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 …

[HTML][HTML] Modulating biomolecular condensates: a novel approach to drug discovery

DM Mitrea, M Mittasch, BF Gomes, IA Klein… - Nature Reviews Drug …, 2022 - nature.com
In the past decade, membraneless assemblies known as biomolecular condensates have
been reported to play key roles in many cellular functions by compartmentalizing specific …

[HTML][HTML] 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 …

Recent progress of supramolecular chemotherapy based on host–guest interactions

M Yan, S Wu, Y Wang, M Liang, M Wang… - Advanced …, 2024 - Wiley Online Library
Chemotherapy is widely recognized as an effective approach for treating cancer due to its
ability to eliminate cancer cells using chemotherapeutic drugs. However, traditional …

[HTML][HTML] Antibody targeting of E3 ubiquitin ligases for receptor degradation

H Marei, WTK Tsai, YS Kee, K Ruiz, J He, C Cox, T Sun… - Nature, 2022 - nature.com
Most current therapies that target plasma membrane receptors function by antagonizing
ligand binding or enzymatic activities. However, typical mammalian proteins comprise …

Target and tissue selectivity of PROTAC degraders

RG Guenette, SW Yang, J Min, B Pei… - Chemical Society …, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …

EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis

J Wang, X Yu, W Gong, X Liu, KS Park, A Ma… - Nature cell …, 2022 - nature.com
Canonically, EZH2 serves as the catalytic subunit of PRC2, which mediates H3K27me3
deposition and transcriptional repression. Here, we report that in acute leukaemias, EZH2 …

[HTML][HTML] 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 …

[HTML][HTML] Emerging degrader technologies engaging lysosomal pathways

Y Ding, D Xing, Y Fei, B Lu - Chemical Society Reviews, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) provides unprecedented opportunities for drug
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …