Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents

Proteolytic targeting chimaeras (PROTACs) have been developed as an effective technology for targeted protein degradation. PROTACs are heterobifunctional molecules that can trigger the polyubiquitination of proteins of interest (POIs) by recruiting the ubiquitin-proteasome system, thereby inhibiting...

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Main Authors: Chao Wang, Yujing Zhang, Lingyu Shi, Shanbo Yang, Jing Chang, Yingjie Zhong, Qian Li, Dongming Xing
Format: Article
Language:English
Published: Taylor & Francis Group 2022-12-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
Online Access:https://www.tandfonline.com/doi/10.1080/14756366.2022.2074414
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author Chao Wang
Yujing Zhang
Lingyu Shi
Shanbo Yang
Jing Chang
Yingjie Zhong
Qian Li
Dongming Xing
author_facet Chao Wang
Yujing Zhang
Lingyu Shi
Shanbo Yang
Jing Chang
Yingjie Zhong
Qian Li
Dongming Xing
author_sort Chao Wang
collection DOAJ
description Proteolytic targeting chimaeras (PROTACs) have been developed as an effective technology for targeted protein degradation. PROTACs are heterobifunctional molecules that can trigger the polyubiquitination of proteins of interest (POIs) by recruiting the ubiquitin-proteasome system, thereby inhibiting the intracellular level of POIs. To date, a variety of small-molecule PROTACs (CRBN, VHL, IAP, and MDM2-based PROTACs) have been developed. IAP-based PROTACs, also known as specific and nongenetic IAP-dependent protein erasers (SNIPERs), are used to degrade the target proteins closely related to diseases. Their structures consist of three parts, including target protein ligand, E3 ligase ligand, and the linker between them. So far, many SNIPERs have been extensively studied worldwide and have performed well in multiple diseases, especially cancer. In this review, we will present the most relevant advances in the field of SNIPERs and provide our perspective on the opportunities and challenges for SNIPERs to become therapeutic agents.
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spelling doaj.art-1bb81f185be94960847f7174c8cefb8e2022-12-22T00:34:27ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742022-12-013711437145310.1080/14756366.2022.2074414Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agentsChao Wang0Yujing Zhang1Lingyu Shi2Shanbo Yang3Jing Chang4Yingjie Zhong5Qian Li6Dongming Xing7The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaThe Affiliated Cardiovascular Hospital of Qingdao University, Qingdao University, Qingdao, ChinaThe Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaThe Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaThe Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaThe Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaThe Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaThe Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaProteolytic targeting chimaeras (PROTACs) have been developed as an effective technology for targeted protein degradation. PROTACs are heterobifunctional molecules that can trigger the polyubiquitination of proteins of interest (POIs) by recruiting the ubiquitin-proteasome system, thereby inhibiting the intracellular level of POIs. To date, a variety of small-molecule PROTACs (CRBN, VHL, IAP, and MDM2-based PROTACs) have been developed. IAP-based PROTACs, also known as specific and nongenetic IAP-dependent protein erasers (SNIPERs), are used to degrade the target proteins closely related to diseases. Their structures consist of three parts, including target protein ligand, E3 ligase ligand, and the linker between them. So far, many SNIPERs have been extensively studied worldwide and have performed well in multiple diseases, especially cancer. In this review, we will present the most relevant advances in the field of SNIPERs and provide our perspective on the opportunities and challenges for SNIPERs to become therapeutic agents.https://www.tandfonline.com/doi/10.1080/14756366.2022.2074414PROTACsIAPSNIPERsdegradationpromising treatment
spellingShingle Chao Wang
Yujing Zhang
Lingyu Shi
Shanbo Yang
Jing Chang
Yingjie Zhong
Qian Li
Dongming Xing
Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents
Journal of Enzyme Inhibition and Medicinal Chemistry
PROTACs
IAP
SNIPERs
degradation
promising treatment
title Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents
title_full Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents
title_fullStr Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents
title_full_unstemmed Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents
title_short Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents
title_sort recent advances in iap based protacs snipers as potential therapeutic agents
topic PROTACs
IAP
SNIPERs
degradation
promising treatment
url https://www.tandfonline.com/doi/10.1080/14756366.2022.2074414
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