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 …

Molecular glues for targeted protein degradation: from serendipity to rational discovery

G Dong, Y Ding, S He, C Sheng - Journal of medicinal chemistry, 2021 - ACS Publications
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …

[PDF][PDF] 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 …

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 …

Bifunctional chemical probes inducing protein–protein interactions

C Maniaci, A Ciulli - Current Opinion in Chemical Biology, 2019 - Elsevier
Inducing biomolecular interactions with synthetic molecules to impact biological function is a
concept of enormous appeal. Recent years have seen a resurgence of interest in designing …

Ligandability of E3 ligases for targeted protein degradation applications

BP Belcher, CC Ward, DK Nomura - Biochemistry, 2021 - ACS Publications
Targeted protein degradation (TPD) using proteolysis targeting chimeras (PROTACs) and
molecular glue degraders has arisen as a powerful therapeutic modality for eliminating …

Targeted protein degradation: expanding the toolbox

M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …

[HTML][HTML] The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation

KM Riching, EA Caine, M Urh, DL Daniels - Chemical Society Reviews, 2022 - pubs.rsc.org
Targeted protein degradation has exploded over the past several years due to preclinical
and early clinical therapeutic success of numerous compounds, and the emergence of new …

[PDF][PDF] The role of reversible and irreversible covalent chemistry in targeted protein degradation

H Kiely-Collins, GE Winter, GJL Bernardes - Cell chemical biology, 2021 - cell.com
Proteolysis-targeting chimeras (PROTACs) that degrade disease-causing proteins by
hijacking the endogenous ubiquitin-proteasome system have emerged as an exciting and …