Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …
proteasome system that recruits substrates such as the hypoxia inducible factor for …
[HTML][HTML] Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective
T Webb, C Craigon, A Ciulli - Bioorganic & Medicinal Chemistry Letters, 2022 - Elsevier
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 …
external stimuli and are prevalent in all higher-order organisms. The establishment of a link …
Discovery of a Potent Proteolysis Targeting Chimera Enables Targeting the Scaffolding Functions of FK506‐Binding Protein 51 (FKBP51)
TM Geiger, M Walz, C Meyners, A Kuehn… - Angewandte Chemie …, 2024 - Wiley Online Library
Abstract The FK506‐binding protein 51 (FKBP51) is a promising target in a variety of
disorders including depression, chronic pain, and obesity. Previous FKBP51‐targeting …
disorders including depression, chronic pain, and obesity. Previous FKBP51‐targeting …
Translational PK–PD for targeted protein degradation
DW Bartlett, AM Gilbert - Chemical Society Reviews, 2022 - pubs.rsc.org
Targeted protein degradation has emerged from the chemical biology toolbox as one of the
most exciting areas for novel therapeutic development across the pharmaceutical industry …
most exciting areas for novel therapeutic development across the pharmaceutical industry …
The 17th EFMC Short Course on Medicinal Chemistry on Small Molecule Protein Degraders
Abstract The 17th EFMC Short Course on Medicinal Chemistry took place April 23–26, 2023
in Oegstgeest, near Leiden in the Netherlands. It covered for the first time the exciting topic …
in Oegstgeest, near Leiden in the Netherlands. It covered for the first time the exciting topic …
Lysine deserts and cullin-RING ligase receptors: Navigating untrodden paths in proteostasis
The ubiquitin-proteasome system (UPS) governs the degradation of proteins by
ubiquitinating their lysine residues. Our study focuses on lysine deserts-regions in proteins …
ubiquitinating their lysine residues. Our study focuses on lysine deserts-regions in proteins …
Introducing structure-based three-dimensional pharmacophore models for accelerating the discovery of selective BRD9 binders
M Pierri, E Gazzillo, MG Chini, MG Ferraro… - Bioorganic …, 2022 - Elsevier
A well-structured in silico workflow is here reported for disclosing structure-based
pharmacophore models against bromodomain-containing protein 9 (BRD9), accelerating …
pharmacophore models against bromodomain-containing protein 9 (BRD9), accelerating …
Identification of 2, 4, 5-trisubstituted-2, 4-dihydro-3H-1, 2, 4-triazol-3-one-based small molecules as selective BRD9 binders
E Colarusso, S Ceccacci, MC Monti, E Gazzillo… - European Journal of …, 2023 - Elsevier
Targeting bromodomain-containing protein 9 (BRD9) represents a promising strategy for the
development of new agents endowed with anticancer properties. With this aim, a set of 2, 4 …
development of new agents endowed with anticancer properties. With this aim, a set of 2, 4 …
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 …
[HTML][HTML] Stereochemical inversion at a 1, 4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity
M Pierri, X Liu, A Kroupova, Z Rutter, AJ Hallatt… - Bioorganic & Medicinal …, 2024 - Elsevier
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small-molecule degraders
made of a linker connecting a target-binding moiety to a ubiquitin E3 ligase-binding moiety …
made of a linker connecting a target-binding moiety to a ubiquitin E3 ligase-binding moiety …