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 …
Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15
The investigational drugs E7820, indisulam and tasisulam (aryl-sulfonamides) promote the
degradation of the splicing factor RBM39 in a proteasome-dependent mechanism. While the …
degradation of the splicing factor RBM39 in a proteasome-dependent mechanism. While the …
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 …
Novel mechanisms of molecular glue-induced protein degradation
S Alabi - Biochemistry, 2021 - ACS Publications
Molecular glues, as defined thus far in the targeted protein degradation (TPD) field, are
monovalent small molecules (< 500 Da) that reshape the surface of an E3 ligase receptor …
monovalent small molecules (< 500 Da) that reshape the surface of an E3 ligase receptor …
[HTML][HTML] Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders
Small molecules that induce protein-protein interactions to exert proximity-driven
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
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 …
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 …
Template-assisted covalent modification underlies activity of covalent molecular glues
Molecular glues are proximity-inducing small molecules that have emerged as an attractive
therapeutic approach. However, developing molecular glues remains challenging, requiring …
therapeutic approach. However, developing molecular glues remains challenging, requiring …
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 …
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 …