[HTML][HTML] Haven't got a glue: protein surface variation for the design of molecular glue degraders

Z Kozicka, NH Thomä - Cell Chemical Biology, 2021 - cell.com
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 …

Molecular glues: the adhesive connecting targeted protein degradation to the clinic

JM Sasso, R Tenchov, DS Wang, LS Johnson… - Biochemistry, 2022 - ACS Publications
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …

Chemical specification of E3 ubiquitin ligase engagement by cysteine-reactive chemistry

RC Sarott, I You, YD Li, ST Toenjes… - Journal of the …, 2023 - ACS Publications
Targeted protein degradation relies on small molecules that induce new protein–protein
interactions between targets and the cellular protein degradation machinery. Most of these …

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 …

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 …

[HTML][HTML] An E3 ligase guide to the galaxy of small-molecule-induced protein degradation

P Jevtić, DL Haakonsen, M Rapé - Cell chemical biology, 2021 - cell.com
Induced protein degradation accomplishes elimination, rather than inhibition, of pathological
proteins. Key to the success of this novel therapeutic modality is the modification of proteins …

[HTML][HTML] 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 …

Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders

A Hanzl, R Casement, H Imrichova, SJ Hughes… - Nature chemical …, 2023 - nature.com
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 …

[HTML][HTML] Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction

KR Simonetta, J Taygerly, K Boyle, SE Basham… - Nature …, 2019 - nature.com
Protein–protein interactions (PPIs) governing the recognition of substrates by E3 ubiquitin
ligases are critical to cellular function. There is significant therapeutic potential in the …

[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 …