Proximity-based modalities for biology and medicine

X Liu, A Ciulli - ACS Central Science, 2023 - ACS Publications
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …

The rise of degrader drugs

M Teng, NS Gray - Cell Chemical Biology, 2023 - cell.com
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) …

[HTML][HTML] Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - … and Targeted Therapy, 2023 - nature.com
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 …

Elucidating the cellular determinants of targeted membrane protein degradation by lysosome-targeting chimeras

G Ahn, NM Riley, RA Kamber, S Wisnovsky… - Science, 2023 - science.org
Targeted protein degradation can provide advantages over inhibition approaches in the
development of therapeutic strategies. Lysosome-targeting chimeras (LYTACs) harness …

[HTML][HTML] Expanding PROTACtable genome universe of E3 ligases

Y Liu, J Yang, T Wang, M Luo, Y Chen, C Chen… - Nature …, 2023 - nature.com
Proteolysis-targeting chimera (PROTAC) and other targeted protein degradation (TPD)
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

B Zhang, RK Brahma, L Zhu, J Feng, S Hu… - Journal of the …, 2023 - ACS Publications
Targeted degradation of the cell-surface and extracellular proteins via the endogenous
lysosomal degradation pathways, such as lysosome-targeting chimeras (LYTACs), has …

Targeted degradation of extracellular secreted and membrane proteins

X Chen, Y Zhou, Y Zhao, W Tang - Trends in Pharmacological Sciences, 2023 - cell.com
Targeted protein degradation (TPD) involving chimeric molecules has emerged as one of
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 …

The Dawn of a New Era: Targeting the “Undruggables” with Antibody-Based Therapeutics

L Qian, X Lin, X Gao, RU Khan, JY Liao, S Du… - Chemical …, 2023 - ACS Publications
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 …

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 …