Chemical specification of E3 ubiquitin ligase engagement by cysteine-reactive chemistry
Targeted protein degradation relies on small molecules that induce new protein–protein
interactions between targets and the cellular protein degradation machinery. Most of these …
interactions between targets and the cellular protein degradation machinery. Most of these …
Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16
X Zhang, VM Crowley, TG Wucherpfennig… - Nature chemical …, 2019 - nature.com
Ligand-dependent protein degradation has emerged as a compelling strategy to
pharmacologically control the protein content of cells. So far, however, only a limited number …
pharmacologically control the protein content of cells. So far, however, only a limited number …
Targeted protein degradation through E2 recruitment
N Forte, D Dovala, MJ Hesse, JM McKenna… - ACS chemical …, 2023 - ACS Publications
Targeted protein degradation (TPD) with proteolysis targeting chimeras (PROTACs),
heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of …
heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of …
DCAF11 supports targeted protein degradation by electrophilic proteolysis-targeting chimeras
X Zhang, LM Luukkonen, CL Eissler… - Journal of the …, 2021 - ACS Publications
Ligand-induced protein degradation has emerged as a compelling approach to promote the
targeted elimination of proteins from cells by directing these proteins to the ubiquitin …
targeted elimination of proteins from cells by directing these proteins to the ubiquitin …
Targeted protein degradation and the enzymology of degraders
SL Fisher, AJ Phillips - Current opinion in chemical biology, 2018 - Elsevier
Targeted protein degradation is an emerging strategy for drug discovery that employs small
molecules to catalyze the ubiquitination of target proteins, ultimately causing their …
molecules to catalyze the ubiquitination of target proteins, ultimately causing their …
[HTML][HTML] Targeted protein degradation via intramolecular bivalent glues
O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida… - Nature, 2024 - nature.com
Targeted protein degradation is a pharmacological modality that is based on the induced
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …
[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] Mechanistic studies of substrate-assisted inhibition of ubiquitin-activating enzyme by adenosine sulfamate analogues
JJ Chen, CA Tsu, JM Gavin, MA Milhollen… - Journal of Biological …, 2011 - ASBMB
Ubiquitin-activating enzyme (UAE or E1) activates ubiquitin via an adenylate intermediate
and catalyzes its transfer to a ubiquitin-conjugating enzyme (E2). MLN4924 is an adenosine …
and catalyzes its transfer to a ubiquitin-conjugating enzyme (E2). MLN4924 is an adenosine …
[HTML][HTML] Haven't got a glue: protein surface variation for the design of molecular glue degraders
Molecular glue degraders are small, drug-like compounds that induce interactions between
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …
Chemical approaches to targeted protein degradation through modulation of the ubiquitin–proteasome pathway
I Collins, H Wang, JJ Caldwell, R Chopra - Biochemical Journal, 2017 - portlandpress.com
Manipulation of the ubiquitin–proteasome system to achieve targeted degradation of
proteins within cells using chemical tools and drugs has the potential to transform …
proteins within cells using chemical tools and drugs has the potential to transform …