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 …
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
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …
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 …
protein degradation (TPD) have advanced to clinical trials, with an initial focus on …
Applications of covalent chemistry in targeted protein degradation
Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …
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 …
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 …
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 …
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 …
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
Recently, targeted degradation has emerged as a powerful therapeutic modality. Relying on
“event-driven” pharmacology, proteolysis targeting chimeras (PROTACs) can degrade …
“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 …
proximity of an E3 ubiquitin ligase, promoting POI ubiquitylation and proteasomal …