Chasing molecular glue degraders: screening approaches
A Domostegui, L Nieto-Barrado… - Chemical Society …, 2022 - pubs.rsc.org
Protein–protein interactions (PPIs) govern all biological processes. Some small molecules
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
Induced protein degradation: an emerging drug discovery paradigm
Small-molecule drug discovery has traditionally focused on occupancy of a binding site that
directly affects protein function, and this approach typically precludes targeting proteins that …
directly affects protein function, and this approach typically precludes targeting proteins that …
Rational discovery of molecular glue degraders via scalable chemical profiling
C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka… - Nature chemical …, 2020 - nature.com
Targeted protein degradation is a new therapeutic modality based on drugs that destabilize
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders
Targeted protein degradation is a novel pharmacology established by drugs that recruit
target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target …
target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target …
[PDF][PDF] X-linked ubiquitin-specific peptidase 11 increases tauopathy vulnerability in women
Although women experience significantly higher tau burden and increased risk for
Alzheimer's disease (AD) than men, the underlying mechanism for this vulnerability has not …
Alzheimer's disease (AD) than men, the underlying mechanism for this vulnerability has not …
Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15
INTRODUCTION Indisulam is an aryl sulfonamide drug that inhibits the proliferation of
certain human cancer cell lines. Its mechanism of action and the mechanism underlying its …
certain human cancer cell lines. Its mechanism of action and the mechanism underlying its …
[PDF][PDF] Cancer mutations of the tumor suppressor SPOP disrupt the formation of active, phase-separated compartments
JJ Bouchard, JH Otero, DC Scott, E Szulc, EW Martin… - Molecular cell, 2018 - cell.com
Mutations in the tumor suppressor SPOP (speckle-type POZ protein) cause prostate, breast,
and other solid tumors. SPOP is a substrate adaptor of the cullin3-RING ubiquitin ligase and …
and other solid tumors. SPOP is a substrate adaptor of the cullin3-RING ubiquitin ligase and …
Structural insights into the catalysis and regulation of E3 ubiquitin ligases
L Buetow, DT Huang - Nature reviews Molecular cell biology, 2016 - nature.com
Covalent attachment (conjugation) of one or more ubiquitin molecules to protein substrates
governs numerous eukaryotic cellular processes, including apoptosis, cell division and …
governs numerous eukaryotic cellular processes, including apoptosis, cell division and …
Driving E3 ligase substrate specificity for targeted protein degradation: lessons from nature and the laboratory
AD Cowan, A Ciulli - Annual Review of Biochemistry, 2022 - annualreviews.org
Methods to direct the degradation of protein targets with proximity-inducing molecules that
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
Mechanisms of activation of the transcription factor Nrf2 by redox stressors, nutrient cues, and energy status and the pathways through which it attenuates …
LE Tebay, H Robertson, ST Durant, SR Vitale… - Free Radical Biology …, 2015 - Elsevier
Abstract Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) regulates the basal and stress-
inducible expression of a battery of genes encoding key components of the glutathione …
inducible expression of a battery of genes encoding key components of the glutathione …