LYTACs: An Emerging Tool for the Degradation of Non‐Cytosolic Proteins

B Ramadas, P Kumar Pain, D Manna - ChemMedChem, 2021 - Wiley Online Library
In the last two decades, targeted protein degradation has rapidly gained popularity as a
technique to eliminate disease‐causing undruggable proteins. Over the years, many tools …

Roadmap for optimizing and broadening antibody-based PROTACs for degradation of cell surface proteins

JA Gramespacher, AD Cotton… - ACS Chemical …, 2022 - ACS Publications
Targeted protein degradation is a promising therapeutic strategy capable of overcoming the
limitations of traditional occupancy-based inhibitors. By ablating all of the associated …

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 …

[HTML][HTML] Targeted protein degradation: mechanisms, strategies and application

L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …

Targeted protein degradation: from mechanisms to clinic

JM Tsai, RP Nowak, BL Ebert, ES Fischer - Nature Reviews Molecular …, 2024 - nature.com
Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …

Redefining the Scope of Targeted Protein Degradation: Translational Opportunities in Hijacking the Autophagy–Lysosome Pathway

K Cassidy, H Zhao - Biochemistry, 2021 - ACS Publications
The advent of multi-specific targeted protein degradation (TPD) therapies has made it
possible to drug targets that have long been considered to be inaccessible. For this reason …

Targeting lysosomal degradation pathways: new strategies and techniques for drug discovery

J Pei, G Wang, L Feng, J Zhang, T Jiang… - Journal of Medicinal …, 2021 - ACS Publications
A series of tools for targeted protein degradation are inspiring scientists to develop new
drugs with advantages over traditional small-molecule drugs. Among these tools, proteolysis …

LYTACs that engage the asialoglycoprotein receptor for targeted protein degradation

G Ahn, SM Banik, CL Miller, NM Riley… - Nature chemical …, 2021 - nature.com
Selective protein degradation platforms have afforded new development opportunities for
therapeutics and tools for biological inquiry. The first lysosome-targeting chimeras (LYTACs) …

[HTML][HTML] Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs

SB Alabi, CM Crews - Journal of Biological Chemistry, 2021 - ASBMB
Of late, targeted protein degradation (TPD) has surfaced as a novel and innovative chemical
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …

Small-molecule degraders beyond PROTACs—challenges and opportunities

JM Kastl, G Davies, E Godsman… - … the Science of Drug …, 2021 - journals.sagepub.com
Targeted protein degradation (TPD) is a recent strategy, utilizing the cell's proteostasis
machinery to deplete specific proteins. This represents a paradigm shift in early drug …