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Catalytic in vivo protein knockdown by small-molecule PROTACs

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Structural basis of PROTAC cooperative recognition for selective protein degradation

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Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

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Targeted protein degradation: expanding the toolbox

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Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

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Single-particle cryo-EM at atomic resolution

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PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

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The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

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PROTACs: great opportunities for academia and industry

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Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

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HECT and RING finger families of E3 ubiquitin ligases at a glance

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Modular PROTAC design for the degradation of oncogenic BCR-ABL

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Plasticity in binding confers selectivity in ligand-induced protein degradation

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Targeted protein degradation: elements of PROTAC design

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The proteasome: structure, function, and role in the cell

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BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

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Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

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Chemical Genetic Control of Protein Levels: Selective in Vivo Targeted Degradation

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Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

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Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

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A Comprehensive Mathematical Model for Three-Body Binding Equilibria

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A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader

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Development of Protacs to Target Cancer-promoting Proteins for Ubiquitination and Degradation

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Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

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Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

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Delineating the role of cooperativity in the design of potent PROTACs for BTK

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Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

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Protein Knockdown Using Methyl Bestatin−Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins

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Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer

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Beyond the Rule of 5: Lessons Learned from AbbVie’s Drugs and Compound Collection

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SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate

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Light-Induced Protein Degradation with Photocaged PROTACs

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Two Decades under the Influence of the Rule of Five and the Changing Properties of Approved Oral Drugs.

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The demographics of the ubiquitin system

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Acquired Resistance to BET-PROTACs (Proteolysis-Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 Ligase Complexes

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MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

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How Beyond Rule of 5 Drugs and Clinical Candidates Bind to Their Targets

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Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7

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Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications

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PHOTACs enable optical control of protein degradation

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Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs

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Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

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Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway

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Light-induced control of protein destruction by opto-PROTAC

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Small‐Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

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PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

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Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models

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Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

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Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals)

Schiedel, M., Herp, D., Hammelmann, S., Swyter, S., Lehotzky, A., Robaa, D., Oláh, J., Ovádi, J., Sippl, W., & Jung, M. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01872 · Cited by 275 · see citing works

Exploring Targeted Degradation Strategy for Oncogenic KRASG12C

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Deep Generative Models for 3D Linker Design

Imrie, F., Bradley, A. R., van der Schaar, M., & Deane, C. M. (2020) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.9b01120 · Cited by 268 · see citing works

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

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Small-Molecule Modulation of Protein Homeostasis.

Burslem, G., & Crews, C. (2017) · Chemical Reviews · doi:10.1021/acs.chemrev.7b00077 · Cited by 256 · see citing works

Structure‐Based Design of a Macrocyclic PROTAC

Testa, A., Hughes, S. J., Lucas, X., Wright, J. E., & Ciulli, A. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201914396 · Cited by 251 · see citing works

Specific Knockdown of Endogenous Tau Protein by Peptide-Directed Ubiquitin-Proteasome Degradation

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Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation

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In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

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Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders

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Targeting Cullin–RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation

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Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations

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Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein

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Impact of linker length on the activity of PROTACs

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Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2

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Optical Control of Small Molecule-Induced Protein Degradation

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PRosettaC: Rosetta Based Modeling of PROTAC Mediated Ternary Complexes

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Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

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ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer.

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A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation

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Antibody Conjugation of a Chimeric BET Degrader Enables <i>in vivo</i> Activity

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Efficient targeted degradation via reversible and irreversible covalent PROTACs

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Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders

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Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders

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Development of the first small molecule histone deacetylase 6 (HDAC6) degraders

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Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders

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Inducible In Vivo Silencing of Brd4 Identifies Potential Toxicities of Sustained BET Protein Inhibition

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Azo-PROTAC: Novel Light-Controlled Small-Molecule Tool for Protein Knockdown

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PROTACs: A novel strategy for cancer therapy

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Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule

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Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader

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Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation

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Fundamental aspects of DMPK optimization of targeted protein degraders

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SNIPERs—Hijacking IAP activity to induce protein degradation

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Pharmacokinetics, metabolism and distribution of PEGs and PEGylated proteins: quo vadis?

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Developing degraders: principles and perspectives on design and chemical space

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Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta

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Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders

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Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands

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First targeted protein degrader hits the clinic

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Chiral Inversion and Hydrolysis of Thalidomide: Mechanisms and Catalysis by Bases and Serum Albumin, and Chiral Stability of Teratogenic Metabolites

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Design, synthesis and biological evaluation of nuclear receptor-degradation inducers

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A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

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Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity

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Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6

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A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

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Selective degradation of CDK6 by a palbociclib based PROTAC

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Targeting IRAK4 for Degradation with PROTACs

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Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel–Lindau (VHL) E3 Ubiquitin Ligase

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Developing potent PROTACs tools for selective degradation of HDAC6 protein

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PROTACs suppression of CDK4/6, crucial kinases for cell cycle regulation in cancer

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Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand

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Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity

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PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes

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Why Some Targets Benefit from beyond Rule of Five Drugs

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Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands

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Harnessing the hypoxia-inducible factor in cancer and ischemic disease

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Design and synthesis of selective degraders of EGFRL858R/T790M mutant

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Plasticity in designing PROTACs for selective and potent degradation of HDAC6

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Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation

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PROTAC-mediated crosstalk between E3 ligases

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Bifunctional chemical probes inducing protein–protein interactions

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Opportunities and guidelines for discovery of orally absorbed drugs in beyond rule of 5 space

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Targeted Degradation of the Aryl Hydrocarbon Receptor by the PROTAC Approach: A Useful Chemical Genetic Tool

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Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader

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Fragment-based drug discovery using cryo-EM

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Jostling for Position: Optimizing Linker Location in the Design of Estrogen Receptor‐Targeting PROTACs

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Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)

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Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties

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Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-X _L

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Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction

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Systematic Investigation of the Permeability of Androgen Receptor PROTACs

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Development of selective small molecule MDM2 degraders based on nutlin

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Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs

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Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology

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Cryo-EM for Small Molecules Discovery, Design, Understanding, and Application

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Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders

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A MedChem toolbox for cereblon-directed PROTACs

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Degradation of target protein in living cells by small-molecule proteolysis inducer

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Is NMR Fragment Screening Fine-Tuned to Assess Druggability of Protein–Protein Interactions?

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Single-particle cryo-EM at atomic resolutionPreprint

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Design and synthesis of α-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation

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New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition

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Triazol: A Privileged Scaffold for Proteolysis Targeting Chimeras

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Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition

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Targeted protein degradation mechanisms

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Development of a PDEδ‐Targeting PROTACs that Impair Lipid Metabolism

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Disordered region of cereblon is required for efficient degradation by proteolysis-targeting chimera

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Scaffold hopping enables direct access to more potent PROTACs with in vivo activity

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Development of PROTACs to address clinical limitations associated with BTK-targeted kinase inhibitors

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Stick it to E3s

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A Caged E3 Ligase Ligand for PROTAC-Mediated Protein Degradation with LightPreprint

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Untitled work

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PROTAC targeted protein degraders: the past is prologue

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Triazoles in Medicinal Chemistry: Physicochemical Properties, Bioisosterism, and Application

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Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood–Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2

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Recent developments in epigenetic cancer therapeutics: clinical advancement and emerging trends

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Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation

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The role of reversible and irreversible covalent chemistry in targeted protein degradation

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Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation

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Linker-Dependent Folding Rationalizes PROTAC Cell Permeability

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Microneedle Patch Delivery of PROTACs for Anti-Cancer Therapy

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PROTAC’ing oncoproteins: targeted protein degradation for cancer therapy

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Deep generative design with 3D pharmacophoric constraints

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Annual review of PROTAC degraders as anticancer agents in 2022

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Delivering on the promise of protein degraders

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What is in Our Kit? An Analysis of Building Blocks Used in Medicinal Chemistry Parallel Libraries

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Designing Soluble PROTACs: Strategies and Preliminary Guidelines

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Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization

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Glutathione‐Scavenging Nanoparticle‐Mediated PROTACs Delivery for Targeted Protein Degradation and Amplified Antitumor Effects

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Exploring the target scope of KEAP1 E3 ligase-based PROTACs

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Molecular Strategies to Target Protein Aggregation in Huntington’s Disease

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Noncovalent CDK12/13 dual inhibitors-based PROTACs degrade CDK12-Cyclin K complex and induce synthetic lethality with PARP inhibitor

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Degrader–Antibody Conjugates: Emerging New Modality

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Discovery of Small-Molecule Degraders of the CDK9-Cyclin T1 Complex for Targeting Transcriptional Addiction in Prostate Cancer

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De Novo Design of an Androgen Receptor DNA Binding Domain‐Targeted peptide PROTAC for Prostate Cancer Therapy

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Targeting the Ubiquitin-Proteasome System for Cancer Therapeutics by Small-Molecule Inhibitors

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DNA-Encoded Library Screening To Inform Design of a Ribonuclease Targeting Chimera (RiboTAC)

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Trends in Molecular Properties, Bioavailability, and Permeability across the Bayer Compound Collection: Miniperspective

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Advancing targeted protein degradation for metabolic diseases therapy

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Optical control of targeted protein degradation

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Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands

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Lenalidomide derivatives and proteolysis-targeting chimeras for controlling neosubstrate degradation

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Computer-Aided Drug Discovery for Undruggable Targets

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Allostery: Allosteric Cancer Drivers and Innovative Allosteric Drugs

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Strategies to Reduce the On‐Target Platelet Toxicity of Bcl‐x L Inhibitors: PROTACs, SNIPERs and Prodrug‐Based Approaches

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A Versatile and Sustainable Multicomponent Platform for the Synthesis of Protein Degraders: Proof-of-Concept Application to BRD4-Degrading PROTACs

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Small-Molecule Ferritin Degrader as a Pyroptosis Inducer

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Degradation of neurodegenerative disease-associated TDP-43 aggregates and oligomers via a proteolysis-targeting chimera

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Multimodal targeting chimeras enable integrated immunotherapy leveraging tumor-immune microenvironment

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A beginner’s guide to current synthetic linker strategies towards VHL-recruiting PROTACs

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Insight into Recent Advances in Degrading Androgen Receptor for Castration-Resistant Prostate Cancer

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Advancement of Targeted Protein Degradation Strategies As Therapeutics for Undruggable Disease Targets

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Identification and Characterization of a Novel Brain-Penetrant Indoleamine 2,3 Dioxygenase 1 Protein Degrader for Glioblastoma

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AI-Integrated QSAR Modeling for Enhanced Drug Discovery: From Classical Approaches to Deep Learning and Structural Insight

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DNA framework-engineered chimeras platform enables selectively targeted protein degradation

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Drug design targeting active posttranslational modification protein isoforms

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Proteolysis-Targeting Chimera (PROTAC) Delivery into the Brain across the Blood-Brain Barrier

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PROTACs and Building Blocks: The 2D Chemical Space in Very Early Drug Discovery

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Impact of Linker Composition on VHL PROTAC Cell Permeability

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PROTACs bearing piperazine-containing linkers: what effect on their protonation state?

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Discovery of a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid Leukemia

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Oral Absorption of Middle-to-Large Molecules and Its Improvement, with a Focus on New Modality Drugs

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Application and challenges of nitrogen heterocycles in PROTAC linker

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Lessons learned in linking PROTACs from discovery to the clinic

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A Top-Down Design Approach for Generating a Peptide PROTAC Drug Targeting Androgen Receptor for Androgenetic Alopecia Therapy

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Radioactive ADME Demonstrates ARV-110’s High Druggability Despite Low Oral Bioavailability

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Tau degradation in Alzheimer's disease: Mechanisms and therapeutic opportunities

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Discovery of LL-K8-22: A Selective, Durable, and Small-Molecule Degrader of the CDK8-Cyclin C Complex

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PROTAC-Induced Glycogen Synthase Kinase 3β Degradation as a Potential Therapeutic Strategy for Alzheimer’s Disease

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Journey of Von Hippel-Lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degraders

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Accelerating PROTACs Discovery Through a Direct‐to‐Biology Platform Enabled by Modular Photoclick Chemistry

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Molecular glues and PROTACs in targeted protein degradation: mechanisms, advances, and therapeutic potential

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Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy

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PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs

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Options to Improve the Action of PROTACs in Cancer: Development of Controlled Delivery Nanoparticles

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Towards design of drugs and delivery systems with the Martini coarse-grained model

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DiffPROTACs is a deep learning-based generator for proteolysis targeting chimeras

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ByeTAC: Bypassing E-Ligase-Targeting Chimeras for Direct Proteasome Degradation

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Designing HDAC-PROTACs: Lessons Learned So Far

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Fragment Linker Prediction Using the Deep Encoder-Decoder Network for PROTACs Drug Design

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Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors

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PROTAC: targeted drug strategy. Principles and limitations

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Targeting PRMT5 through PROTAC for the treatment of triple-negative breast cancer

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Targeted degradation of extracellular proteins: state of the art and diversity of degrader designs

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PROTACs: Current Trends in Protein Degradation by Proteolysis-Targeting Chimeras

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Selective Wee1 degradation by PROTAC degraders recruiting VHL and CRBN E3 ubiquitin ligases

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What influences the activity of Degrader−Antibody conjugates (DACs)

Guo, Y., Li, X., Xie, Y., & Wang, D. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116216 · Cited by 35 · see citing works

PROTACable Is an Integrative Computational Pipeline of 3-D Modeling and Deep Learning To Automate the De Novo Design of PROTACs

Mslati, H., Gentile, F., Pandey, M. K., Ban, F., & Cherkasov, A. R. (2024) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.3c01878 · Cited by 34 · see citing works

IMHB-Mediated Chameleonicity in Drug Design: A Focus on Structurally Related PROTACs

Jiménez, D. G., Sebastiano, M. R., Vallaro, M., Ermondi, G., & Caron, G. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01200 · Cited by 34 · see citing works

Design of Tracers in Fluorescence Polarization Assay for Extensive Application in Small Molecule Drug Discovery

Hua, L., Wang, D., Wang, K., Wang, Y., Gu, J., Zhang, Q., You, Q., & Wang, L. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00881 · Cited by 33 · see citing works

Target protein degradation by protacs: A budding cancer treatment strategy

Choudhary, D., Kaur, A., Singh, P., Chaudhary, G., Kaur, R., Bayan, M. F., Chandrasekaran, B., Marji, S. M., & Ayman, R. (2023) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2023.108525 · Cited by 31 · see citing works

The efflux pump ABCC1/MRP1 constitutively restricts PROTAC sensitivity in cancer cells

Wolf, G., Craigon, C., Teoh, S. T., Essletzbichler, P., Onstein, S., Cassidy, D. M., Uijttewaal, E. C. H., Dvorak, V., Cao, Y., Bensimon, A., et al. (2025) · Cell chemical biology · doi:10.1016/j.chembiol.2024.11.009 · Cited by 31 · see citing works

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

Current strategies for improving limitations of proteolysis targeting chimeras

Pu, C., Wang, S., Liu, L., Feng, Z., Zhang, H., Gong, Q., Sun, Y., Guo, Y., & Li, R. (2022) · Chinese Chemical Letters · doi:10.1016/j.cclet.2022.107927 · Cited by 29 · see citing works

Distinct Amino Acid-Based PROTACs Target Oncogenic Kinases for Degradation in Non-Small Cell Lung Cancer (NSCLC)

Zhang, J., Chen, X., Chen, C., Li, F., Song, X., Liu, C., Liao, K., Su, M.-Y., Tan, C. S. H., Fang, L., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00208 · Cited by 28 · see citing works

A comprehensive review of emerging approaches in machine learning for de novo PROTAC design

Gharbi, Y., & Mercado, R. (2024) · Digital Discovery · doi:10.1039/d4dd00177j · Cited by 31 · see citing works

An Autophagy-Targeting Chimera Induces Degradation of Androgen Receptor Mutants and AR-v7 in Castration-Resistant Prostate Cancer

Bae, T. H., Sung, K. W., Pham, T. M., Najy, A. J., Zamiri, A., Jang, H., Mun, S. R., Kim, S., Kwon, H.-K., Son, Y. S., et al. (2024) · Cancer Research · doi:10.1158/0008-5472.can-24-0591 · Cited by 30 · see citing works

Protacs in cancer therapy: mechanisms, design, clinical trials, and future directions

Vikal, A., Maurya, R., Patel, B. B., Sharma, R. K., Patel, P., Patil, U. K., & Kurmi, B. D. (2024) · Drug Delivery and Translational Research · doi:10.1007/s13346-024-01754-z · Cited by 28 · see citing works

Bifunctional degraders of cyclin dependent kinase 9 (CDK9): Probing the relationship between linker length, properties, and selective protein degradation

Tokarski, R. J., Sharpe, C., Huntsman, A. C., Mize, B. K., Ayinde, O. R., Stahl, E. H., Lerma, J. R., Reed, A., Carmichael, B., Muthusamy, N., et al. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115342 · Cited by 28 · see citing works

The new direction of drug development: Degradation of undruggable targets through targeting chimera technology

Liang, X., Ren, H., Han, F., Liang, R., Zhao, J., & Liu, H. S. (2023) · Medicinal Research Reviews · doi:10.1002/med.21992 · Cited by 28 · see citing works

Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity

Hu, J., Xu, H., Wu, T., Zhang, C., Shen, H., Dong, R., Hu, Q., Xiang, Q., Chai, S., Luo, G., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c02195 · Cited by 27 · see citing works

Rational Design and Optimization of a Potent IDO1 Proteolysis Targeting Chimera (PROTAC)

Monsen, P. J., Bommi, P. V., Grigorescu, A. A., Lauing, K. L., Mao, Y., Berardi, P., Zhai, L., Ojo, O., Penco-Campillo, M., Koch, T., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00026 · Cited by 27 · see citing works

Discovery and Characterization of RP03707: A Highly Potent and Selective KRAS G12D PROTAC

Ji, X. L., Li, H., Wu, G., Zhang, Q., He, X., Wu, Y., Zong, B., Xu, X., Liang, C., Wang, B., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00428 · Cited by 28 · see citing works

PROTAC Technology as a New Tool for Modern Pharmacotherapy

Kubryń, N., Fijałkowski, Ł., Nowaczyk, J., Jamil, A., & Nowaczyk, A. (2025) · Molecules · doi:10.3390/molecules30102123 · Cited by 28 · see citing works

A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras

Cross, J. M., Coulson, M. E., Smalley, J. P., Pytel, W. A., Ismail, O., Trory, J. S., Cowley, S. M., & Hodgkinson, J. T. (2022) · RSC Medicinal Chemistry · doi:10.1039/d2md00199c · Cited by 27 · see citing works

Computer aided drug design in the development of proteolysis targeting chimeras

Tunjic, T. M., Weber, N., & Brunsteiner, M. (2023) · Computational and Structural Biotechnology Journal · doi:10.1016/j.csbj.2023.02.042 · Cited by 27 · see citing works

Reversible Assembly of Proteolysis Targeting Chimeras

Gui, W., Giardina, S. F., Balzarini, M., Barany, F., & Kodadek, T. J. (2023) · ACS Chemical Biology · doi:10.1021/acschembio.3c00199 · Cited by 27 · see citing works

Novel approaches for the rational design of PROTAC linkers

Zagidullin, A. A., Milyukov, V. A., Rizvanov, A. A., & Bulatov, E. (2020) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2020.00023 · Cited by 70 · see citing works

Generative Models for PROTAC Linker Design Using Ternary Complex Geometry and Degradation Data

Wright, E., Bennett, C., & Turner, J. (2026) · Pharmacophore · doi:10.51847/jr4vtce12r

Linker attachment points: “finishing touch” in PROTAC design

jiang, Q., Shi, H.-S., Zhao, C.-S., Wang, Z.-Y., Yu, M.-M., Zhang, X.-Y., & Liu, C.-J. (2026) · RSC Medicinal Chemistry · doi:10.1039/d6md00346j

Characteristic roadmap of linker governs the rational design of PROTACs

Dong, Y., Ma, T., Xu, T., Feng, Z., Li, Y., Song, L., Yao, X., Ashby, C. R., & Hao, G.-F. (2024) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2024.04.007 · Cited by 146 · see citing works

Linkerology in PROTACs: learnings for proximity-inducing therapeutics

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