes,–. Mediator is recruited by transcriptional activators and …

p27 allosterically activates cyclin-dependent kinase 4 and antagonizes palbociclib inhibition

KZ Guiley, JW Stevenson, K Lou, KJ Barkovich… - Science, 2019 - science.org
INTRODUCTION The cyclin D (CycD)–dependent kinases CDK4 and CDK6 (CDK4/6)
phosphorylate the retinoblastoma (Rb) tumor suppressor protein to cause entry into the cell …

The application and prospect of CDK4/6 inhibitors in malignant solid tumors

Q Du, X Guo, M Wang, Y Li, X Sun, Q Li - Journal of hematology & …, 2020 - Springer
Abstract Cyclin-dependent kinase 4/6 (CDK4/6) inhibitors, which block the transition from the
G1 to S phase of the cell cycle by interfering with Rb phosphorylation and E2F release, have …

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 …

A critical evaluation of protein kinase regulation by activation loop autophosphorylation

R Reinhardt, TA Leonard - Elife, 2023 - elifesciences.org
Phosphorylation of proteins is a ubiquitous mechanism of regulating their function,
localization, or activity. Protein kinases, enzymes that use ATP to phosphorylate protein …

Ligand binding remodels protein side-chain conformational heterogeneity

SA Wankowicz, SH de Oliveira, DW Hogan… - Elife, 2022 - elifesciences.org
While protein conformational heterogeneity plays an important role in many aspects of
biological function, including ligand binding, its impact has been difficult to quantify …

Target protein degradation by protacs: A budding cancer treatment strategy

D Choudhary, A Kaur, P Singh, G Chaudhary… - Pharmacology & …, 2023 - Elsevier
Cancer is one of the most common causes of death. So, its lethal effect increases with time.
Near about hundreds of cancers are known in humans. Cancer treatment is done to cure or …