Emerging strategies for prospective discovery of molecular glue degraders
Molecular glue (MG) degraders are monovalent small molecule compounds that co-opt E3
ubiquitin ligases to target neo-substrates for proteasomal degradation. Here, we provide a …
ubiquitin ligases to target neo-substrates for proteasomal degradation. Here, we provide a …
Molecular glues for targeted protein degradation: from serendipity to rational discovery
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
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 …
Molecular glue degraders: exciting opportunities for novel drug discovery
T Lemaitre, M Cornu, F Schwalen, M Since… - Expert Opinion on …, 2024 - Taylor & Francis
ABSTRACT Introduction Molecular Glue Degraders (MGDs) is a concept that refers to a
class of compounds that facilitate the interaction between two proteins or molecules within a …
class of compounds that facilitate the interaction between two proteins or molecules within a …
Molecular glue concept solidifies
K Baek, BA Schulman - Nature chemical biology, 2020 - nature.com
Molecular-glue-mediated proximity-induced degradation now allows unprecedented
therapeutic targeting of previously undruggable proteins. Structures showing how aryl …
therapeutic targeting of previously undruggable proteins. Structures showing how aryl …
Lessons from natural molecular glue degraders
S Cao - Biochemical Society Transactions, 2024 - portlandpress.com
Molecular glue (MG) degraders include plant hormones and therapeutic drugs and have
become a hot topic in drug discovery. Unlike bivalent proteolysis targeting chimeras …
become a hot topic in drug discovery. Unlike bivalent proteolysis targeting chimeras …
Molecular glues: the adhesive connecting targeted protein degradation to the clinic
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 …
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …
Discovery of molecular glue degraders via isogenic morphological profiling
A Ng, F Offensperger, JA Cisneros… - ACS Chemical …, 2023 - ACS Publications
Molecular glue degraders (MGDs) are small molecules that degrade proteins of interest via
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …
Oligomeric remodeling by molecular glues revealed using native mass spectrometry and mass photometry
Molecular glues stabilize interactions between E3 ligases and novel substrates to promote
substrate degradation, thereby facilitating the inhibition of traditionally “undruggable” protein …
substrate degradation, thereby facilitating the inhibition of traditionally “undruggable” protein …
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 …