[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 …
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 …
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), 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 …
to the onset of diseases. Proteolysis targeting chimera (PROTAC) technology has been …
Assays and technologies for developing proteolysis targeting chimera degraders
Targeted protein degradation by small-molecule degraders represents an emerging mode of
action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules …
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 …
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 …
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
Protein N-terminal methylation catalyzed by N-terminal methyltransferase 1 (NTMT1) is an
emerging methylation present in eukaryotes, playing important regulatory roles in various …
emerging methylation present in eukaryotes, playing important regulatory roles in various …
Functionalized scout fragments for site-specific covalent ligand discovery and optimization
Covalent ligands are a versatile class of chemical probes and drugs that can target
noncanonical sites on proteins and display differentiated pharmacodynamic properties …
noncanonical sites on proteins and display differentiated pharmacodynamic properties …
Recent advances in induced proximity modalities
Challenging disease targets necessitate new approaches for therapeutic intervention.
Rewiring protein-biomolecule interactions with proximity-inducing agents extends …
Rewiring protein-biomolecule interactions with proximity-inducing agents extends …