[HTML][HTML] Small-molecule approaches to targeted protein degradation

TB Faust, KA Donovan, H Yue… - Annual Review of …, 2021 - annualreviews.org
Many essential biological processes are regulated through proximity, from membrane
receptor signaling to transcriptional activity. The ubiquitin-proteasome system controls …

[HTML][HTML] Recent advances in targeted protein degraders as potential therapeutic agents

N Yang, B Kong, Z Zhu, F Huang, L Zhang, T Lu… - Molecular …, 2024 - Springer
Targeted protein degradation (TPD) technology has gradually become widespread in the
past 20 years, which greatly boosts the development of disease treatment. Contrary to small …

[HTML][HTML] Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead

RP Nowak, L Ragosta, F Huerta, H Liu… - RSC Chemical …, 2023 - pubs.rsc.org
Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras
(PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described …

PROTACS: a technology with a gold rush-like atmosphere

YW Wang, L Lan, M Wang, JY Zhang, YH Gao… - European Journal of …, 2023 - Elsevier
Abnormally expressed or malfunctioning proteins may affect or even damage cells, leading
to the onset of diseases. Proteolysis targeting chimera (PROTAC) technology has been …

Assays and technologies for developing proteolysis targeting chimera degraders

X Liu, X Zhang, D Lv, Y Yuan, G Zheng… - Future Medicinal …, 2020 - Taylor & Francis
Targeted protein degradation by small-molecule degraders represents an emerging mode of
action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules …

Research progress of MEK1/2 inhibitors and degraders in the treatment of cancer

C Wang, H Wang, C Zheng, Z Liu, X Gao, F Xu… - European journal of …, 2021 - Elsevier
Mitogen-activated protein kinase kinases 1 and 2 (MEK1/2) are the crucial part of the RAS-
RAF-MEK-ERK pathway (or ERK pathway), which is involved in the regulation of various …

Hijacking methyl reader proteins for nuclear-specific protein degradation

DA Nalawansha, K Li, J Hines… - Journal of the American …, 2022 - ACS Publications
Targeted protein degradation (TPD) by PROTACs is a promising strategy to control disease-
causing protein levels within the cell. While TPD is emerging as an innovative drug …

Design and characterization of PROTAC degraders specific to protein N-terminal methyltransferase 1

Q Zhou, W Wu, K Jia, G Qi, XS Sun, P Li - European journal of medicinal …, 2022 - Elsevier
Protein N-terminal methylation catalyzed by N-terminal methyltransferase 1 (NTMT1) is an
emerging methylation present in eukaryotes, playing important regulatory roles in various …

Functionalized scout fragments for site-specific covalent ligand discovery and optimization

VM Crowley, M Thielert, BF Cravatt - ACS central science, 2021 - ACS Publications
Covalent ligands are a versatile class of chemical probes and drugs that can target
noncanonical sites on proteins and display differentiated pharmacodynamic properties …

Recent advances in induced proximity modalities

CSC Ng, SM Banik - Current Opinion in Chemical Biology, 2022 - Elsevier
Challenging disease targets necessitate new approaches for therapeutic intervention.
Rewiring protein-biomolecule interactions with proximity-inducing agents extends …