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protein-degradation's Introduction

Year Month First author Title / Link Journal Computational?
2021 11 Lv Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity Nature Communications X
2021 10 Wang UbiBrowser 2.0: a comprehensive resource for proteome-wide known and predicted ubiquitin ligase/deubiquitinase–substrate interactions in eukaryotic species Nucleic Acids Research
2021 10 Imaide Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity Nature Chemical Biology
2021 10 Zhang Covalently Engineered Nanobody Chimeras for Targeted Membrane Protein Degradation JACS *
2021 09 Zhang Machine learning modeling of protein-intrinsic features predicts tractability of targeted protein degradation bioRxiv *
2021 09 Belcher Ligandability of E3 Ligases for Targeted Protein Degradation Applications Biochemistry
2021 08 Hughes The rise and rise of protein degradation: Opportunities and challenges ahead Drug Discovery Today
2021 08 Shao Destruction of DNA-Binding Proteins by Programmable Oligonucleotide PROTAC (O'PROTAC): Effective Targeting of LEF1 and ERG Advanced Science
2021 07 Schneider The PROTACtable genome Nature Reviews Drug Discovery *
2021 07 Rodriguez-Rivera Unifying Catalysis Framework to Dissect Proteasomal Degradation Paradigms ACS Central Science
2021 07 Douglas Ternary Kinetic Models for Rational Design of Molecular Glues chemRxiv *
2021 06 Reynders Optical control of targeted protein degradation Cell Chemical Biology
2021 06 Dale Advancing targeted protein degradation for cancer therapy Nature Reviews Cancer
2021 06 Liu TF-PROTACs Enable Targeted Degradation of Transcription Factors Journal of the American Chemical Society
2021 05 Kannt Expanding the arsenal of E3 ubiquitin ligases for proximity-induced protein degradation Cell Chemical Biology
2021 05 Nishiguchi Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators Journal of Medicinal Chemistry
2021 05 Cecchini From Conception to Development: Investigating PROTACs Features for Improved Cell Permeability and Successful Protein Degradation Frontiers in Chemistry
2021 04 Jetvic An E3 ligase guide to the galaxy of small-molecule-induced protein degradation Cell Chemical Biology
2021 04 Henning Discovery of a Covalent FEM1B Recruiter for Targeted Protein Degradation Applications bioRxiv
2021 04 Henneberg Decoding the messaging of the ubiquitin system using chemical and protein probes Cell Chemical Biology
2021 04 Scholes Identification and selectivity profiling of small-molecule degraders via multi-omics approaches Cell Chemical Biology
2021 04 Farnaby Transforming targeted cancer therapy with PROTACs: A forward-looking perspective Current Opinion in Pharmacology
2021 03 Kiely-Collins The role of reversible and irreversible covalent chemistry in targeted protein degradation Cell Chemical Biology
2021 03 Zhang DCAF11 Supports Targeted Protein Degradation by Electrophilic Proteolysis-Targeting Chimeras JACS
2021 03 Castaldi Advances in Protein Degradation SLAS Discovery
2021 03 Ahn Degradation from the outside in: targeting extracellular and membrane proteins for degradation through the endolysosomal pathway Cell Chemical Biology
2021 03 Ege Phenotypic screening with target identification and validation in the discovery and development of E3 ligase modulators Cell Chemical Biology
2021 03 Bond Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation RSC Chemical Biology
2021 03 Ahn LYTACs that engage the asialoglycoprotein receptor for targeted protein degradation Nature Chemical Biology
2021 03 Pei Targeting Lysosomal Degradation Pathways: New Strategies and Techniques for Drug Discovery Journal of Medicinal Chemistry
2021 03 Jiang Discovery and resistance mechanism of a selective CDK12 degrader Nature Chemical Biology
2021 03 Hundley A comprehensive phenotypic CRISPR-Cas9 screen of the ubiquitin pathway uncovers roles of ubiquitin ligases in mitosis Molecular Cell
2021 03 Mullard Targeted protein degraders crowd into the clinic Nature Reviews Drug Discovery
2021 03 Spradlin Reimagining Druggability Using Chemoproteomic Platforms Accounts of Chemical Research
2021 03 Shao Destruction of DNA-binding proteins by programmable O’PROTAC: Oligonucleotide-based PROTAC bioRxiv
2021 03 Zheng Novel PROTACs for degradation of SHP2 protein Bioorganic Chemistry
2021 03 Jaeger Fast-acting chemical tools to delineate causality in transcriptional control Molecular Cell
2021 03 Mohler An Overview of Next-Generation Androgen Receptor-Targeted Therapeutics in Development for the Treatment of Prostate Cancer International Journal of Molecular Sciences
2021 03 Wang Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy Nature Chemical Biology
2021 03 Kim Avoid the trap: targeting PARP1 beyond human malignancy Cell Chemical Biology
2021 03 Jan Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide Nature Reviews Clinical Oncology
2021 03 Zhang Ubiquitination of Nonhistone Proteins in Cancer Development and Treatment Frontiers in Oncology
2021 03 Kastl Small-Molecule Degraders beyond PROTACs—Challenges and Opportunities SLAS Discovery
2021 02 Peter A novel, universally active C-terminal protein degradation signal generated by alternative splicing Journal of Molecular Biology
2021 02 Schreiber The Rise of Molecular Glues Cell
2021 02 Zhang SPIN4 Is a Principal Endogenous Substrate of the E3 Ubiquitin Ligase DCAF16 Biochemistry
2021 02 Kolb Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells Nature Communications
2021 02 Bai Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta Journal of Chemical Information and Modeling X
2021 02 Liu Design and Synthesis of EZH2-Based PROTACs to Degrade the Complex for Targeting the Noncatalytic Activity of EZH2 Journal of Medicinal Chemistry
2021 02 Dragovich Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties Journal of Medicinal Chemistry
2021 02 Dragovich Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy Journal of Medicinal Chemistry
2021 02 Tokheim Systematic characterization of mutations altering protein degradation in human cancers Molecular Cell X
2021 02 Alabi Mutant-selective degradation by BRAF-targeting PROTACs Nature Communications
2021 02 Kaiho-Soma TRIP12 promotes small-molecule-induced degradation through K29/K48-branched ubiquitin chains Molecular Cell
2021 02 Powell Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library ACS Chemical Biology
2021 02 Cao Recent insight into the role of RING-finger E3 ligases in glioma Biochemical Society Transactions
2021 02 Horn-Ghetko Ubiquitin ligation to F-box protein targets by SCF–RBR E3–E3 super-assembly Nature
2021 02 Koduri Targeting oncoproteins with a positive selection assay for protein degraders Science Advances
2021 02 Gabizon The rise of covalent proteolysis targeting chimeras Current Opinion in Chemical Biology
2021 01 Ermondi PROTACs and Building Blocks: The 2D Chemical Space in Very Early Drug Discovery Molecules X
2021 01 Maiwald Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay ACS Medicinal Chemistry Letters
2021 01 Kessler DUB esterase activity further decodes ubiquitin’s enigma PNAS
2021 01 De Cesare Deubiquitinating enzyme amino acid profiling reveals a class of ubiquitin esterases PNAS
2021 01 Yeh The C‐degron pathway eliminates mislocalized proteins and products of deubiquitinating enzymes EMBO Journal
2021 01 Serapian Exploiting the folding and degradation machineries to target undruggable proteins: What can the computational approach tell us? ChemMedChem X
2021 01 Luo Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function Cell Chemical Biology
2021 01 Jan Reversible ON- and OFF-switch chimeric antigen receptors controlled by lenalidomide Science Translational Medicine
2021 01 Shirasaki Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins Cell Reports
2021 01 Benowitz The therapeutic potential of PROTACs Expert Opinion on Therapeutic Patents
2021 01 Yan Discovery of a PROTAC targeting ALK with in vivo activity European Journal of Medicinal Chemistry
2021 01 Cotton Development of Antibody-Based PROTACs for the Degradation of the Cell-Surface Immune Checkpoint Protein PD-L1 Journal of the American Chemical Society
2021 01 Banchenko Structural insights into Cullin4-RING ubiquitin ligase remodelling by Vpr from simian immunodeficiency viruses bioRxiv
2021 01 Zeng Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges European Journal of Medicinal Chemistry
2021 01 Martín-Acosta PROTACs to address the challenges facing small molecule inhibitors European Journal of Medicinal Chemistry
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2020 12 Atilaw Solution Conformations Shed Light on PROTAC Cell Permeability ACS Medicinal Chemistry Letters
2020 12 Caine Targeted Protein Degradation Phenotypic Studies Using HaloTag CRISPR/Cas9 Endogenous Tagging Coupled with HaloPROTAC3 Current Protocols in Pharmacology
2020 12 Leissing Structure driven compound optimization in targeted protein degradation Drug Discovery Today
2020 12 Tong Bardoxolone conjugation enables targeted protein degradation of BRD4 Scientific Reports
2020 12 Liu A Proteomic Platform to Identify Off-Target Proteins Associated with Therapeutic Modalities that Induce Protein Degradation or Gene Silencing bioRxiv
2020 12 Donovan Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development Cell
2020 11 Chatterjee Targeted intracellular degradation of SARS-CoV-2 via computationally optimized peptide fusions Communications Biology
2020 11 Matyskiela Cereblon Modulators Target ZBTB16 and Its Oncogenic Fusion Partners for Degradation via Distinct Structural Degrons ACS Chemical Biology
2020 11 Schiemer Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes Nature Chemical Biology
2020 11 Adhikari PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase Nature Chemical Biology
2020 10 Nabet Charting a New Path Towards Degrading Every Protein ChemBioChem
2020 10 Jiang PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases European Journal of Medicinal Chemistry
2020 10 Ghidini RNA‐PROTACs – degraders of RNA‐binding proteins Angewandte Chemie International Edition
2020 10 Bartlett A kinetic proofreading model for bispecific protein degraders Journal of Pharmacokinetics and Pharmacodynamics X
2020 10 Samarasinghe Targeted Degradation of Transcription Factors by TRAFTACs: Transcription Factor Targeting Chimeras bioRxiv
2020 10 Weinmann and Crews Protein Degradation with New Chemical Modalities: Successful Strategies in Drug Discovery and Chemical Biology Ebook: Royal Society of Chemistry X (some)
2020 10 Lee Targeted Degradation of Transcription Coactivator SRC‐1 through the N‐Degron Pathway Angewandte Chemie International Edition
2020 10 Goracci Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications Journal of Medicinal Chemistry
2020 10 Miyamae A Method for Conditional Regulation of Protein Stability in Native or Near-Native Form Cell Chemical Biology
2020 10 Weng PROTAC-DB: an online database of PROTACs Nucleic Acids Research X
2020 10 Yang Structural basis for substrate recognition and chemical inhibition of oncogenic MAGE ubiquitin ligases Nature Communications
2020 10 Bushman Proteomics-Based Identification of DUB Substrates Using Selective Inhibitors Cell Chemical Biology
2020 09 Furihata Structural bases of IMiD selectivity that emerges by 5-hydroxythalidomide Nature Communications
2020 09 Qin The therapeutic effect of the BRD4-degrading PROTAC A1874 in human colon cancer cells Cell Death and Disease
2020 09 Zaidman PRosettaC: Rosetta based modeling of PROTAC mediated ternary complexes Journal of Chemical Information and Modeling X
2020 09 Drummond Improved Accuracy for Modeling PROTAC-Mediated Ternary Complex Formation and Targeted Protein Degradation via New In Silico Methodologies Journal of Chemical Information and Modeling X
2020 09 Cao Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC) European Journal of Medicinal Chemistry
2020 09 Simpson Inducible Degradation of Target Proteins through a Tractable Affinity-Directed Protein Missile System Cell Chemical Biology
2020 08 Nalawansha PROTACs: An Emerging Therapeutic Modality in Precision Medicine Cell Chemical Biology
2020 08 Liang Design and pharmaceutical applications of proteolysis-targeting chimeric molecules Biochemical Pharmacology
2020 08 Cipriano Targeting epigenetic reader domains by chemical biology Current Opinion in Chemical Biology
2020 08 Mayor-Ruiz Rational discovery of molecular glue degraders via scalable chemical profiling Nature Chemical Biology
2020 08 Han A suite of mathematical solutions to describe ternary complex formation and their application to targeted protein degradation by heterobifunctional ligands Journal of Biological Chemistry X
2020 08 Mabbitt Structural basis for RING-Cys-Relay E3 ligase activity and its role in axon integrity Nature Chemical Biology
2020 07 Timms Tying up loose ends: the N-degron and C-degron pathways of protein degradation Biochemical Society Transactions
2020 07 Beveridge Native Mass Spectrometry Can Effectively Predict PROTAC Efficacy ACS Central Science
2020 07 Chung Structural Insights into PROTAC-Mediated Degradation of Bcl-xL ACS Chemical Biology
2020 07 Ruprecht A mass spectrometry-based proteome map of drug action in lung cancer cell lines Nature Chemical Biology
2020 06 Hanzl Targeted protein degradation: current and future challenges Current Opinion in Chemical Biology
2020 05 Luh Prey for the Proteasome: Targeted Protein Degradation – A Medicinal Chemist´s Perspective Angewandte Chemie International Edition
2020 03 Imrie Deep Generative Models for 3D Linker Design Journal of Chemical Information and Modeling X
2020 03 Wu Small molecules that target the ubiquitin system Biochemical Society Transactions
2020 02 Deshaies Multispecific drugs herald a new era of biopharmaceutical innovation Nature
2020 02 Wang Degradation of proteins by PROTACs and other strategies Acta Pharmaceutica Sinica B
2020 01 Moreau Proteolysis‐targeting chimeras in drug development: A safety perspective British Journal of Pharmacology
2020 01 Gong Targeting Cullin-RING Ubiquitin Ligases and the Applications in PROTACs Advances in Experimental Medicine and Biology
2020 01 Yang The Evolving Druggability and Developability Space: Chemically Modified New Modalities and Emerging Small Molecules The AAPS Journal
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2019 12 Sun Protacs: Great opportunities for academia and industry Signal Transduction and Targeted Therapy
2019 10 Schapira Targeted protein degradation: expanding the toolbox Current Opinion in Chemical Biology
2019 10 Maple Developing degraders: principles and perspectives on design and chemical space MedChemComm
2019 09 Chamberlain Development of targeted protein degradation therapeutics Nature Chemical Biology
2019 08 Maniaci Bifunctional chemical probes inducing protein–protein interactions Current Opinion in Chemical Biology
2019 07 Spradlin Harnessing the anti-cancer natural product nimbolide for targeted protein degradation Nature Chemical Biology
2019 06 Ella The Hunt for Degrons of the 26S Proteasome Biomolecules
2019 04 Paiva Targeted protein degradation: elements of PROTAC design Current Opinion in Chemical Biology
2019 04 Roth Advances in targeted degradation of endogenous proteins Cellular and Molecular Life Sciences
2019 03 Simonetta Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction Nature Communications X
2019 02 Drummond In Silico Modeling of PROTAC-Mediated Ternary Complexes: Validation and Application Journal of Chemical Information and Modeling X
2019 01 Buhimschi Evolving Rules for Protein Degradation? Insights from the Zinc Finger Degrome Biochemistry
2019 01 Liu UbiHub: a data hub for the explorers of ubiquitination pathways Bioinformatics X
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2018 09 Clift Acute and rapid degradation of endogenous proteins by Trim-Away Nature Protocols X
2018 08 Lucas Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase Journal of Medicinal Chemistry X
2018 06 Fisher Targeted protein degradation and the enzymology of degraders Current Opinion in Chemical Biology
2018 03 Ge Integrated Genomic Analysis of the Ubiquitin Pathway across Cancer Types Cell Reports X
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2017 05 Gadd Structural basis of PROTAC cooperative recognition for selective protein degradation Nature Chemical Biology
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2016 07 Medvar Comprehensive database of human E3 ubiquitin ligases: application to aquaporin-2 regulation Physiological genomics

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