Emerging strategies to target RAS signaling in human cancer therapy

K Chen, Y Zhang, L Qian, P Wang - Journal of hematology & oncology, 2021 - Springer
Abstract RAS mutations (HRAS, NRAS, and KRAS) are among the most common
oncogenes, and around 19% of patients with cancer harbor RAS mutations. Cells harboring …

Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation

MJ Bond, CM Crews - RSC chemical biology, 2021 - pubs.rsc.org
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …

Delivering on the promise of protein degraders

MN O'Brien Laramy, S Luthra, MF Brown… - Nature Reviews Drug …, 2023 - nature.com
Over the past 3 years, the first bivalent protein degraders intentionally designed for targeted
protein degradation (TPD) have advanced to clinical trials, with an initial focus on …

Applications of covalent chemistry in targeted protein degradation

D Lu, X Yu, H Lin, R Cheng, EY Monroy, X Qi… - Chemical Society …, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …

The rise of covalent proteolysis targeting chimeras

R Gabizon, N London - Current opinion in chemical biology, 2021 - Elsevier
Targeted protein degradation offers several advantages over direct inhibition of protein
activity and is gaining increasing interest in chemical biology and drug discovery …

Opportunities and challenges of protein-based targeted protein degradation

F Shen, LMK Dassama - Chemical Science, 2023 - pubs.rsc.org
In the 20 years since the first report of a proteolysis targeting chimeric (PROTAC) molecule,
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …

A comprehensive overview of small-molecule androgen receptor degraders: Recent progress and future perspectives

S Ha, G Luo, H Xiang - Journal of medicinal chemistry, 2022 - ACS Publications
Prostate cancer (PC), the second most prevalent malignancy in men worldwide, has been
proven to depend on the aberrant activation of androgen receptor (AR) signaling. Long-term …

Post-translational modification of RAS proteins

SL Campbell, MR Philips - Current opinion in structural biology, 2021 - Elsevier
Mutations of RAS genes drive cancer more frequently than any other oncogene. RAS
proteins integrate signals from a wide array of receptors and initiate downstream signaling …

Lipid-mediated intracellular delivery of recombinant bioPROTACs for the rapid degradation of undruggable proteins

A Chan, RM Haley, MA Najar… - Nature …, 2024 - nature.com
Recently, targeted degradation has emerged as a powerful therapeutic modality. Relying on
“event-driven” pharmacology, proteolysis targeting chimeras (PROTACs) can degrade …

Target protein localization and its impact on PROTAC-mediated degradation

LM Simpson, L Glennie, A Brewer, JF Zhao… - Cell Chemical …, 2022 - cell.com
Proteolysis-targeting chimeras (PROTACs) bring a protein of interest (POI) into spatial
proximity of an E3 ubiquitin ligase, promoting POI ubiquitylation and proteasomal …