The emerging role of mass spectrometry-based proteomics in drug discovery
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 …
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 …
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
[HTML][HTML] Modulating biomolecular condensates: a novel approach to drug discovery
In the past decade, membraneless assemblies known as biomolecular condensates have
been reported to play key roles in many cellular functions by compartmentalizing specific …
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 …
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 …
ability to eliminate cancer cells using chemotherapeutic drugs. However, traditional …
[HTML][HTML] Antibody targeting of E3 ubiquitin ligases for receptor degradation
Most current therapies that target plasma membrane receptors function by antagonizing
ligand binding or enzymatic activities. However, typical mammalian proteins comprise …
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 …
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
Canonically, EZH2 serves as the catalytic subunit of PRC2, which mediates H3K27me3
deposition and transcriptional repression. Here, we report that in acute leukaemias, EZH2 …
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 …
putative protein targets. However, the antitumor performance of PROTACs is impaired by …
[HTML][HTML] Emerging degrader technologies engaging lysosomal pathways
Targeted protein degradation (TPD) provides unprecedented opportunities for drug
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …