Development and therapeutic potential of GSPT1 molecular glue degraders: A medicinal chemistry perspective

X Chang, F Qu, C Li, J Zhang, Y Zhang… - Medicinal Research …, 2024 - Wiley Online Library
Unprecedented therapeutic targeting of previously undruggable proteins has now been
achieved by molecular‐glue‐mediated proximity‐induced degradation. As a small GTPase …

Potential of the nanoplatform and PROTAC interface to achieve targeted protein degradation through the Ubiquitin–Proteasome system

H Xie, C Zhang - European Journal of Medicinal Chemistry, 2024 - Elsevier
In eukaryotic cells, the ubiquitin–proteasome system (UPS) plays a crucial role in selectively
breaking down specific proteins. The ability of the UPS to target proteins effectively and …

Uncovering PROTAC Sensitivity and Efficacy by Multidimensional Proteome Profiling: A Case for STAT3

Y Suo, D Du, C Chen, H Zhu, X Wang… - Journal of Medicinal …, 2024 - ACS Publications
Proteolysis-targeting chimera (PROTAC) is a powerful technology that can effectively trigger
the degradation of target proteins. The intricate interplay among various factors leads to a …

[HTML][HTML] Screening for molecular glues–challenges and opportunities

GA Holdgate, C Bardelle, SK Berry, A Lanne… - SLAS Discovery, 2023 - Elsevier
Molecular glues are small molecules, typically smaller than PROTACs, and usually with
improved physicochemical properties that aim to stabilise the interaction between two …

[HTML][HTML] Blockade of the lncRNA-DOT1L-LAMP5 axis enhances autophagy and promotes degradation of MLL fusion proteins

TQ Chen, HJ Huang, SX Zhu, XT Chen, KJ Pu… - … Hematology & Oncology, 2024 - Springer
Background Mixed-lineage leukemia (MLL) fusion gene caused by chromosomal
rearrangement is a dominant oncogenic driver in leukemia. Due to having diverse MLL …

Targeted dephosphorylation of TFEB promotes its nuclear translocation.

JF Zhao, N Shpiro, G Sathe, A Brewer, TJ Macartney… - iScience, 2024 - cell.com
Reversible phosphorylation of the transcription factor EB (TFEB) coordinates cellular
responses to metabolic and other stresses. During nutrient replete and stressor-free …

Advancing targeted protein degradation modalities

JC Madukwe - Trends in Pharmacological Sciences, 2023 - cell.com
Drug discovery efforts have traditionally focused on developing small molecules to directly
inhibit or modulate the enzymatic activity of disease-relevant proteins. However, the …

[HTML][HTML] Characterisation of high throughput screening outputs for small molecule degrader discovery

LE Bell, C Bardelle, MJ Packer, J Kastl, GA Holdgate… - SLAS Discovery, 2024 - Elsevier
Targeted protein degradation is an important mechanism carried out by the cellular
machinery, one that is gaining momentum as an exploitable strategy for the development of …

Degradome analysis to identify direct protein substrates of small-molecule degraders

M Jochem, A Schrempf, LM Wagner, J Cisneros, A Ng… - bioRxiv, 2024 - biorxiv.org
Targeted protein degradation (TPD) has emerged as a powerful strategy to selectively
eliminate cellular proteins using small-molecule degraders, offering therapeutic promise for …

Bifunctional compound for targeted degradation of the immune checkpoint protein PD-L1

C Chen, H Shi, R Hao, L Fang, H Xu - Acta Chimica Sinica - sioc-journal.cn
Programmed death ligand 1 (PD-L1) is a protein overexpressed in numerous tumor cells as
an essential immune checkpoint that can facilitate immune escape of tumor cells through …