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 …
Small‐molecule PROTACS: new approaches to protein degradation
M Toure, CM Crews - Angewandte Chemie International …, 2016 - Wiley Online Library
The current inhibitor‐based approach to therapeutics has inherent limitations owing to its
occupancy‐based model: 1) there is a need to maintain high systemic exposure to ensure …
occupancy‐based model: 1) there is a need to maintain high systemic exposure to ensure …
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 …
development and application of protein activity modulators, particularly inhibitors, has been …
Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …
targeted protein degradation (TPD) has changed the landscape of drug development …
[HTML][HTML] The rise and rise of protein degradation: opportunities and challenges ahead
SJ Hughes, A Testa, N Thompson, I Churcher - Drug Discovery Today, 2021 - Elsevier
The transformational mechanism of action underpinning targeted protein degradation
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …
Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond
Y Zhong, F Chi, H Wu, Y Liu, Z Xie, W Huang… - European journal of …, 2022 - Elsevier
Targeted protein degradation technology has evolved a brand-new therapeutic modality
from an innovative drug discovery perspective. Though the classical PROTACs has …
from an innovative drug discovery perspective. Though the classical PROTACs has …
Targeted protein degradation directly engaging lysosomes or proteasomes
J Kim, I Byun, H Joh, HJ Kim, MJ Lee - Chemical Society Reviews, 2024 - pubs.rsc.org
Targeted protein degradation (TPD) has been established as a viable alternative to
attenuate the function of a specific protein of interest in both biological and clinical contexts …
attenuate the function of a specific protein of interest in both biological and clinical contexts …
Targeted protein degradation: A promise for undruggable proteins
KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …
environment within the cell. However, when natural proteostasis mechanisms are …
Targeted protein degradation: from mechanisms to clinic
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 …
degradation of proteins. In its most common form, this degradation is achieved through …
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 …
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …