[HTML][HTML] Screening for molecular glues–challenges and opportunities

GA Holdgate, C Bardelle, SK Berry, A Lanne… - SLAS Discovery, 2023 - Elsevier
Molecular glues are small molecules, typically smaller than PROTACs, and usually with
improved physicochemical properties that aim to stabilise the interaction between two …

[HTML][HTML] Clues to molecular glues

TM Geiger, SC Schäfer, JK Dreizler, M Walz… - Current Research in …, 2022 - Elsevier
Molecular Glues, here defined as small molecules that interact with two protein surfaces to
induce or enhance affinity of these two proteins to each other, have received substantial …

Molecular glues and induced proximity: An evolution of tools and discovery

SA Robinson, SM Banik - Cell Chemical Biology, 2024 - cell.com
Small molecule molecular glues can nucleate protein complexes and rewire interactomes.
Molecular glues are widely used as probes for understanding functional proximity at a …

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 …

Molecular glue discovery: current and future approaches

JA Dewey, C Delalande, SA Azizi, V Lu… - Journal of medicinal …, 2023 - ACS Publications
The intracellular interactions of biomolecules can be maneuvered to redirect signaling,
reprogram the cell cycle, or decrease infectivity using only a few dozen atoms. Such …

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 …

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 for protein-protein interactions: Progressing toward a new dream

M Konstantinidou, MR Arkin - Cell Chemical Biology, 2024 - cell.com
The modulation of protein-protein interactions with small molecules is one of the most
rapidly developing areas in drug discovery. In this review, we discuss advances over the …

E3 ligase ligands for PROTACs: how they were found and how to discover new ones

T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …

A platform for the rapid synthesis of molecular glues (Rapid-Glue) under miniaturized conditions for direct biological screening

J Li, C Li, Z Zhang, Z Zhang, Z Wu, J Liao… - European Journal of …, 2023 - Elsevier
Molecular glues, functioning via inducing degradation of the target protein while having
similar molecular weight as traditional small molecule drugs, are emerging as a promising …