Targeted protein degradation tools: overview and future perspectives

Y Prozzillo, G Fattorini, MV Santopietro, L Suglia… - Biology, 2020 - mdpi.com
protein degradation systems. This review highlights the most recent advances in targeted
proteindegradation (TPD) are emerging strategies which aim to achieve loss of function and …

Glutathione‐Scavenging Nanoparticle‐Mediated PROTACs Delivery for Targeted Protein Degradation and Amplified Antitumor Effects

HJ Liu, W Chen, G Wu, J Zhou, C Liu, Z Tang… - Advanced …, 2023 - Wiley Online Library
targeted proteins is an emerging therapeutic strategy, noted for its high selectivity and efficiency
of protein degradation. [ 1, … the bioavailability of PROTACs for cancer treatment. [ 22-24 ] …

Targeted protein degradation: An important tool for drug discovery for “Undruggable” tumor transcription factors

M Dai, S Radhakrishnan, R Li, R Tan… - … & Treatment, 2022 - journals.sagepub.com
… in targeting TF proteins. For this reason, technologies that enable targeted protein degradation,
such as proteolysis-targeting … Currently, the main inhibition strategy for c-MYC focuses on …

Role of protein degradation systems in colorectal cancer

Z Cui, M Cong, S Yin, Y Li, Y Ye, X Liu, J Tang - Cell Death Discovery, 2024 - nature.com
… novel therapeutic strategies that simultaneously target both pathways, aiming to improve …
This makes the protein degradation pathway a potential target for treating cancer [4]. This …

Redefining the Scope of Targeted Protein Degradation: Translational Opportunities in Hijacking the Autophagy–Lysosome Pathway

K Cassidy, H Zhao - Biochemistry, 2021 - ACS Publications
… disease-relevant proteins via a therapeutic strategy termed targeted protein degradation (TPD). …
, a membrane-associated protein that plays a significant role in cancer cell proliferation. …

Targeted protein degradation induced by HEMTACs based on HSP90

Z Li, S Ma, L Zhang, S Zhang, Z Ma… - Journal of Medicinal …, 2022 - ACS Publications
Targeted protein degradation (TPD) strategies open up new … heat shock protein 90 (HSP90)–mediated
targeting chimeras … relationship between HSP90 and cancer, as described here, …

… Tumor Targeting and Penetration of Proteolysis-Targeting Chimeras through iRGD Peptide Conjugation: A Strategy for Precise Protein Degradation in Breast Cancer

S He, Y Fang, M Wu, P Zhang, F Gao… - Journal of Medicinal …, 2023 - ACS Publications
… Crucially, the iRGD modification strategy offers remarkable advantages in the … of targeted
protein degradation therapeutics. Our future endeavors will focus on exploring diverse targeting

[HTML][HTML] The rise and rise of protein degradation: opportunities and challenges ahead

SJ Hughes, A Testa, N Thompson, I Churcher - Drug Discovery Today, 2021 - Elsevier
… action underpinning targeted protein degradation strategies, including proteolysis-targeting
in tumors, a factor that severely limits the clinical utility of existing targeted cancer therapies. …

[PDF][PDF] The advantages of targeted protein degradation over inhibition: an RTK case study

GM Burslem, BE Smith, AC Lai, S Jaime-Figueroa… - Cell chemical …, 2018 - cell.com
… of the kinase activity, is a strategy with the potential to yield a … can be accomplished using
Proteolysis targeting chimeras (… Given their well-defined role in human cancers and the broad …

The emerging role of targeted protein degradation to treat and study cancer

MH Brodermann, EK Henderson, RS Sellar - The Journal of Pathology - Wiley Online Library
… The evolution of cancer treatment has provided increasingly targeted strategies both in the
upfront and relapsed disease settings. Small-molecule inhibitors and immunotherapy have …