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 …

[HTML][HTML] 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 …

Molecular pathogenesis and systemic therapies for hepatocellular carcinoma

JM Llovet, R Pinyol, RK Kelley, A El-Khoueiry… - Nature cancer, 2022 - nature.com
Hepatocellular carcinoma (HCC) remains one of the most prevalent and deadliest cancers.
The poor outcome associated with HCC is dramatically changing due to the advent of …

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 …

The manipulation of apoptosis for cancer therapy using BH3-mimetic drugs

ST Diepstraten, MA Anderson, PE Czabotar… - Nature Reviews …, 2022 - nature.com
Apoptosis is a form of programmed cell death that is regulated by the balance between
prosurvival and proapoptotic BCL-2 protein family members. Evasion of apoptosis is a …

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 …

[HTML][HTML] 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 …

[HTML][HTML] The AUTOTAC chemical biology platform for targeted protein degradation via the autophagy-lysosome system

CH Ji, HY Kim, MJ Lee, AJ Heo, DY Park, S Lim… - Nature …, 2022 - nature.com
Targeted protein degradation allows targeting undruggable proteins for therapeutic
applications as well as eliminating proteins of interest for research purposes. While several …

Molecular glues for targeted protein degradation: from serendipity to rational discovery

G Dong, Y Ding, S He, C Sheng - Journal of medicinal chemistry, 2021 - ACS Publications
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …

[HTML][HTML] Roles of METTL3 in cancer: mechanisms and therapeutic targeting

C Zeng, W Huang, Y Li, H Weng - Journal of hematology & oncology, 2020 - Springer
Abstract N 6-methyladenosine (m 6 A) is the most abundant mRNA modification and is
catalyzed by the methyltransferase complex, in which methyltransferase-like 3 (METTL3) is …