Innovative, combinatorial and high-throughput approaches to degrader synthesis
R Stevens, JDF Thompson, JCL Fournier… - Chemical Society …, 2024 - pubs.rsc.org
Targeted protein degraders such as PROTACs and molecular glues are a rapidly emerging
therapeutic modality within industry and academia. Degraders possess unique mechanisms …
therapeutic modality within industry and academia. Degraders possess unique mechanisms …
Discovery of Molecular Glue Degraders via Isogenic Morphological Profiling
A Ng, F Offensperger, JA Cisneros… - ACS Chemical …, 2023 - ACS Publications
Molecular glue degraders (MGDs) are small molecules that degrade proteins of interest via
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …
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 …
Offsetting Low-Affinity Carbohydrate Binding with Covalency to Engage Sugar-Specific Proteins for Tumor-Immune Proximity Induction
BPM Lake, AF Rullo - ACS Central Science, 2023 - ACS Publications
Carbohydrate-binding receptors are often used by the innate immune system to potentiate
inflammation, target endocytosis/destruction, and adaptive immunity (eg, CD206, DC-SIGN …
inflammation, target endocytosis/destruction, and adaptive immunity (eg, CD206, DC-SIGN …
[HTML][HTML] Expanding the horizons of targeted protein degradation: A non-small molecule perspective
X Huang, F Wu, J Ye, L Wang, X Wang, X Li… - … Pharmaceutica Sinica B, 2024 - Elsevier
Targeted protein degradation (TPD) represented by proteolysis targeting chimeras
(PROTACs) marks a significant stride in drug discovery. A plethora of innovative …
(PROTACs) marks a significant stride in drug discovery. A plethora of innovative …
A chemical magnet: Approaches to guide precise protein localization
Small molecules that chemically induce proximity between two proteins have been widely
used to precisely modulate protein levels, stability, and activity. Recently, several studies …
used to precisely modulate protein levels, stability, and activity. Recently, several studies …
Selection of DNA-encoded Chemical Libraries for Compounds that can Induce Protein Ubiquitination
C Huang, X Liu, X Wu, L Meng, X Lu, X Li - 2024 - chemrxiv.org
We report a selection method of DNA-encoded libraries (DELs) that can identify the
compounds able to induce ubiquitination of the protein of intertest (POI). Since the selection …
compounds able to induce ubiquitination of the protein of intertest (POI). Since the selection …
[PDF][PDF] Isogenic CPA: A morphological profiling approach for discovering molecular glues
RHA Ng - repositorium.meduniwien.ac.at
This inhibitor/activator-centric view of small molecule drugs has hindered the development
of drugs against over 70% of the human proteome. Many proteins in this 70% are well …
of drugs against over 70% of the human proteome. Many proteins in this 70% are well …