Themed collection Molecular Glues

6 items
Open Access Review Article

Bringing enzymes to the proximity party

Targeted enzymes can drive cell type-selective reactions that are not yet possible with other therapeutic approaches.

Graphical abstract: Bringing enzymes to the proximity party
From the themed collection: Molecular Glues
Open Access Review Article

Protein–protein interfaces in molecular glue-induced ternary complexes: classification, characterization, and prediction

This review surveys molecular glue-induced ternary complexes in the PDB and provides an overview of computational methods that can be utilized to predict them.

Graphical abstract: Protein–protein interfaces in molecular glue-induced ternary complexes: classification, characterization, and prediction
From the themed collection: Molecular Glues
Open Access Paper

Bind&Bite: covalently stabilized heterodimeric coiled-coil peptides for the site-selective, cysteine-free chemical modification of proteins

A pair of heterodimeric coiled-coil peptides was modified to enable covalent stabilization of the dimer without using enzymes or cysteine. Fusion of the peptides to a protein and a chemical moiety, respectively, facilitates site-selective protein modification.

Graphical abstract: Bind&Bite: covalently stabilized heterodimeric coiled-coil peptides for the site-selective, cysteine-free chemical modification of proteins
From the themed collection: Molecular Glues
Open Access Paper

A model-informed method to retrieve intrinsic from apparent cooperativity and project cellular target occupancy for ternary complex-forming compounds

Estimating intrinsic from apparent cooperativities to calculate concentrations of ternary complexes in biochemical and cellular assays.

Graphical abstract: A model-informed method to retrieve intrinsic from apparent cooperativity and project cellular target occupancy for ternary complex-forming compounds
From the themed collection: Molecular Glues
Open Access Paper

Straightforward model construction and analysis of multicomponent biomolecular systems in equilibrium

A framework for equilibrium models, such as molecular glues and other contemporary biomolecular multicomponent systems, is presented that automatically generates custom mass-balance models based on the reversible reactions of each system.

Graphical abstract: Straightforward model construction and analysis of multicomponent biomolecular systems in equilibrium
From the themed collection: Molecular Glues
Open Access Paper

Accessing three-branched high-affinity cereblon ligands for molecular glue and protein degrader design

The Petasis borono-Mannich reaction was employed for an entry towards three-branched cereblon ligands. The high-affinity ligands were used to assemble molecular glues and proteolysis targeting chimeras (PROTACs) targeting BRD4 for degradation.

Graphical abstract: Accessing three-branched high-affinity cereblon ligands for molecular glue and protein degrader design
From the themed collection: Molecular Glues
6 items

About this collection

This themed collection, guest edited by Michelle Arkin (University of California San Francisco, USA), Luc Brunsveld (TU Eindhoven, Netherlands), and Eric Fischer (Dana-Farber Cancer Institute and Harvard Medical School, USA), encompasses the wide scope of molecular glues. Topics include protein degradation glues, protein binders and stabilizers, bi-functional molecules for protein degradation and beyond with a particular interest on molecular recognition.


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