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 …

[HTML][HTML] Inhibiting CDK4/6 in breast cancer with palbociclib, ribociclib, and abemaciclib: similarities and differences

CL Braal, EM Jongbloed, SM Wilting, RHJ Mathijssen… - Drugs, 2021 - Springer
The cyclin-dependent kinase (CDK) 4/6 inhibitors belong to a new class of drugs that
interrupt proliferation of malignant cells by inhibiting progression through the cell cycle …

Cyclin-dependent kinase 4 and 6 inhibitors for hormone receptor-positive breast cancer: past, present, and future

LM Spring, SA Wander, F Andre, B Moy, NC Turner… - The Lancet, 2020 - thelancet.com
The development and approval of cyclin-dependent kinase (CDK) 4 and 6 inhibitors for
hormone receptor-positive and human epidermal growth factor receptor 2 (HER2)-negative …

Leveraging the replication stress response to optimize cancer therapy

E Cybulla, A Vindigni - Nature Reviews Cancer, 2023 - nature.com
High-fidelity DNA replication is critical for the faithful transmission of genetic information to
daughter cells. Following genotoxic stress, specialized DNA damage tolerance pathways …

Cell cycle proteins as promising targets in cancer therapy

T Otto, P Sicinski - Nature Reviews Cancer, 2017 - nature.com
Cancer is characterized by uncontrolled tumour cell proliferation resulting from aberrant
activity of various cell cycle proteins. Therefore, cell cycle regulators are considered …

Discovery of Sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-helical peptide in clinical development

V Guerlavais, TK Sawyer, L Carvajal… - Journal of Medicinal …, 2023 - ACS Publications
We report the discovery of sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-
helical peptide to enter clinical trials. ALRN-6924 is a “stapled peptide” that mimics the N …

Targeting CDK4 and CDK6: from discovery to therapy

CJ Sherr, D Beach, GI Shapiro - Cancer discovery, 2016 - AACR
Biochemical and genetic characterization of D-type cyclins, their cyclin D–dependent
kinases (CDK4 and CDK6), and the polypeptide CDK4/6 inhibitor p16INK4 over two …

The history and future of targeting cyclin-dependent kinases in cancer therapy

U Asghar, AK Witkiewicz, NC Turner… - Nature reviews Drug …, 2015 - nature.com
Cancer represents a pathological manifestation of uncontrolled cell division; therefore, it has
long been anticipated that our understanding of the basic principles of cell cycle control …

The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first-line treatment of oestrogen receptor-positive, HER2 …

RS Finn, JP Crown, I Lang, K Boer… - The lancet …, 2015 - thelancet.com
Summary Background Palbociclib (PD-0332991) is an oral, small-molecule inhibitor of
cyclin-dependent kinases (CDKs) 4 and 6 with preclinical evidence of growth-inhibitory …

Early adaptation and acquired resistance to CDK4/6 inhibition in estrogen receptor–positive breast cancer

MT Herrera-Abreu, M Palafox, U Asghar, MA Rivas… - Cancer research, 2016 - AACR
Small-molecule inhibitors of the CDK4/6 cell-cycle kinases have shown clinical efficacy in
estrogen receptor (ER)-positive metastatic breast cancer, although their cytostatic effects are …