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 …

[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… - Signal transduction and …, 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 …

Progress and challenges in targeted protein degradation for neurodegenerative disease therapy

Y Fang, J Wang, M Zhao, Q Zheng, C Ren… - Journal of Medicinal …, 2022 - ACS Publications
Neurodegenerative diseases (NDs) are currently incurable diseases that cause progressive
degeneration of nerve cells. Many of the disease-causing proteins of NDs are “undruggable” …

PROTACs targeting MLKL protect cells from necroptosis

OH Rathje, L Perryman, RJ Payne… - Journal of Medicinal …, 2023 - ACS Publications
Mixed Lineage Kinase domain-Like pseudokinase (MLKL) is implicated in a broad range of
diseases due to its role as the ultimate effector of necroptosis and has therefore emerged as …

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 …

Engineered autonomous dynamic regulation of metabolic flux

M Ream, KLJ Prather - Nature Reviews Bioengineering, 2024 - nature.com
Metabolic engineering is a powerful tool to reprogramme cells to produce value-added
chemicals. Such engineering strategies require the fine-tuning of a cell's metabolism to …

Targeted Protein Degradation: Current and Emerging Approaches for E3 Ligase Deconvolution

Y Xiao, Y Yuan, Y Liu, Z Lin, G Zheng… - Journal of Medicinal …, 2024 - ACS Publications
Targeted protein degradation (TPD), including the use of proteolysis-targeting chimeras
(PROTACs) and molecular glue degraders (MGDs) to degrade proteins, is an emerging …

Destabilized reporters for background-subtracted, chemically-gated, and multiplexed deep-tissue imaging

J Yun, Y Huang, ADC Miller, BL Chang, L Baldini… - Chemical …, 2024 - pubs.rsc.org
Tracking gene expression in deep tissues requires genetic reporters that can be
unambiguously detected using tissue penetrant techniques. Magnetic resonance imaging …

[HTML][HTML] Targeted Protein Degradation Systems: Controlling Protein Stability Using E3 Ubiquitin Ligases in Eukaryotic Species

Y Ogawa, TP Ueda, K Obara, K Nishimura, T Kamura - Cells, 2024 - mdpi.com
This review explores various methods for modulating protein stability to achieve target
protein degradation, which is a crucial aspect in the study of biological processes and drug …

Synthesis and Evaluation of Cereblon‐Recruiting HaloPROTACs

BK Ody, J Zhang, SE Nelson, Y Xie, R Liu… - …, 2023 - Wiley Online Library
Target validation is key to the development of protein degrading molecules such as
proteolysis‐targeting chimeras (PROTACs) to identify cellular proteins amenable for induced …