Emerging strategies for prospective discovery of molecular glue degraders

B Wang, S Cao, N Zheng - Current Opinion in Structural Biology, 2024 - Elsevier
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 …

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 …

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 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 …

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 …

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 …

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 …

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 …

Oligomeric remodeling by molecular glues revealed using native mass spectrometry and mass photometry

X Huang, H Kamadurai, P Siuti, E Ahmed… - Journal of the …, 2023 - ACS Publications
Molecular glues stabilize interactions between E3 ligases and novel substrates to promote
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

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 …