Novel approaches to targeted protein degradation technologies in drug discovery
Y Xue, AA Bolinger, J Zhou - Expert Opinion on Drug Discovery, 2023 - Taylor & Francis
Introduction Target protein degradation (TPD) provides a novel therapeutic modality, other
than inhibition, through the direct depletion of target proteins. Two primary human protein …
than inhibition, through the direct depletion of target proteins. Two primary human protein …
[HTML][HTML] Recent advances in covalent drug discovery
D Schaefer, X Cheng - Pharmaceuticals, 2023 - mdpi.com
In spite of the increasing number of biologics license applications, the development of
covalent inhibitors is still a growing field within drug discovery. The successful approval of …
covalent inhibitors is still a growing field within drug discovery. The successful approval of …
Chemical Specification of E3 Ubiquitin Ligase Engagement by Cysteine-Reactive Chemistry
Targeted protein degradation relies on small molecules that induce new protein–protein
interactions between targets and the cellular protein degradation machinery. Most of these …
interactions between targets and the cellular protein degradation machinery. Most of these …
Targeted Protein Degradation through Recruitment of the CUL4 Complex Adaptor Protein DDB1
M Meyers, S Cismoski, A Panidapu… - ACS Chemical …, 2024 - ACS Publications
Targeted protein degradation has arisen as a powerful therapeutic modality for eliminating
proteins. Thus far, most heterobifunctional proteolysis targeting chimeras (PROTACs) have …
proteins. Thus far, most heterobifunctional proteolysis targeting chimeras (PROTACs) have …
[HTML][HTML] Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders
Small molecules that induce protein-protein interactions to exert proximity-driven
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
Structural and functional annotation of solute carrier transporters: implication for drug discovery
V Dvorak, G Superti-Furga - Expert Opinion on Drug Discovery, 2023 - Taylor & Francis
ABSTRACT Introduction Solute carriers (SLCs) represent the largest group of membrane
transporters in the human genome. They play a central role in controlling the …
transporters in the human genome. They play a central role in controlling the …
The expanding repertoire of covalent warheads for drug discovery
The reactive functionalities of drugs that engage in covalent interactions with the
enzyme/receptor residue in either a reversible or an irreversible manner are …
enzyme/receptor residue in either a reversible or an irreversible manner are …
[HTML][HTML] Functionalizing tandem mass tags for streamlining click-based quantitative chemoproteomics
Mapping the ligandability or potential druggability of all proteins in the human proteome is a
central goal of mass spectrometry-based covalent chemoproteomics. Achieving this …
central goal of mass spectrometry-based covalent chemoproteomics. Achieving this …
[HTML][HTML] Tracking the mechanism of covalent molecular glue stabilization using native mass spectrometry
CJA Verhoef, DF Kay, L van Dijck, RG Doveston… - Chemical …, 2023 - pubs.rsc.org
Molecular glues are powerful tools for the control of protein–protein interactions. Yet, the
mechanisms underlying multi-component protein complex formation remain poorly …
mechanisms underlying multi-component protein complex formation remain poorly …
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 …