Antibody‒drug conjugates: Recent advances in linker chemistry

Bis(vinylsulfonyl)piperazines as efficient linkers for highly homogeneous antibody-drug conjugates

(2020) Rong Huang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Reducing the antigen-independent toxicity of antibody-drug conjugates by minimizing their non-specific clearance through PEGylation

(2020) Jessica K. Simmons et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Antibody-Drug Conjugate Using Ionized Cys-Linker-MMAE as the Potent Payload Shows Optimal Therapeutic Safety

(2020) Yanming Wang et al.   Cancers

FDA Approval Summary: Enfortumab Vedotin for Locally Advanced or Metastatic Urothelial Carcinoma

(2020) Elaine Chang et al.   CLINICAL CANCER RESEARCH

Belantamab Mafodotin: First Approval

(2020) Anthony Markham   DRUGS

An Efficient Conjugation Approach for Coupling Drugs to Native Antibodies via the Pt II Linker Lx for Improved Manufacturability of Antibody–Drug Conjugates

(2020) Eugen Merkul et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Aryl Sulfate is a Useful Motif for Conjugating and Releasing Phenolic Molecules: Sulfur Fluorine Exchange Click Chemistry Enables Discovery of Ortho-Hydroxy-Protected Aryl Sulfate Linker

(2019) Suho Park et al.   BIOCONJUGATE CHEMISTRY

Exposure-Efficacy Analysis of Antibody-Drug Conjugates Delivering an Excessive Level of Payload to Tissues

(2019) Donglu Zhang et al.   DRUG METABOLISM AND DISPOSITION

First platinum(II)-based metal-organic linker technology (Lx®) for a plug-and-play development of antibody-drug conjugates (ADCs)

(2019) Eugen Merkul et al.   Expert Opinion on Drug Delivery

Effect of Linker Stereochemistry on the Activity of Indolinobenzodiazepine Containing Antibody–Drug Conjugates (ADCs)

(2019) Emily E. Reid et al.   ACS Medicinal Chemistry Letters

Novel Silyl Ether-Based Acid-Cleavable Antibody-MMAE Conjugates with Appropriate Stability and Efficacy

(2019) Yanming Wang et al.   Cancers

Hydrophilic Sequence-Defined Cross-Linkers for Antibody–Drug Conjugates

(2019) Joshua A. Walker et al.   BIOCONJUGATE CHEMISTRY

Correction to: Polatuzumab Vedotin: First Global Approval

(2019) Emma D. Deeks   DRUGS

Copper-Triggered Bioorthogonal Cleavage Reactions for Reversible Protein and Cell Surface Modifications

(2019) Xin Wang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Optimizing Lysosomal Activation of Antibody–Drug Conjugates (ADCs) by Incorporation of Novel Cleavable Dipeptide Linkers

(2019) Paulin L. Salomon et al.   MOLECULAR PHARMACEUTICS

Cellular Delivery of Bioorthogonal Pretargeting Therapeutics in PSMA-Positive Prostate Cancer

(2019) Sudath Hapuarachchige et al.   MOLECULAR PHARMACEUTICS

A Switchable Site-Specific Antibody Conjugate

(2018) Zhigang Lyu et al.   ACS Chemical Biology

Site-specific and hydrophilic ADCs through disulfide-bridged linker and branched PEG

(2018) Shuai Shao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Intratumoral Payload Concentration Correlates with the Activity of Antibody–Drug Conjugates

(2018) Donglu Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Toward a Ferrous Iron-Cleavable Linker for Antibody–Drug Conjugates

(2018) Benjamin Spangler et al.   MOLECULAR PHARMACEUTICS

Moxetumomab Pasudotox: First Global Approval

(2018) Sohita Dhillon   DRUGS

N-Methyl-N-phenylvinylsulfonamides for Cysteine-Selective Conjugation

(2018) Rong Huang et al.   ORGANIC LETTERS

Targeting CD74 in multiple myeloma with the novel, site-specific antibody-drug conjugate STRO-001

(2018) Cristina L. Abrahams et al.   Oncotarget

Development and evaluation of β-galactosidase-sensitive antibody-drug conjugates

(2017) Sergii Kolodych et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development and Properties of Valine-Alanine based Antibody-Drug Conjugates with Monomethyl Auristatin E as the Potent Payload

(2017) Yanming Wang et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Pyrrolobenzodiazepine Dimer Antibody–Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers

(2017) Stephen J. Gregson et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2017) BinQing Wei et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2017) Thomas H. Pillow et al.   MOLECULAR CANCER THERAPEUTICS

Structural investigation of cyclo-dioxo maleimide cross-linkers for acid and serum stability

(2017) Elisabetta Tobaldi et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

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

(2017) Thomas H. Pillow et al.   Chemical Science

Understanding How the Stability of the Thiol-Maleimide Linkage Impacts the Pharmacokinetics of Lysine-Linked Antibody–Maytansinoid Conjugates

(2016) Jose F. Ponte et al.   BIOCONJUGATE CHEMISTRY

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

(2016) Jeffrey C. Kern et al.   BIOCONJUGATE CHEMISTRY

A Novel Platinum(II)–Based Bifunctional ADC Linker Benchmarked Using89Zr-Desferal and Auristatin F–Conjugated Trastuzumab

(2016) Niels J. Sijbrandi et al.   CANCER RESEARCH

A Novel Tumor-Activated Prodrug Strategy Targeting Ferrous Iron Is Effective in Multiple Preclinical Cancer Models

(2016) Benjamin Spangler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Pyrophosphate Diesters as Tunable, Soluble, and Bioorthogonal Linkers for Site-Specific Antibody–Drug Conjugates

(2016) Jeffrey C. Kern et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Molecular Basis of Valine-Citrulline-PABC Linker Instability in Site-Specific ADCs and Its Mitigation by Linker Design

(2016) M. Dorywalska et al.   MOLECULAR CANCER THERAPEUTICS

Development of Novel Quaternary Ammonium Linkers for Antibody-Drug Conjugates

(2016) P. J. Burke et al.   MOLECULAR CANCER THERAPEUTICS

A New Triglycyl Peptide Linker for Antibody–Drug Conjugates (ADCs) with Improved Targeted Killing of Cancer Cells

(2016) Rajeeva Singh et al.   MOLECULAR CANCER THERAPEUTICS

2-(Maleimidomethyl)-1,3-Dioxanes (MD): a Serum-Stable Self-hydrolysable Hydrophilic Alternative to Classical Maleimide Conjugation

(2016) Igor Dovgan et al.   Scientific Reports

Near-IR Light-Mediated Cleavage of Antibody-Drug Conjugates Using Cyanine Photocages

(2015) Roger R. Nani et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Site-Specific Dual Antibody Conjugation via Engineered Cysteine and Selenocysteine Residues

(2015) Xiuling Li et al.   BIOCONJUGATE CHEMISTRY

Fate of Patients with Newly Diagnosed Acute Myeloid Leukemia Who Fail Primary Induction Therapy

(2015) Megan Othus et al.   BIOLOGY OF BLOOD AND MARROW TRANSPLANTATION

Platinum(II) as Bifunctional Linker in Antibody-Drug Conjugate Formation: Coupling of a 4-Nitrobenzo-2-oxa-1,3-diazole Fluorophore to Trastuzumab as a Model

(2015) Dennis C. J. Waalboer et al.   ChemMedChem

Enhanced Delivery of SN-38 to Human Tumor Xenografts with an Anti-Trop-2-SN-38 Antibody Conjugate (Sacituzumab Govitecan)

(2015) R. M. Sharkey et al.   CLINICAL CANCER RESEARCH

Stabilization of cysteine-linked antibody drug conjugates with N-aryl maleimides

(2015) R. James Christie et al.   JOURNAL OF CONTROLLED RELEASE

Recent Advances in the Development of New Auristatins: Structural Modifications and Application in Antibody Drug Conjugates

(2015) Andreas Maderna et al.   MOLECULAR PHARMACEUTICS

Novel antibody–antibiotic conjugate eliminates intracellular S. aureus

(2015) Sophie M. Lehar et al.   NATURE

Reducing hydrophobicity of homogeneous antibody-drug conjugates improves pharmacokinetics and therapeutic index

(2015) Robert P Lyon et al.   NATURE BIOTECHNOLOGY

Bridging Disulfides for Stable and Defined Antibody Drug Conjugates

(2014) George Badescu et al.   BIOCONJUGATE CHEMISTRY

Long-Term Stabilization of Maleimide–Thiol Conjugates

(2014) Shaun D. Fontaine et al.   BIOCONJUGATE CHEMISTRY

Ado-trastuzumab Emtansine (T-DM1): An Antibody–Drug Conjugate (ADC) for HER2-Positive Breast Cancer

(2014) John M. Lambert et al.   JOURNAL OF MEDICINAL CHEMISTRY

Site-Specific Trastuzumab Maytansinoid Antibody–Drug Conjugates with Improved Therapeutic Activity through Linker and Antibody Engineering

(2014) Thomas H. Pillow et al.   JOURNAL OF MEDICINAL CHEMISTRY

Self-hydrolyzing maleimides improve the stability and pharmacological properties of antibody-drug conjugates

(2014) Robert P Lyon et al.   NATURE BIOTECHNOLOGY

UV Radiation and the Skin

(2013) John D'Orazio et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Milatuzumab-SN-38 Conjugates for the Treatment of CD74+ Cancers

(2013) S. V. Govindan et al.   MOLECULAR CANCER THERAPEUTICS

Maturing antibody–drug conjugate pipeline hits 30

(2013) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Synthesis and Evaluation of Hydrophilic Linkers for Antibody–Maytansinoid Conjugates

(2011) Robert Y. Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phase I Study of Trastuzumab-DM1, an HER2 Antibody-Drug Conjugate, Given Every 3 Weeks to Patients With HER2-Positive Metastatic Breast Cancer

(2010) Ian E. Krop et al.   JOURNAL OF CLINICAL ONCOLOGY

Aggregation Control of Squaraines and Their Use as Near-Infrared Fluorescent Sensors for Protein

(2010) Yongqian Xu et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Brentuximab Vedotin (SGN-35) for Relapsed CD30-Positive Lymphomas

(2010) Anas Younes et al.   NEW ENGLAND JOURNAL OF MEDICINE

Sensors and regulators of intracellular pH

(2009) Joseph R. Casey et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

First Total Synthesis of Tubulysin B

(2009) Orlando Pando et al.   ORGANIC LETTERS

The azaquinone-methide elimination: comparison study of 1,6- and 1,4-eliminations under physiological conditions

(2008) Rotem Erez et al.   ORGANIC & BIOMOLECULAR CHEMISTRY