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 …

Chemistries of bifunctional PROTAC degraders

C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …

Cell cycle on the crossroad of tumorigenesis and cancer therapy

J Liu, Y Peng, W Wei - Trends in cell biology, 2022 - cell.com
Aberrancy in cell cycle progression is one of the fundamental mechanisms underlying
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …

Targeted MDM2 degradation reveals a new vulnerability for p53-inactivated triple-negative breast cancer

CM Adams, R Mitra, Y Xiao, P Michener, J Palazzo… - Cancer discovery, 2023 - AACR
Triple-negative breast cancers (TNBC) frequently inactivate p53, increasing their
aggressiveness and therapy resistance. We identified an unexpected protein vulnerability in …

Developments of CRBN-based PROTACs as potential therapeutic agents

C Wang, Y Zhang, Y Wu, D Xing - European journal of medicinal chemistry, 2021 - Elsevier
Protease-targeted chimeras (PROTACs) are a new technology that is receiving much
attention in the treatment of diseases. The mechanism is to inhibit protein function by …

Strategies for designing proteolysis targeting chimaeras (PROTACs)

S He, G Dong, J Cheng, Y Wu… - Medicinal Research …, 2022 - Wiley Online Library
Proteolysis targeting chimaeras (PROTACs) is a cutting edge and rapidly growing technique
for new drug discovery and development. Currently, the largest challenge in the molecular …

Targeting cell-cycle machinery in cancer

JM Suski, M Braun, V Strmiska, P Sicinski - Cancer cell, 2021 - cell.com
Abnormal activity of the core cell-cycle machinery is seen in essentially all tumor types and
represents a driving force of tumorigenesis. Recent studies revealed that cell-cycle proteins …

[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 …