Precision therapeutics and emerging strategies for HR-positive metastatic breast cancer

MR Lloyd, K Jhaveri, K Kalinsky, A Bardia… - Nature Reviews …, 2024 - nature.com
Anti-oestrogen-based therapies, often combined with a CDK4/6 inhibitor, are the current
standard-of-care first-line therapy for patients with advanced-stage hormone receptor …

[HTML][HTML] The Pivotal Role of Preclinical Animal Models in Anti-Cancer Drug Discovery and Personalized Cancer Therapy Strategies

H Guo, X Xu, J Zhang, Y Du, X Yang, Z He, L Zhao… - Pharmaceuticals, 2024 - mdpi.com
The establishment and utilization of preclinical animal models constitute a pivotal aspect
across all facets of cancer research, indispensably contributing to the comprehension of …

Resistance mechanisms and therapeutic strategies of CDK4 and CDK6 kinase targeting in cancer

JJ Asciolla, X Wu, C Adamopoulos, E Gavathiotis… - Nature Cancer, 2025 - nature.com
Abstract Cyclin-dependent kinases (CDKs) 4 and 6 (CDK4/6) are important regulators of the
cell cycle. Selective CDK4/6 small-molecule inhibitors have shown clinical activity in …

CDK4/6 inhibitors: The Devil is in the Detail

T Magge, S Rajendran, AM Brufsky, J Foldi - Current Oncology Reports, 2024 - Springer
Purpose of review Update on the most recent clinical evidence on CDK4/6 inhibitors
(CDK4/6i) in the treatment of hormone receptor (HR)-positive, human epidermal growth …

An allosteric cyclin E-CDK2 site mapped by paralog hop** with covalent probes

Y Zhang, Z Liu, M Hirschi, O Brodsky… - Nature Chemical …, 2024 - nature.com
More than half of the~ 20,000 protein-encoding human genes have paralogs. Chemical
proteomics has uncovered many electrophile-sensitive cysteines that are exclusive to …

Cyclin-dependent kinase 2 (CDK2) inhibitors and others novel CDK inhibitors (CDKi) in breast cancer: clinical trials, current impact, and future directions

R Gerosa, R De Sanctis, F Jacobs, C Benvenuti… - Critical Reviews in …, 2024 - Elsevier
Aberrant cyclin-dependent kinase 2 (CDK2) activation has been identified as a main
resistance mechanism to CDK4/6 inhibition in hormone-positive (HR+) breast cancer …

Chemogenomics for NR1 nuclear hormone receptors

L Isigkeit, E Schallmayer, R Busch, L Brunello… - Nature …, 2024 - nature.com
Nuclear receptors (NRs) regulate transcription in response to ligand binding and NR
modulation allows pharmacological control of gene expression. Although some NRs are …

Structure-Based Drug Design of 2-Amino-[1,1′-biphenyl]-3-carboxamide Derivatives as Selective PKMYT1 Inhibitors for the Treatment of CCNE1-Amplified Breast …

C Wang, Y Fang, Z Zhou, Z Liu, F Feng… - Journal of Medicinal …, 2024 - ACS Publications
CCNE1 amplification occurs in breast cancer and currently lacks effective therapies.
PKMYT1 as a synthetic lethal target for CCNE1 amplification holds promise for the treatment …

Targeting CDK2 to combat drug resistance in cancer therapy

S Kasirzadeh, JL Lenjisa, S Wang - Future Oncology, 2024 - Taylor & Francis
Drug resistance remains a major obstacle in cancer treatment, leading to treatment failures
and high mortality rates. Despite advancements in therapies, overcoming resistance …

Breaking through therapeutic barriers: Insights into CDK4/6 inhibition resistance in hormone receptor-positive metastatic breast Cancer

Y Zheng, Z Zhang, D Li, R Huang, S Ning - Biochimica et Biophysica Acta …, 2024 - Elsevier
The therapeutic landscape for hormone receptor-positive (HR+) breast carcinoma has
undergone a significant transformation with the advent of cyclin-dependent kinase (CDK) 4/6 …