Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

Selective inhibition of BET bromodomains

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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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Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer

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THE COVALENT STRUCTURE OF AN ENTIRE γG IMMUNOGLOBULIN MOLECULE

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

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Bystander killing effect of <scp>DS</scp> ‐8201a, a novel anti‐human epidermal growth factor receptor 2 antibody–drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity

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

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Site-Specific Antibody–Drug Conjugates: The Nexus of Bioorthogonal Chemistry, Protein Engineering, and Drug Development

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Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

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PROTACs: An Emerging Therapeutic Modality in Precision Medicine

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Site-selective modification strategies in antibody–drug conjugates

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BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment

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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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Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

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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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Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

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

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Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

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

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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

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Antibody–PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4

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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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Intracellular Released Payload Influences Potency and Bystander-Killing Effects of Antibody-Drug Conjugates in Preclinical Models

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Drug Discovery Targeting Bromodomain-Containing Protein 4

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Small-Molecule Modulation of Protein Homeostasis

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Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective

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A Potent Anti-CD70 Antibody–Drug Conjugate Combining a Dimeric Pyrrolobenzodiazepine Drug with Site-Specific Conjugation Technology

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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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Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery

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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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Tubulin Inhibitor-Based Antibody-Drug Conjugates for Cancer Therapy

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Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy

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Cathepsin B Is Dispensable for Cellular Processing of Cathepsin B-Cleavable Antibody–Drug Conjugates

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Design and Synthesis of Tesirine, a Clinical Antibody–Drug Conjugate Pyrrolobenzodiazepine Dimer Payload

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Developing degraders: principles and perspectives on design and chemical space

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Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies

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SLC46A3 Is Required to Transport Catabolites of Noncleavable Antibody Maytansine Conjugates from the Lysosome to the Cytoplasm

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Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates

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Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

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Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions

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Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

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A chemical approach for global protein knockdown from mice to non-human primates

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Discovery of Peptidomimetic Antibody–Drug Conjugate Linkers with Enhanced Protease Specificity

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High-Throughput Cysteine Scanning To Identify Stable Antibody Conjugation Sites for Maleimide- and Disulfide-Based Linkers

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Monodisperse polysarcosine-based highly-loaded antibody-drug conjugates

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GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins

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Novel Phosphate Modified Cathepsin B Linkers: Improving Aqueous Solubility and Enhancing Payload Scope of ADCs

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SLC46A3 as a Potential Predictive Biomarker for Antibody–Drug Conjugates Bearing Noncleavable Linked Maytansinoid and Pyrrolobenzodiazepine Warheads

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A Novel Anti-HER2 Antibody–Drug Conjugate XMT-1522 for HER2-Positive Breast and Gastric Cancers Resistant to Trastuzumab Emtansine

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The Methylene Alkoxy Carbamate Self‐Immolative Unit: Utilization for the Targeted Delivery of Alcohol‐Containing Payloads with Antibody–Drug Conjugates

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Processes for Constructing Homogeneous Antibody Drug Conjugates

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The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor

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Modulating Therapeutic Activity and Toxicity of Pyrrolobenzodiazepine Antibody–Drug Conjugates with Self-Immolative Disulfide Linkers

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Direct Measurement of Intracellular Compound Concentration by RapidFire Mass Spectrometry Offers Insights into Cell Permeability

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