Construction of an IMiD-based azide library as a kit for PROTAC research

Liu, Haixia; Sun, Renhong; Ren, Chaowei; Qiu, Xing; Yang, Xiaobao; Jiang, Biao

doi:10.1039/d0ob02120b

Cited by 23 publications

(22 citation statements)

References 49 publications

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“…The triazole motif is often used to assemble PROTACs due to its ease of rapid and efficient construction by click chemistry. [116][117][118][119][120] The triazole motif can increase the solubility and metabolic stability of PROTACs.…”

Section: Assembly Of Protacsmentioning

confidence: 99%

Chemistries of bifunctional PROTAC degraders

et al. 2022

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Section: Assembly Of Protacsmentioning

confidence: 99%

Chemistries of bifunctional PROTAC degraders

et al. 2022

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“…30 ) were obtained. 152 These two degraders showed strong BET protein-degradation activity when the concentration was 50 nM. At the same, it could show strong anti-proliferation inhibitory activity on MV4-11 cells.…”

Section: Protacs Targeting Cancer-related Targetsmentioning

confidence: 83%

“…Subsequently, Jiang group synthesized a series of CRBN-based degraders by conjugating Dasatinib to pomalidomide or lenalidomide. 152 As an important example, a pomalidomide-based degrader 89 ( SIAIS056 , Fig. 21 ), possessing sulfur-substituted carbon chain linker, exhibited the potent degradation of wild-type and clinically relevant resistance-conferring mutations of BCR-ABL.…”

Section: Protacs Targeting Cancer-related Targetsmentioning

confidence: 99%

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

Cao

et al. 2022

Sig Transduct Target Ther

135

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PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-degradation strategy that has emerged in recent years. It uses bifunctional small molecules to induce the ubiquitination and degradation of target proteins through the ubiquitin–proteasome system. PROTACs can not only be used as potential clinical treatments for diseases such as cancer, immune disorders, viral infections, and neurodegenerative diseases, but also provide unique chemical knockdown tools for biological research in a catalytic, reversible, and rapid manner. In 2019, our group published a review article “PROTACs: great opportunities for academia and industry” in the journal, summarizing the representative compounds of PROTACs reported before the end of 2019. In the past 2 years, the entire field of protein degradation has experienced rapid development, including not only a large increase in the number of research papers on protein-degradation technology but also a rapid increase in the number of small-molecule degraders that have entered the clinical and will enter the clinical stage. In addition to PROTAC and molecular glue technology, other new degradation technologies are also developing rapidly. In this article, we mainly summarize and review the representative PROTACs of related targets published in 2020–2021 to present to researchers the exciting developments in the field of protein degradation. The problems that need to be solved in this field will also be briefly introduced.

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“…Two groups have developed click chemistry‐based platforms for the rapid and efficient assembly of PROTACs containing triazole linkers (Figure 5C). 35,80 Namely, Rao's group designed PROTACs with triazole‐containing linkers that target focal adhesion kinase (FAK) 81,82 . At concentrations ranging from 10 to 40 nM, an initially developed FAK‐targeting PROTAC degraded only one‐half of the FAK proteins to which it was exposed 83 .…”

Section: General Strategies For the Design And Optimization Of Protacsmentioning

confidence: 99%

Strategies for designing proteolysis targeting chimaeras (PROTACs)

Dong

Cheng

et al. 2022

Medicinal Research Reviews

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Proteolysis targeting chimaeras (PROTACs) is a cutting edge and rapidly growing technique for new drug discovery and development. Currently, the largest challenge in the molecular design and drug development of PROTACs is efficient identification of potent and drug-like degraders. This review aims to comprehensively summarize and analyse state-ofthe-art methods and strategies in the design of PROTACs.We provide a detailed illustration of the general principles and tactics for designing potent PROTACs, highlight representative case studies, and discuss the advantages and limitations of these strategies. Particularly, structure-based rational PROTAC design and emerging new types of PROTACs (e.g., homo-PROTACs, multitargeting PROTACs, photo-control PROTACs and PROTAC-based conjugates) will be focused on.

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Construction of an IMiD-based azide library as a kit for PROTAC research

Abstract: As a promising protein degradation strategy, PROTAC technology is increasingly becoming a new star in cancer treatment.

Cited by 23 publications

References 49 publications

Chemistries of bifunctional PROTAC degraders

Chemistries of bifunctional PROTAC degraders

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

Strategies for designing proteolysis targeting chimaeras (PROTACs)

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