Emerging new concepts of degrader technologies

Y Ding, Y Fei, B Lu - Trends in Pharmacological Sciences, 2020 - cell.com
Traditional drug discovery focuses on identifying direct inhibitors of target proteins. This
typically relies on a measurable biochemical readout and accessible binding sites whose …

Targeted Protein Degradation: A Promising Option for Cancer Drug Developers: Instead of inhibiting disease-causing proteins, targeted protein degraders consign …

T Yesavage - Genetic Engineering & Biotechnology News, 2023 - liebertpub.com
Most targeted protein degraders make use of what is called the ubiquitinprotea-some
system, which can be thought of as the recycling system of the cell. However, as will be …

Advancing targeted protein degradation modalities

JC Madukwe - Trends in Pharmacological Sciences, 2023 - cell.com
Drug discovery efforts have traditionally focused on developing small molecules to directly
inhibit or modulate the enzymatic activity of disease-relevant proteins. However, the …

Targeted protein degradation: from chemical biology to drug discovery

PM Cromm, CM Crews - Cell chemical biology, 2017 - cell.com
Traditional pharmaceutical drug discovery is almost exclusively focused on directly
controlling protein activity to cure diseases. Modulators of protein activity, especially …

Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation

MJ Bond, CM Crews - RSC chemical biology, 2021 - pubs.rsc.org
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: Principles, Strategies, and Applications

T He, C Wen, G Yang, X Yang - Advanced Biology, 2023 - Wiley Online Library
Protein degradation is a general process to maintain cell homeostasis. The intracellular
protein quality control system mainly includes the ubiquitin‐proteasome system and the …

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: A promising approach for cancer treatment

MZI Khan, A Nazli, I Naz, D Khan, I Haq… - Journal of Pharmaceutical …, 2023 - Elsevier
Targeted protein degradation (TPD) is a promising approach that has the ability to address
disease-causing proteins. Compared to traditional inhibition, proteolysis targeting chimera …

Beyond canonical PROTAC: biological targeted protein degradation (bioTPD)

H Wang, R Zhou, F Xu, K Yang, L Zheng… - Biomaterials …, 2023 - spj.science.org
Targeted protein degradation (TPD) is an emerging therapeutic strategy with the potential to
modulate disease-associated proteins that have previously been considered undruggable …

[引用][C] Targeted protein degraders are redefining how small molecules look and act

LM Jarvis - Chem. Eng. News, 2018