Chemistries of bifunctional PROTAC degraders
Abstract
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic strategy using small molecules to induce ubiquitin-dependent degradation of proteins.
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Although some have entered clinical trials with a primary focus on PROTAC, the diverse range of protein regulation methods has undoubtedly laid a robust foundation for developing drugs targeting previously undruggable proteins.
“Although some have entered clinical trials with a primary focus on PROTAC, the diverse range of protein regulation methods has undoubtedly laid a robust foundation for developing drugs targeting previously undruggable proteins.477–479”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [477]
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Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling
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The Role of New Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia
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Integrative Modeling of PROTAC-Mediated Ternary Complexes
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Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity
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Functional characterization of a PROTAC directed against BRAF mutant V600E
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Small-molecule PROTAC degraders of the Bromodomain and Extra Terminal (BET) proteins — A review
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Targeting EZH2 and PRC2 dependence as novel anticancer therapy
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A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL
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An overview of PROTACs: a promising drug discovery paradigm
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Characteristic roadmap of linker governs the rational design of PROTACs
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PROTAC-DB 3.0: an updated database of PROTACs with extended pharmacokinetic parameters
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Nano Proteolysis Targeting Chimeras (PROTACs) with Anti‐Hook Effect for Tumor Therapy
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Annual review of PROTAC degraders as anticancer agents in 2022
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Targeting the undruggables—the power of protein degraders
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Targeting Arginine Methyltransferase PRMT5 for Cancer Therapy: Updated Progress and Novel Strategies
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Stimuli‐Responsive PROTACs for Controlled Protein Degradation
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Current advances and development strategies of orally bioavailable PROTACs
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Targeted Protein Degradation Induced by HEMTACs Based on HSP90
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ClickRNA-PROTAC for Tumor-Selective Protein Degradation and Targeted Cancer Therapy
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Discovery of Novel PROTAC SIRT6 Degraders with Potent Efficacy against Hepatocellular Carcinoma
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Targeted protein degradation in cancers: Orthodox PROTACs and beyond
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Research in the Field of Drug Design and Development
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Discovery of a Drug-like, Natural Product-Inspired DCAF11 Ligand Chemotype
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Senolysis Enabled by Senescent Cell‐Sensitive Bioorthogonal Tetrazine Ligation
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Development of PROTACs using computational approaches
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Current advances of small molecule E3 ligands for proteolysis-targeting chimeras design
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PROTACs: Novel tools for improving immunotherapy in cancer
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In Vivo Self‐Assembly of PROTACs by Bioorthogonal Chemistry for Precision Cancer Therapy
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Linker-free PROTACs efficiently induce the degradation of oncoproteins
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Application of Novel Degraders Employing Autophagy for Expediting Medicinal Research
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Selective degradation of the p53‐R175H oncogenic hotspot mutant by an RNA aptamer‐based PROTAC
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Discovery of a Selective and Orally Bioavailable FGFR2 Degrader for Treating Gastric Cancer
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Ligation to Scavenging Strategy Enables On-Demand Termination of Targeted Protein Degradation
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Degraders in epigenetic therapy: PROTACs and beyond
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Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)
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Selective Elimination of Senescent Cancer Cells by Galacto-Modified PROTACs
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Decoy-PROTAC for specific degradation of “Undruggable” STAT3 transcription factor
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Recent advances in targeted protein degraders as potential therapeutic agents
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Targeting PRMT5 through PROTAC for the treatment of triple-negative breast cancer
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Deubiquitinase-Targeting Chimeras (DUBTACs) as a Potential Paradigm-Shifting Drug Discovery Approach
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An updated patent review of BRD4 degraders
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From PROTAC to TPD: Advances and Opportunities in Targeted Protein Degradation
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DDR1-targeted therapies: current limitations and future potential
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Self-citationRIPTACs: A groundbreaking approach to drug discovery
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Versatile Split-and-Mix Liposome PROTAC Platform for Efficient Degradation of Target Protein In Vivo
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PROTACs in the Management of Prostate Cancer
Poornachandra, Y., Babalghith, A. O., Andra, V. V., & Syed, R. (2023) · Molecules · doi:10.3390/molecules28093698 · Cited by 30 · see citing works
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Small-Molecule PROTACs for Cancer Immunotherapy
Liu, Z., Zhang, Y., Xiang, Y., & Kang, X. (2022) · Molecules · doi:10.3390/molecules27175439 · Cited by 29 · see citing works
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Small-molecule-based targeted therapy in liver cancer
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Discovery and Characterization of RP03707: A Highly Potent and Selective KRAS G12D PROTAC
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Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders
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Structure-Based Design of “Head-to-Tail” Macrocyclic PROTACs
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Advances in KEAP1-based PROTACs as emerging therapeutic modalities: Structural basis and progress
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Amphiphilic Affibody-PROTAC conjugate Self-Assembled nanoagents for targeted cancer therapy
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CRBN‐PROTACs in Cancer Therapy: From Mechanistic Insights to Clinical Applications
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Analyzing the Linker Structure of PROTACs throughout the Induction Process: Computational Insights
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Multi-Faceted Roles of DNAJB Protein in Cancer Metastasis and Clinical Implications
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Advances of bioorthogonal coupling reactions in drug development
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In silico modeling of targeted protein degradation
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Innovative, combinatorial and high-throughput approaches to degrader synthesis
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Advancing Design Strategy of PROTACs for Cancer Therapy
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Exploiting E3 ligases for lung cancer therapy: The promise of DCAF-PROTACs
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Facilitating the development of molecular glues: Opportunities from serendipity and rational design
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High‐Throughput Miniaturized Synthesis of PROTAC‐Like Molecules
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Senolytic Prodrugs: A Promising Approach to Enhancing Senescence‐Targeting Intervention
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Distal C(sp 3 )-H Amidation via Ind*Rh III Catalyzed Nitrene Transfer
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Application of PROTACs in target identification and validation
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Pt(IV)-PROTAC Complexes with Synergistic Antitumor Activity and Enhanced Membrane Permeability
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- Authors
- Cao, C., He, M., Wang, L., He, Y., & Rao, Y.
- Affiliations
- Ministry of Education (MOE) Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Tsinghua University, Beijing 100084, P. R. China
- Tsinghua University (CN)
- Corresponding author
- Rao, Yu
- Venue
- Chemical Society Reviews
- Publisher
- Royal Society of Chemistry (RSC)
- Published
- 2022
- Volume
- 51
- Issue
- 16
- Pages
- 7066-7114
- ISSN
- 0306-0012 (ISSN-L)
- 1460-4744
- OpenAlex
- W4289450662
- Cited by
- 313
- References
- 270
- Citations by year
- 2026: 67 · 2025: 89 · 2024: 96 · 2023: 52 · 2022: 9
- FWCI
- 6.42
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Chemical Society Reviews (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China (#81773567, #82125034)
- National Major Science and Technology Projects of China (#2020YFE0202200, #2021YFA1300200, #2021YFA1302100)
- National Key Research and Development Program of China (2021YFA1302100)
- Postdoctoral Research Foundation of China (#2021M691832, #2021M701953)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ubiquitin and proteasome pathways
- Keywords
- PROTACs, bifunctional degraders, ubiquitin-dependent protein degradation, PROTAC design, small-molecule degraders, protein degradation
- MeSH terms
- Ubiquitin-Protein Ligases, Proteolysis
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