PROTAC targeted protein degraders: the past is prologue
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 …
tackle disease-causing proteins that have historically been highly challenging to target with …
Targeted protein degradation: mechanisms, strategies and application
L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …
development and application of protein activity modulators, particularly inhibitors, has been …
H3K4me3 regulates RNA polymerase II promoter-proximal pause-release
Trimethylation of histone H3 lysine 4 (H3K4me3) is associated with transcriptional start sites
and has been proposed to regulate transcription initiation,. However, redundant functions of …
and has been proposed to regulate transcription initiation,. However, redundant functions of …
Exclusion of m6A from splice-site proximal regions by the exon junction complex dictates m6A topologies and mRNA stability
Summary N6-methyladenosine (m6A), a widespread destabilizing mark on mRNA, is non-
uniformly distributed across the transcriptome, yet the basis for its selective deposition is …
uniformly distributed across the transcriptome, yet the basis for its selective deposition is …
Cohesin and CTCF control the dynamics of chromosome folding
In mammals, interactions between sequences within topologically associating domains
enable control of gene expression across large genomic distances. Yet it is unknown how …
enable control of gene expression across large genomic distances. Yet it is unknown how …
RNA polymerase II dynamics shape enhancer–promoter interactions
How enhancers control target gene expression over long genomic distances remains an
important unsolved problem. Here we investigated enhancer–promoter communication by …
important unsolved problem. Here we investigated enhancer–promoter communication by …
Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021
Q Wu, W Qian, X Sun, S Jiang - Journal of hematology & oncology, 2022 - Springer
Abstract The United States Food and Drug Administration (US FDA) has always been a
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …
Advancing targeted protein degradation for cancer therapy
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 …
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 …
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
Proximity-based modalities for biology and medicine
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …