PROTACs: past, present and future

K Li, CM Crews - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …

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 …

The MYC oncogene — the grand orchestrator of cancer growth and immune evasion

R Dhanasekaran, A Deutzmann… - Nature reviews Clinical …, 2022 - nature.com
The MYC proto-oncogenes encode a family of transcription factors that are among the most
commonly activated oncoproteins in human neoplasias. Indeed, MYC aberrations or …

The emerging role of mass spectrometry-based proteomics in drug discovery

F Meissner, J Geddes-McAlister, M Mann… - Nature Reviews Drug …, 2022 - nature.com
Proteins are the main targets of most drugs; however, system-wide methods to monitor
protein activity and function are still underused in drug discovery. Novel biochemical …

Chemistries of bifunctional PROTAC degraders

C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …

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 …

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …

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 …

Targeting STAT3 in cancer immunotherapy

S Zou, Q Tong, B Liu, W Huang, Y Tian, X Fu - Molecular cancer, 2020 - Springer
As a point of convergence for numerous oncogenic signaling pathways, signal transducer
and activator of transcription 3 (STAT3) is central in regulating the anti-tumor immune …

Lysosome-targeting chimaeras for degradation of extracellular proteins

SM Banik, K Pedram, S Wisnovsky, G Ahn, NM Riley… - Nature, 2020 - nature.com
The majority of therapies that target individual proteins rely on specific activity-modulating
interactions with the target protein—for example, enzyme inhibition or ligand blocking …