Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

CJ Diehl, A Ciulli - Chemical Society Reviews, 2022 - pubs.rsc.org
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

[HTML][HTML] Breast cancer development and progression: Risk factors, cancer stem cells, signaling pathways, genomics, and molecular pathogenesis

Y Feng, M Spezia, S Huang, C Yuan, Z Zeng, L Zhang… - Genes & diseases, 2018 - Elsevier
As the most commonly occurring cancer in women worldwide, breast cancer poses a
formidable public health challenge on a global scale. Breast cancer consists of a group of …

[HTML][HTML] Selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) in cancer treatment

HK Patel, T Bihani - Pharmacology & therapeutics, 2018 - Elsevier
Breast cancer is the most frequently diagnosed cancer in women, with estrogen receptor
positive (ER+) breast cancer making up approximately 75% of all breast cancers diagnosed …

[HTML][HTML] Genetic markers in triple-negative breast cancer

Z Sporikova, V Koudelakova, R Trojanec… - Clinical breast cancer, 2018 - Elsevier
Triple-negative breast cancer (TNBC) accounts for 15% to 20% of breast cancer cases and
is characterized by the absence of estrogen, progesterone, and human epidermal growth …

Cyclin-dependent kinase 4/6 inhibitors in breast cancer: palbociclib, ribociclib, and abemaciclib

D Kwapisz - Breast cancer research and treatment, 2017 - Springer
Purpose The cyclin D-cyclin dependent kinase (CDK) 4/6-inhibitor of CDK4 (INK4)-
retinoblastoma (Rb) pathway plays a crucial role in cell cycle progression and its …

Real-world study of overall survival with palbociclib plus aromatase inhibitor in HR+/HER2− metastatic breast cancer

HS Rugo, A Brufsky, X Liu, B Li, L McRoy, C Chen… - NPJ Breast …, 2022 - nature.com
Data on real-world effectiveness of cyclin-dependent kinase 4/6 inhibitor combination
therapy versus endocrine therapy alone are limited. The Flatiron Health Analytic Database …

Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders

C Steinebach, YLD Ng, I Sosič, CS Lee, S Chen… - Chemical …, 2020 - pubs.rsc.org
Cyclin-dependent kinase 6 (CDK6) is an important regulator of the cell cycle. Together with
CDK4, it phosphorylates and inactivates retinoblastoma (Rb) protein. In tumour cells, CDK6 …

[HTML][HTML] Mechanisms of sensitivity and resistance to CDK4/CDK6 inhibitors in hormone receptor-positive breast cancer treatment

A Glaviano, SA Wander, RD Baird, KCH Yap… - Drug Resistance …, 2024 - Elsevier
Cell cycle dysregulation is a hallmark of cancer that promotes eccessive cell division. Cyclin-
dependent kinase 4 (CDK4) and cyclin-dependent kinase 6 (CDK6) are key molecules in …

[HTML][HTML] Cyclin-dependent kinases 4/6 inhibitors in breast cancer: current status, resistance, and combination strategies

Y Niu, J Xu, T Sun - Journal of Cancer, 2019 - ncbi.nlm.nih.gov
Dysregulated activation of the cyclin-dependent kinases (CDKs) 4/6, leading to uncontrolled
cell division, is hallmark of cancers. Further study of the cell cycle will advance the cancer …

[HTML][HTML] Combination of palbociclib with navitoclax based-therapies enhances in vivo antitumoral activity in triple-negative breast cancer

A Estepa-Fernández, A García-Fernández… - Pharmacological …, 2023 - Elsevier
Triple-negative breast cancer (TNBC) is a very aggressive subtype of breast cancer with a
poor prognosis and limited effective therapeutic options. Induction of senescence, arrest of …