PROTAC technology: From drug development to probe technology for target deconvolution

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 276, С. 116725 - 116725

Опубликована: Июль 30, 2024

Язык: Английский

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Nano-PROTACs: state of the art and perspectives

Nanoscale, Год журнала: 2024, Номер 16(9), С. 4378 - 4391

Опубликована: Янв. 1, 2024

Schematic illustration of the combinational strategy nanotechnology and PROTACs (Nano-PROTACs): typical shortcomings traditional nanotechnology-based strategies for PROTAC drugs optimization.

Язык: Английский

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PROTACs: Current and Future Potential as a Precision Medicine Strategy to Combat Cancer

Molecular Cancer Therapeutics, Год журнала: 2024, Номер 23(4), С. 454 - 463

Опубликована: Янв. 10, 2024

Abstract Proteolysis targeting chimeras (PROTAC) are an emerging precision medicine strategy, which targets key proteins for proteolytic degradation to ultimately induce cancer cell killing. These hetero-bifunctional molecules hijack the ubiquitin proteasome system selectively add polyubiquitin chains onto a specific protein target degradation. Importantly, PROTACs have capacity virtually any intracellular and transmembrane degradation, including oncoproteins previously considered undruggable, strategically positions at crossroads of multiple research areas. In this review, we present normal functions regulation describe application improve efficacy current broad-spectrum therapeutics. We subsequently potential exploit vulnerabilities through synthetic genetic approaches, may expedite development, translation, utility novel therapies in cancer. Finally, challenges associated with ongoing efforts overcome these issues streamline clinical translation. Ultimately, lead their routine use, is expected revolutionize treatment strategies, delay familial onset, lives outcomes those living

Язык: Английский

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Applications of protein ubiquitylation and deubiquitylation in drug discovery

Journal of Biological Chemistry, Год журнала: 2024, Номер 300(5), С. 107264 - 107264

Опубликована: Апрель 5, 2024

The ubiquitin-proteasome system (UPS) is the major machinery mediating specific protein turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and driving their degradation, UPS involved many important cellular processes. Several new UPS-based technologies, including molecular glue degraders PROTACs (Proteolysis-targeting chimeras) to promote DUBTACs (deubiquitinase-targeting increase stability, have been developed. specifically inducing interactions between different ubiquitin ligases targeted that are not otherwise related, degrade via system; contrast, by proximity of deubiquitinases, created clear degradable polyubiquitin chains stabilize proteins. In this review, we summarize recent research progress degraders, PROTACs, applications. We discuss immunomodulatory drugs (IMiDs), sulfonamides, CDK-targeting development PROTACs. also introduce principle DUBTAC its Finally, propose a few future directions these three technologies related homeostasis.

Язык: Английский

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Advances in the therapeutic delivery and applications of functionalized Pluronics: A critical review

Advances in Colloid and Interface Science, Год журнала: 2021, Номер 299, С. 102563 - 102563

Опубликована: Ноя. 18, 2021

Язык: Английский

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