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 |
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2021 |
10 |
Imaide |
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity |
Nature Chemical Biology |
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2021 |
10 |
Zhang |
Covalently Engineered Nanobody Chimeras for Targeted Membrane Protein Degradation |
JACS |
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2021 |
09 |
Zhang |
Machine learning modeling of protein-intrinsic features predicts tractability of targeted protein degradation |
bioRxiv |
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2021 |
09 |
Belcher |
Ligandability of E3 Ligases for Targeted Protein Degradation Applications |
Biochemistry |
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2021 |
08 |
Hughes |
The rise and rise of protein degradation: Opportunities and challenges ahead |
Drug Discovery Today |
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2021 |
08 |
Shao |
Destruction of DNA-Binding Proteins by Programmable Oligonucleotide PROTAC (O'PROTAC): Effective Targeting of LEF1 and ERG |
Advanced Science |
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2021 |
07 |
Schneider |
The PROTACtable genome |
Nature Reviews Drug Discovery |
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2021 |
07 |
Rodriguez-Rivera |
Unifying Catalysis Framework to Dissect Proteasomal Degradation Paradigms |
ACS Central Science |
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2021 |
07 |
Douglas |
Ternary Kinetic Models for Rational Design of Molecular Glues |
chemRxiv |
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2021 |
06 |
Reynders |
Optical control of targeted protein degradation |
Cell Chemical Biology |
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2021 |
06 |
Dale |
Advancing targeted protein degradation for cancer therapy |
Nature Reviews Cancer |
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2021 |
06 |
Liu |
TF-PROTACs Enable Targeted Degradation of Transcription Factors |
Journal of the American Chemical Society |
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2021 |
05 |
Kannt |
Expanding the arsenal of E3 ubiquitin ligases for proximity-induced protein degradation |
Cell Chemical Biology |
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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 |
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2021 |
05 |
Cecchini |
From Conception to Development: Investigating PROTACs Features for Improved Cell Permeability and Successful Protein Degradation |
Frontiers in Chemistry |
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2021 |
04 |
Jetvic |
An E3 ligase guide to the galaxy of small-molecule-induced protein degradation |
Cell Chemical Biology |
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2021 |
04 |
Henning |
Discovery of a Covalent FEM1B Recruiter for Targeted Protein Degradation Applications |
bioRxiv |
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2021 |
04 |
Henneberg |
Decoding the messaging of the ubiquitin system using chemical and protein probes |
Cell Chemical Biology |
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2021 |
04 |
Scholes |
Identification and selectivity profiling of small-molecule degraders via multi-omics approaches |
Cell Chemical Biology |
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2021 |
04 |
Farnaby |
Transforming targeted cancer therapy with PROTACs: A forward-looking perspective |
Current Opinion in Pharmacology |
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2021 |
03 |
Kiely-Collins |
The role of reversible and irreversible covalent chemistry in targeted protein degradation |
Cell Chemical Biology |
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2021 |
03 |
Zhang |
DCAF11 Supports Targeted Protein Degradation by Electrophilic Proteolysis-Targeting Chimeras |
JACS |
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2021 |
03 |
Castaldi |
Advances in Protein Degradation |
SLAS Discovery |
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2021 |
03 |
Ahn |
Degradation from the outside in: targeting extracellular and membrane proteins for degradation through the endolysosomal pathway |
Cell Chemical Biology |
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2021 |
03 |
Ege |
Phenotypic screening with target identification and validation in the discovery and development of E3 ligase modulators |
Cell Chemical Biology |
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2021 |
03 |
Bond |
Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation |
RSC Chemical Biology |
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2021 |
03 |
Ahn |
LYTACs that engage the asialoglycoprotein receptor for targeted protein degradation |
Nature Chemical Biology |
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2021 |
03 |
Pei |
Targeting Lysosomal Degradation Pathways: New Strategies and Techniques for Drug Discovery |
Journal of Medicinal Chemistry |
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2021 |
03 |
Jiang |
Discovery and resistance mechanism of a selective CDK12 degrader |
Nature Chemical Biology |
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2021 |
03 |
Hundley |
A comprehensive phenotypic CRISPR-Cas9 screen of the ubiquitin pathway uncovers roles of ubiquitin ligases in mitosis |
Molecular Cell |
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2021 |
03 |
Mullard |
Targeted protein degraders crowd into the clinic |
Nature Reviews Drug Discovery |
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2021 |
03 |
Spradlin |
Reimagining Druggability Using Chemoproteomic Platforms |
Accounts of Chemical Research |
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2021 |
03 |
Shao |
Destruction of DNA-binding proteins by programmable O’PROTAC: Oligonucleotide-based PROTAC |
bioRxiv |
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2021 |
03 |
Zheng |
Novel PROTACs for degradation of SHP2 protein |
Bioorganic Chemistry |
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2021 |
03 |
Jaeger |
Fast-acting chemical tools to delineate causality in transcriptional control |
Molecular Cell |
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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 |
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2021 |
03 |
Wang |
Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy |
Nature Chemical Biology |
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2021 |
03 |
Kim |
Avoid the trap: targeting PARP1 beyond human malignancy |
Cell Chemical Biology |
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2021 |
03 |
Jan |
Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide |
Nature Reviews Clinical Oncology |
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2021 |
03 |
Zhang |
Ubiquitination of Nonhistone Proteins in Cancer Development and Treatment |
Frontiers in Oncology |
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2021 |
03 |
Kastl |
Small-Molecule Degraders beyond PROTACs—Challenges and Opportunities |
SLAS Discovery |
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2021 |
02 |
Peter |
A novel, universally active C-terminal protein degradation signal generated by alternative splicing |
Journal of Molecular Biology |
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2021 |
02 |
Schreiber |
The Rise of Molecular Glues |
Cell |
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2021 |
02 |
Zhang |
SPIN4 Is a Principal Endogenous Substrate of the E3 Ubiquitin Ligase DCAF16 |
Biochemistry |
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2021 |
02 |
Kolb |
Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells |
Nature Communications |
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2021 |
02 |
Bai |
Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta |
Journal of Chemical Information and Modeling |
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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 |
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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 |
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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 |
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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 |
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2021 |
02 |
Kaiho-Soma |
TRIP12 promotes small-molecule-induced degradation through K29/K48-branched ubiquitin chains |
Molecular Cell |
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2021 |
02 |
Powell |
Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library |
ACS Chemical Biology |
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2021 |
02 |
Cao |
Recent insight into the role of RING-finger E3 ligases in glioma |
Biochemical Society Transactions |
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2021 |
02 |
Horn-Ghetko |
Ubiquitin ligation to F-box protein targets by SCF–RBR E3–E3 super-assembly |
Nature |
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2021 |
02 |
Koduri |
Targeting oncoproteins with a positive selection assay for protein degraders |
Science Advances |
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2021 |
02 |
Gabizon |
The rise of covalent proteolysis targeting chimeras |
Current Opinion in Chemical Biology |
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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 |
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2021 |
01 |
Kessler |
DUB esterase activity further decodes ubiquitin’s enigma |
PNAS |
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2021 |
01 |
De Cesare |
Deubiquitinating enzyme amino acid profiling reveals a class of ubiquitin esterases |
PNAS |
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2021 |
01 |
Yeh |
The C‐degron pathway eliminates mislocalized proteins and products of deubiquitinating enzymes |
EMBO Journal |
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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 |
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2021 |
01 |
Jan |
Reversible ON- and OFF-switch chimeric antigen receptors controlled by lenalidomide |
Science Translational Medicine |
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2021 |
01 |
Shirasaki |
Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins |
Cell Reports |
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2021 |
01 |
Benowitz |
The therapeutic potential of PROTACs |
Expert Opinion on Therapeutic Patents |
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2021 |
01 |
Yan |
Discovery of a PROTAC targeting ALK with in vivo activity |
European Journal of Medicinal Chemistry |
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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 |
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2021 |
01 |
Banchenko |
Structural insights into Cullin4-RING ubiquitin ligase remodelling by Vpr from simian immunodeficiency viruses |
bioRxiv |
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2021 |
01 |
Zeng |
Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges |
European Journal of Medicinal Chemistry |
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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 |
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2020 |
12 |
Caine |
Targeted Protein Degradation Phenotypic Studies Using HaloTag CRISPR/Cas9 Endogenous Tagging Coupled with HaloPROTAC3 |
Current Protocols in Pharmacology |
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2020 |
12 |
Leissing |
Structure driven compound optimization in targeted protein degradation |
Drug Discovery Today |
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2020 |
12 |
Tong |
Bardoxolone conjugation enables targeted protein degradation of BRD4 |
Scientific Reports |
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2020 |
12 |
Liu |
A Proteomic Platform to Identify Off-Target Proteins Associated with Therapeutic Modalities that Induce Protein Degradation or Gene Silencing |
bioRxiv |
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2020 |
12 |
Donovan |
Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development |
Cell |
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2020 |
11 |
Chatterjee |
Targeted intracellular degradation of SARS-CoV-2 via computationally optimized peptide fusions |
Communications Biology |
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2020 |
11 |
Matyskiela |
Cereblon Modulators Target ZBTB16 and Its Oncogenic Fusion Partners for Degradation via Distinct Structural Degrons |
ACS Chemical Biology |
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2020 |
11 |
Schiemer |
Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes |
Nature Chemical Biology |
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2020 |
11 |
Adhikari |
PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase |
Nature Chemical Biology |
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2020 |
10 |
Nabet |
Charting a New Path Towards Degrading Every Protein |
ChemBioChem |
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2020 |
10 |
Jiang |
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases |
European Journal of Medicinal Chemistry |
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2020 |
10 |
Ghidini |
RNA‐PROTACs – degraders of RNA‐binding proteins |
Angewandte Chemie International Edition |
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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 |
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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 |
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2020 |
10 |
Goracci |
Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications |
Journal of Medicinal Chemistry |
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2020 |
10 |
Miyamae |
A Method for Conditional Regulation of Protein Stability in Native or Near-Native Form |
Cell Chemical Biology |
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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 |
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2020 |
10 |
Bushman |
Proteomics-Based Identification of DUB Substrates Using Selective Inhibitors |
Cell Chemical Biology |
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2020 |
09 |
Furihata |
Structural bases of IMiD selectivity that emerges by 5-hydroxythalidomide |
Nature Communications |
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2020 |
09 |
Qin |
The therapeutic effect of the BRD4-degrading PROTAC A1874 in human colon cancer cells |
Cell Death and Disease |
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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 |
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2020 |
09 |
Simpson |
Inducible Degradation of Target Proteins through a Tractable Affinity-Directed Protein Missile System |
Cell Chemical Biology |
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2020 |
08 |
Nalawansha |
PROTACs: An Emerging Therapeutic Modality in Precision Medicine |
Cell Chemical Biology |
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2020 |
08 |
Liang |
Design and pharmaceutical applications of proteolysis-targeting chimeric molecules |
Biochemical Pharmacology |
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2020 |
08 |
Cipriano |
Targeting epigenetic reader domains by chemical biology |
Current Opinion in Chemical Biology |
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2020 |
08 |
Mayor-Ruiz |
Rational discovery of molecular glue degraders via scalable chemical profiling |
Nature Chemical Biology |
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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 |
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2020 |
07 |
Timms |
Tying up loose ends: the N-degron and C-degron pathways of protein degradation |
Biochemical Society Transactions |
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2020 |
07 |
Beveridge |
Native Mass Spectrometry Can Effectively Predict PROTAC Efficacy |
ACS Central Science |
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2020 |
07 |
Chung |
Structural Insights into PROTAC-Mediated Degradation of Bcl-xL |
ACS Chemical Biology |
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2020 |
07 |
Ruprecht |
A mass spectrometry-based proteome map of drug action in lung cancer cell lines |
Nature Chemical Biology |
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2020 |
06 |
Hanzl |
Targeted protein degradation: current and future challenges |
Current Opinion in Chemical Biology |
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2020 |
05 |
Luh |
Prey for the Proteasome: Targeted Protein Degradation – A Medicinal Chemist´s Perspective |
Angewandte Chemie International Edition |
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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 |
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2020 |
02 |
Deshaies |
Multispecific drugs herald a new era of biopharmaceutical innovation |
Nature |
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2020 |
02 |
Wang |
Degradation of proteins by PROTACs and other strategies |
Acta Pharmaceutica Sinica B |
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2020 |
01 |
Moreau |
Proteolysis‐targeting chimeras in drug development: A safety perspective |
British Journal of Pharmacology |
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2020 |
01 |
Gong |
Targeting Cullin-RING Ubiquitin Ligases and the Applications in PROTACs |
Advances in Experimental Medicine and Biology |
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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 |
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2019 |
10 |
Schapira |
Targeted protein degradation: expanding the toolbox |
Current Opinion in Chemical Biology |
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2019 |
10 |
Maple |
Developing degraders: principles and perspectives on design and chemical space |
MedChemComm |
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2019 |
09 |
Chamberlain |
Development of targeted protein degradation therapeutics |
Nature Chemical Biology |
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2019 |
08 |
Maniaci |
Bifunctional chemical probes inducing protein–protein interactions |
Current Opinion in Chemical Biology |
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2019 |
07 |
Spradlin |
Harnessing the anti-cancer natural product nimbolide for targeted protein degradation |
Nature Chemical Biology |
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2019 |
06 |
Ella |
The Hunt for Degrons of the 26S Proteasome |
Biomolecules |
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2019 |
04 |
Paiva |
Targeted protein degradation: elements of PROTAC design |
Current Opinion in Chemical Biology |
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2019 |
04 |
Roth |
Advances in targeted degradation of endogenous proteins |
Cellular and Molecular Life Sciences |
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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 |
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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 |
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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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