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View article: BromoCatch: a self-labelling tag platform for protein analysis and live cell imaging
BromoCatch: a self-labelling tag platform for protein analysis and live cell imaging Open
Visualizing and manipulating proteins in live cells is crucial for studying complex biological processes. Self-labelling protein (SLP) tags such as HaloTag and SNAP-tag can be fused to genes of interest to allow protein labelling in cells.…
View article: Use of Aldehyde–Alkyne–Amine Couplings to Generate Medicinal Chemistry-Relevant Linkers
Use of Aldehyde–Alkyne–Amine Couplings to Generate Medicinal Chemistry-Relevant Linkers Open
Copper catalyzed aldehyde-alkyne-amine (A3) couplings lead to multifunctional, racemic, propargylic amines, many on a multigram scale. As part of an industrial collaboration, a selection of linkers was purified by chiral HPLC to afford sin…
View article: Leveraging Dual-Ligase Recruitment to Enhance Protein Degradation via a Heterotrivalent Proteolysis Targeting Chimera
Leveraging Dual-Ligase Recruitment to Enhance Protein Degradation via a Heterotrivalent Proteolysis Targeting Chimera Open
Proteolysis targeting chimera (PROTAC) degraders are typically bifunctional with one E3 ligase ligand connected to one target protein ligand via a linker. While augmented valency has been shown with trivalent PROTACs targeting two binding …
View article: Mechanism of degrader-targeted protein ubiquitinability
Mechanism of degrader-targeted protein ubiquitinability Open
Small-molecule degraders of disease-driving proteins offer a clinically proven modality with enhanced therapeutic efficacy and potential to tackle previously undrugged targets. Stable and long-lived degrader-mediated ternary complexes driv…
View article: Leveraging dual-ligase recruitment to enhance degradation via a heterotrivalent PROTAC
Leveraging dual-ligase recruitment to enhance degradation via a heterotrivalent PROTAC Open
Proteolysis targeting chimera (PROTAC) degraders are typically bifunctional with one moiety of an E3 ligase ligand connected to one target protein ligand via a linker. While augmented valency has been shown with trivalent PROTACs targeting…
View article: Targeted protein degradation via intramolecular bivalent glues
Targeted protein degradation via intramolecular bivalent glues Open
Targeted protein degradation is a pharmacological modality based on the induced proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and proteasomal degradation. This has been achieved either via bifunc…
View article: Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective
Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective Open
Epigenetic modulators perform critical functions in gene expression for rapid adaption to external stimuli and are prevalent in all higher-order organisms. The establishment of a link between dysregulation of epigenetic processes and disea…
View article: Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity
Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity Open
Criteria for predicting the druglike properties of "beyond Rule of 5" Proteolysis Targeting Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often combined via amide couplings due to their reliability. Amides, however,…
View article: Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity Open
Bivalent PROTACs work drive protein degradation by simultaneously binding a target protein and an E3 ligase and forming a productive ternary complex. We hypothesized that increasing binding valency within a PROTAC could enhanced degradatio…
View article: Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity Open
Bivalent PROTACs work drive protein degradation by simultaneously binding a target protein and an E3 ligase and forming a productive ternary complex. We hypothesized that increasing binding valency within a PROTAC could enhanced degradatio…
View article: Development of BromoTag: A “Bump-and-Hole”–PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins
Development of BromoTag: A “Bump-and-Hole”–PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins Open
Small-molecule-induced protein depletion technologies, also called inducible degrons, allow degradation of genetically engineered target proteins within cells and animals. Here, we design and develop the BromoTag, a new inducible degron sy…
View article: Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity
Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity Open
Bifunctional PROTAC degraders belong to "beyond Rule of 5" chemical space, and criteria for predicting their drug-like properties are underdeveloped. PROTAC components are often combined via late-stage amide couplings, due to the reliabili…
View article: Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity
Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity Open
Bifunctional PROTAC degraders belong to "beyond Rule of 5" chemical space, and criteria for predicting their drug-like properties are underdeveloped. PROTAC components are often combined via late-stage amide couplings, due to the reliabili…