Overcoming CDK4/6 inhibitor resistance in ER-positive breast cancer

N Portman, S Alexandrou, E Carson… - Endocrine-related …, 2019 - erc.bioscientifica.com
Three inhibitors of CDK4/6 kinases were recently FDA approved for use in combination with
endocrine therapy, and they significantly increase the progression-free survival of patients …

Lessons learned from past cyclin-dependent kinase drug discovery efforts

Z Xie, S Hou, X Yang, Y Duan, J Han… - Journal of Medicinal …, 2022 - ACS Publications
Inhibition of cyclin-dependent kinases (CDKs) has become an effective therapeutic strategy
for treating various diseases, especially cancer. Over almost three decades, although great …

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 …

Pd-catalyzed cross-couplings: On the importance of the catalyst quantity descriptors, mol% and ppm

CS Horbaczewskyj, IJS Fairlamb - Organic Process Research & …, 2022 - ACS Publications
This Review examines parts per million (ppm) palladium concentrations in catalytic cross-
coupling reactions and their relationship with mole percentage (mol%). Most studies in …

[HTML][HTML] Selective inhibition of CDK4/6: A safe and effective strategy for developing anticancer drugs

K Yuan, X Wang, H Dong, W Min, H Hao… - … Pharmaceutica Sinica B, 2021 - Elsevier
The sustained cell proliferation resulting from dysregulation of the cell cycle and activation of
cyclin-dependent kinases (CDKs) is a hallmark of cancer. The inhibition of CDKs is a highly …

Synthesis of monofluoroalkenes: a leap forward

M Drouin, JD Hamel, JF Paquin - Synthesis, 2018 - thieme-connect.com
Monofluoroalkenes have found wide application in organic chemistry, medicinal chemistry,
and materials science. This review summarizes the most recent advances made regarding …

[HTML][HTML] Antiproliferative activity of thiazole and oxazole derivatives: A systematic review of in vitro and in vivo studies

NY Guerrero-Pepinosa, MC Cardona-Trujillo… - Biomedicine & …, 2021 - Elsevier
Thiazole and oxazole are compounds with a heterocyclic nucleus that have attracted the
attention of medicinal chemistry due to the great variety of biological activities that they …

Design and synthesis of 3-(4-pyridyl)-5-(4-sulfamido-phenyl)-1, 2, 4-oxadiazole derivatives as novel GSK-3β inhibitors and evaluation of their potential as …

M Wang, T Liu, S Chen, M Wu, J Han, Z Li - European Journal of Medicinal …, 2021 - Elsevier
Pleiotropic intervention has prominent advantages for complex pathomechanisms, such as
Alzheimer's disease (AD). In this study, a series of novel 3-(4-pyridyl)-5-(4-sulfamido-phenyl) …

CDK4/6 inhibitors: a brief overview and prospective research directions

T Adon, D Shanmugarajan, HY Kumar - RSC advances, 2021 - pubs.rsc.org
The discovery of cyclin-dependent kinases (CDK) and their mechanism in regulating the cell
cycle process was considered a game-changer in cancer therapy. Cell cycle arrest and …

Recent progress in CDK4/6 inhibitors and PROTACs

H Wang, J Ba, Y Kang, Z Gong, T Liang, Y Zhang, J Qi… - Molecules, 2023 - mdpi.com
Cell division in eukaryotes is a highly regulated process that is critical to the life of a cell.
Dysregulated cell proliferation, often driven by anomalies in cell Cyclin-dependent kinase …