Enriching proteolysis targeting chimeras with a second modality: When two are better than one
A Salerno, F Seghetti, J Caciolla, E Uliassi… - Journal of Medicinal …, 2022 - ACS Publications
Proteolysis targeting chimera (PROTAC)-mediated protein degradation has prompted a
radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness …
radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness …
Strategies for the discovery of oral PROTAC degraders aimed at cancer therapy
In the past two decades, we have witnessed the discovery and development of many potent
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
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: 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 …
PROTACs: emerging targeted protein degradation approaches for advanced druggable strategies
NI Sincere, K Anand, S Ashique, J Yang, C You - Molecules, 2023 - mdpi.com
A potential therapeutic strategy to treat conditions brought on by the aberrant production of a
disease-causing protein is emerging for targeted protein breakdown using the PROTACs …
disease-causing protein is emerging for targeted protein breakdown using the PROTACs …
Aptamer‐protac conjugates (apcs) for tumor‐specific targeting in breast cancer
S He, F Gao, J Ma, H Ma, G Dong… - Angewandte …, 2021 - Wiley Online Library
Abstract Development of proteolysis targeting chimeras (PROTACs) is emerging as a
promising strategy for targeted protein degradation. However, the drug development using …
promising strategy for targeted protein degradation. However, the drug development using …
[HTML][HTML] Monitoring and deciphering protein degradation pathways inside cells
A new series of therapeutic modalities resulting in degradation of target proteins, termed
proteolysis targeting chimeras (PROTACs), hold significant therapeutic potential with …
proteolysis targeting chimeras (PROTACs), hold significant therapeutic potential with …
PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
The state of the art of PROTAC technologies for drug discovery
C Wang, C Zheng, H Wang, L Zhang, Z Liu… - European Journal of …, 2022 - Elsevier
Protein degradation technology has progressed dramatically since 2001 when proteolysis
targeting chimera (PROTAC) was first reported. Various of distinctive degradation …
targeting chimera (PROTAC) was first reported. Various of distinctive degradation …
Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy
J Gao, B Hou, Q Zhu, L Yang, X Jiang, Z Zou… - Nature …, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) has been exploited to degrade
putative protein targets. However, the antitumor performance of PROTACs is impaired by …
putative protein targets. However, the antitumor performance of PROTACs is impaired by …