Targeted protein degradation in cancers: Orthodox PROTACs and beyond

J Li, X Chen, A Lu, C Liang - The Innovation, 2023 - cell.com
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …

PROTAC targeted protein degraders: the past is prologue

M Békés, DR Langley, CM Crews - Nature Reviews Drug Discovery, 2022 - nature.com
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …

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 …

Advancement of targeted protein degradation strategies as therapeutics for undruggable disease targets

MP Kannan, S Sreeraman, CS Somala… - Future Medicinal …, 2023 - Taylor & Francis
Targeted protein degradation (TPD) aids in developing novel bifunctional small-molecule
degraders and eliminates proteins of interest. The TPD approach shows promising results in …

[HTML][HTML] Targeted protein degrader development for cancer: advances, challenges, and opportunities

Y Fang, S Wang, S Han, Y Zhao, C Yu, H Liu… - Trends in pharmacological …, 2023 - cell.com
Anticancer-targeted therapies inhibit various kinases implicated in cancer and have been
used in clinical settings for decades. However, many cancer-related targets are proteins …

Proteolysis-targeting chimeras (PROTACs) in cancer therapy: present and future

R Li, M Liu, Z Yang, J Li, Y Gao, R Tan - Molecules, 2022 - mdpi.com
The PROteolysis TArgeting Chimeras (PROTACs) is an innovative technique for the
selective degradation of target proteins via the ubiquitin–proteasome system. Compared …

Protein degraders enter the clinic—a new approach to cancer therapy

D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …

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 …

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 …

PROTACs: current trends in protein degradation by proteolysis-targeting chimeras

J Madan, VK Ahuja, K Dua, S Samajdar… - BioDrugs, 2022 - Springer
In the recent past, proteolysis-targeting chimera (PROTAC) technology has received
enormous attention for its ability to overcome the limitations of protein inhibitors and its …