Targeted protein degradation: expanding the toolbox
M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
Proteolysis-targeting chimeras (PROTACs) in cancer therapy
X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
PROTACs: great opportunities for academia and industry
X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …
Targeted protein degradation: elements of PROTAC design
SL Paiva, CM Crews - Current opinion in chemical biology, 2019 - Elsevier
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
Revisiting the grammar of Tau aggregation and pathology formation: how new insights from brain pathology are sha** how we study and target Tauopathies
Converging evidence continues to point towards Tau aggregation and pathology formation
as central events in the pathogenesis of Alzheimer's disease and other Tauopathies …
as central events in the pathogenesis of Alzheimer's disease and other Tauopathies …
[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review
RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …
Small-molecule-induced polymerization triggers degradation of BCL6
Effective and sustained inhibition of non-enzymatic oncogenic driver proteins is a major
pharmacological challenge. The clinical success of thalidomide analogues demonstrates …
pharmacological challenge. The clinical success of thalidomide analogues demonstrates …
Targeted protein degradation: A promise for undruggable proteins
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 …
PROTAC technology: opportunities and challenges
H Gao, X Sun, Y Rao - ACS medicinal chemistry letters, 2020 - ACS Publications
PROTACs-induced targeted protein degradation has emerged as a novel therapeutic
strategy in drug development and attracted the favor of academic institutions, large …
strategy in drug development and attracted the favor of academic institutions, large …
E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
protein degradation, have proven their great therapeutic potential and usefulness as …