DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic-and acquired-degrader resistance
M Schröder, M Renatus, X Liang, F Meili… - Nature …, 2024 - nature.com
Targeted protein degradation (TPD) mediates protein level through small molecule induced
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …
Emerging strategies for prospective discovery of molecular glue degraders
Molecular glue (MG) degraders are monovalent small molecule compounds that co-opt E3
ubiquitin ligases to target neo-substrates for proteasomal degradation. Here, we provide a …
ubiquitin ligases to target neo-substrates for proteasomal degradation. Here, we provide a …
Discovery of new binders for DCAF1, an emerging ligase target in the targeted protein degradation field
A Vulpetti, P Holzer, N Schmiedeberg… - ACS Medicinal …, 2023 - ACS Publications
In this study, we describe the rapid identification of potent binders for the WD40 repeat
domain (WDR) of DCAF1. This was achieved by two rounds of iterative focused screening of …
domain (WDR) of DCAF1. This was achieved by two rounds of iterative focused screening of …
Discovery of a novel DCAF1 ligand using a drug–target interaction prediction model: generalizing machine learning to new drug targets
SW Kimani, J Owen, SR Green, F Li, Y Li… - Journal of Chemical …, 2023 - ACS Publications
DCAF1 functions as a substrate recruitment subunit for the RING-type CRL4DCAF1 and the
HECT family EDVPDCAF1 E3 ubiquitin ligases. The WDR domain of DCAF1 serves as a …
HECT family EDVPDCAF1 E3 ubiquitin ligases. The WDR domain of DCAF1 serves as a …
Discovery of a First-in-Class Small-Molecule Ligand for WDR91 Using DNA-Encoded Chemical Library Selection Followed by Machine Learning
WD40 repeat-containing protein 91 (WDR91) regulates early-to-late endosome conversion
and plays vital roles in endosome fusion, recycling, and transport. WDR91 was recently …
and plays vital roles in endosome fusion, recycling, and transport. WDR91 was recently …
Construction of isocytosine scaffolds via DNA-Compatible biginelli-like reaction
Z Ding, Y Wu, L Liu, B Qi, Z Peng - Organic Letters, 2023 - ACS Publications
Herein we report a DNA-compatible Biginelli reaction to construct isocytosine scaffolds. This
reaction utilizes a one-pot reaction of DNA-conjugated guanidines with aldehydes and …
reaction utilizes a one-pot reaction of DNA-conjugated guanidines with aldehydes and …
[HTML][HTML] Expanding the ligand spaces for E3 ligases for the design of protein degraders
Targeted protein degradation (TPD) has recently emerged as an exciting new drug modality.
However, the strategy of developing small molecule-based protein degraders has evolved …
However, the strategy of developing small molecule-based protein degraders has evolved …
Development of Ligands and Degraders Targeting MAGE-A3
K Li, MW Krone, A Butrin, MJ Bond… - Journal of the …, 2024 - ACS Publications
Type I melanoma antigen (MAGE) family members are detected in numerous tumor types,
and expression is correlated with poor prognosis, high tumor grade, and increased …
and expression is correlated with poor prognosis, high tumor grade, and increased …
Bioisoteres for carboxylic acids: From ionized isosteres to novel unionized replacements
A Hall, M Chatzopoulou, J Frost - Bioorganic & Medicinal Chemistry, 2024 - Elsevier
Carboxylic acids are key pharmacophoric elements in many molecules. They can be seen
as a problem by some, due to perceived permeability challenges, potential for high plasma …
as a problem by some, due to perceived permeability challenges, potential for high plasma …