The Therapeutic Potential of PROTACs

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 March 2023) | Viewed by 4199

Special Issue Editor

State Key Laboratory of Biotherapy, Collaborative Innovation Center of Biotherapy and Cancer Center, Sichuan University, Chengdu 610041, China
Interests: proteolysis-targeting chimeras; antitumor small molecules; anti-HIV drugs

Special Issue Information

Dear Colleagues,

Proteolysis-targeting chimeras (PROTACs) is an emerging therapeutic modality with the potential to tackle disease-causing proteins that have historically been highly challenging to target with conventional small molecules. It has received extensive attention from both academia and industry, as it can potentially access previously inaccessible targets. Since the report of the concept of PROTACs using the ubiquitin–proteasome system to degrade target proteins, more and more PROTACs molecules targeting tumor-related proteins have been reported one after another, and many of these key molecules have also entered clinical trials. In the future, we also firmly believe that with the wider discovery of PROTACs target proteins and the expansion of the use of ubiquitin ligases, PROTACs will inevitably expand its model beyond oncology and bring disruptive change to drug discovery.

This Special Issue has the aim to summarize the state-of-the-art, and the latest findings published in the PROTACs field, as well as to elucidate future directions. Topics include: PROTAC technology, targeted protein degradation, degrader and drug development.

Dr. Rui Li
Guest Editor

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Keywords

  • PROTAC technology
  • inaccessible targets
  • targeted protein degradation
  • drug discovery

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Published Papers (1 paper)

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Review

25 pages, 7560 KiB  
Review
Protein-Targeted Degradation Agents Based on Natural Products
by Yan Li, Yi Jia, Xiaolin Wang, Hai Shang and Yu Tian
Pharmaceuticals 2023, 16(1), 46; https://doi.org/10.3390/ph16010046 - 28 Dec 2022
Cited by 8 | Viewed by 3783
Abstract
Natural products are an important source of drug lead compounds, and natural products with significant biological activity are constantly being discovered and used in clinical practice. At present, natural products play an important role in the targeted therapy of cancer, cardiovascular and cerebrovascular [...] Read more.
Natural products are an important source of drug lead compounds, and natural products with significant biological activity are constantly being discovered and used in clinical practice. At present, natural products play an important role in the targeted therapy of cancer, cardiovascular and cerebrovascular diseases, nervous system diseases, and autoimmune diseases. Meanwhile, in recent years, the rise of protein-targeted degradation technologies, such as proteolysis-targeting chimeras (PROTACs) and molecular glues, has provided a new solution for drug resistance caused by clinical molecular-targeting drugs. It is noteworthy that natural products and their derivatives, as important components of PROTACs and molecular glues, play an important role in the development of protein-targeting drugs. Hence, this review summarized the protein-targeted degradation agents based on natural products, such as PROTACs and molecular glues. More natural products with the potential to be used in the development of PROTACs and molecular glues as targeted protein degradation agents are still being investigated. Full article
(This article belongs to the Special Issue The Therapeutic Potential of PROTACs)
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