[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 …
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 …
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 …
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
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 …
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 …
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 …
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
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 …
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 …
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 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
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 …
similar molecular weight as traditional small molecule drugs, are emerging as a promising …