Proximity-based modalities for biology and medicine
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
The rise of degrader drugs
The cancer genomics revolution has served up a plethora of promising and challenging
targets for the drug discovery community. The field of targeted protein degradation (TPD) …
targets for the drug discovery community. The field of targeted protein degradation (TPD) …
[HTML][HTML] Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …
structures or functions that are difficult to interfere with using conventional drug design …
Elucidating the cellular determinants of targeted membrane protein degradation by lysosome-targeting chimeras
Targeted protein degradation can provide advantages over inhibition approaches in the
development of therapeutic strategies. Lysosome-targeting chimeras (LYTACs) harness …
development of therapeutic strategies. Lysosome-targeting chimeras (LYTACs) harness …
[HTML][HTML] Expanding PROTACtable genome universe of E3 ligases
Proteolysis-targeting chimera (PROTAC) and other targeted protein degradation (TPD)
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …
Insulin-like Growth Factor 2 (IGF2)-Fused Lysosomal Targeting Chimeras for Degradation of Extracellular and Membrane Proteins
Targeted degradation of the cell-surface and extracellular proteins via the endogenous
lysosomal degradation pathways, such as lysosome-targeting chimeras (LYTACs), has …
lysosomal degradation pathways, such as lysosome-targeting chimeras (LYTACs), has …
Targeted degradation of extracellular secreted and membrane proteins
Targeted protein degradation (TPD) involving chimeric molecules has emerged as one of
the most promising therapeutic modalities in recent years. Among various reported TPD …
the most promising therapeutic modalities in recent years. Among various reported TPD …
Targeted protein degradation in drug development: Recent advances and future challenges
J Song, M Hu, J Zhou, S Xie, T Li, Y Li - European Journal of Medicinal …, 2023 - Elsevier
Targeted protein degradation (TPD) has emerged as a promising therapeutic approach with
potential advantages over traditional occupancy-based inhibitors in terms of dosing, side …
potential advantages over traditional occupancy-based inhibitors in terms of dosing, side …
The Dawn of a New Era: Targeting the “Undruggables” with Antibody-Based Therapeutics
The high selectivity and affinity of antibodies toward their antigens have made them a highly
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …
Opportunities and challenges of protein-based targeted protein degradation
L Dassama, F Shen - Chemical Science, 2023 - pubs.rsc.org
In the 20 years since the first report of a proteolysis targeting chimeric (PROTAC) molecule,
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …