Targeting CDK4 and CDK6 in cancer

S Goel, JS Bergholz, JJ Zhao - Nature Reviews Cancer, 2022 - nature.com
Abstract Cyclin-dependent kinase 4 (CDK4) and CDK6 are critical mediators of cellular
transition into S phase and are important for the initiation, growth and survival of many …

CDK4 and CDK6 kinases: From basic science to cancer therapy

A Fassl, Y Geng, P Sicinski - Science, 2022 - science.org
BACKGROUND Cyclins and cyclin-dependent kinases (CDKs) drive cell division. Of
particular importance to the cancer field are D-cyclins, which activate CDK4 and CDK6. In …

Targeting oncogene and non-oncogene addiction to inflame the tumour microenvironment

G Petroni, A Buqué, LM Coussens… - Nature reviews Drug …, 2022 - nature.com
Immune checkpoint inhibitors (ICIs) have revolutionized the clinical management of multiple
tumours. However, only a few patients respond to ICIs, which has generated considerable …

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 …

Combination Therapies with CDK4/6 Inhibitors to Treat KRAS-Mutant Pancreatic Cancer

CM Goodwin, AM Waters, JE Klomp, S Javaid… - Cancer research, 2023 - AACR
Mutational loss of CDKN2A (encoding p16INK4A) tumor-suppressor function is a key
genetic step that complements activation of KRAS in promoting the development and …

Reversible lysine-targeted probes reveal residence time-based kinase selectivity

T Yang, A Cuesta, X Wan, GB Craven… - Nature chemical …, 2022 - nature.com
The expansion of the target landscape of covalent inhibitors requires the engagement of
nucleophiles beyond cysteine. Although the conserved catalytic lysine in protein kinases is …

Single-cell morphological and topological atlas reveals the ecosystem diversity of human breast cancer

S Zhao, DP Chen, T Fu, JC Yang, D Ma, XZ Zhu… - Nature …, 2023 - nature.com
Digital pathology allows computerized analysis of tumor ecosystem using whole slide
images (WSIs). Here, we present single-cell morphological and topological profiling (sc …

[HTML][HTML] CDK4: a master regulator of the cell cycle and its role in cancer

SJ Baker, PI Poulikakos, HY Irie, S Parekh… - Genes & …, 2022 - ncbi.nlm.nih.gov
The cell cycle is regulated in part by cyclins and their associated serine/threonine cyclin-
dependent kinases, or CDKs. CDK4, in conjunction with the D-type cyclins, mediates …

[HTML][HTML] Cancer takes many paths through G1/S

ES Knudsen, AK Witkiewicz, SM Rubin - Trends in Cell Biology, 2024 - cell.com
In the commonly accepted paradigm for control of the mammalian cell cycle, sequential
cyclin-dependent kinase (CDK) and cyclin activities drive the orderly transition from G1 to S …

Emerging systemic therapy options beyond CDK4/6 inhibitors for hormone receptor-positive HER2-negative advanced breast cancer

J Ma, JJ Chan, CH Toh, YS Yap - NPJ Breast Cancer, 2023 - nature.com
Endocrine therapy (ET) with cyclin-dependent kinase 4/6 inhibitor (CDK4/6i) is currently the
standard first-line treatment for most patients with hormone receptor (HR) positive, human …