[HTML][HTML] PROTAC targeted protein degraders: the past is prologue
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …
tackle disease-causing proteins that have historically been highly challenging to target with …
E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
protein degradation, have proven their great therapeutic potential and usefulness as …
Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders
Targeted protein degradation is a novel pharmacology established by drugs that recruit
target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target …
target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target …
Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity
VG Klein, AG Bond, C Craigon… - Journal of medicinal …, 2021 - ACS Publications
Criteria for predicting the druglike properties of “beyond Rule of 5” Proteolysis Targeting
Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often …
Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often …
Bifunctional compounds as molecular degraders for integrin-facilitated targeted protein degradation
J Zheng, W He, J Li, X Feng, Y Li, B Cheng… - Journal of the …, 2022 - ACS Publications
As effective ways to regulate protein levels, targeted protein degradation technologies have
attracted great attention in recent years. Here, we established a novel integrin-facilitated …
attracted great attention in recent years. Here, we established a novel integrin-facilitated …
Aptamer-based targeted protein degradation
The selective removal of misfolded, aggregated, or aberrantly overexpressed protein plays
an essential role in maintaining protein-dominated biological processes. In parallel, the …
an essential role in maintaining protein-dominated biological processes. In parallel, the …
Formation of C(sp2)–C(sp3) Bonds Instead of Amide C–N Bonds from Carboxylic Acid and Amine Substrate Pools by Decarbonylative Cross-Electrophile Coupling
J Wang, LE Ehehalt, Z Huang, OM Beleh… - Journal of the …, 2023 - ACS Publications
Carbon–heteroatom bonds, most often amide and ester bonds, are the standard method to
link together two complex fragments because carboxylic acids, amines, and alcohols are …
link together two complex fragments because carboxylic acids, amines, and alcohols are …
[HTML][HTML] BacPROTACs mediate targeted protein degradation in bacteria
FE Morreale, S Kleine, J Leodolter, S Junker, DM Hoi… - Cell, 2022 - cell.com
Hijacking the cellular protein degradation system offers unique opportunities for drug
discovery, as exemplified by proteolysis-targeting chimeras. Despite their great promise for …
discovery, as exemplified by proteolysis-targeting chimeras. Despite their great promise for …
Prey for the proteasome: targeted protein degradation—a medicinal chemist's perspective
LM Luh, U Scheib, K Juenemann… - Angewandte Chemie …, 2020 - Wiley Online Library
Targeted protein degradation (TPD), the ability to control a proteins fate by triggering its
degradation in a highly selective and effective manner, has created tremendous excitement …
degradation in a highly selective and effective manner, has created tremendous excitement …
Identification of potent, selective, and orally bioavailable small-molecule GSPT1/2 degraders from a focused library of cereblon modulators
G Nishiguchi, F Keramatnia, J Min… - Journal of medicinal …, 2021 - ACS Publications
Whereas the PROTAC approach to target protein degradation greatly benefits from rational
design, the discovery of small-molecule degraders relies mostly on phenotypic screening …
design, the discovery of small-molecule degraders relies mostly on phenotypic screening …