The renaissance of chemically generated bispecific antibodies

A Plug-and-Play Approach for the De Novo Generation of Dually Functionalized Bispecifics

(2020) Antoine Maruani et al.   BIOCONJUGATE CHEMISTRY

Cysteine-specific protein multi-functionalization and disulfide bridging using 3-bromo-5-methylene pyrrolones

(2020) Yingqian Zhang et al.   Nature Communications

A Bioorthogonal Click Chemistry Toolbox for Targeted Synthesis of Branched and Well‐Defined Protein–Protein Conjugates

(2020) Mathis Baalmann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Disulfide Modified IgG1: An Investigation of Biophysical Profile and Clinically Relevant Fc Interactions

(2019) Calise Bahou et al.   BIOCONJUGATE CHEMISTRY

Bispecific antibodies: a mechanistic review of the pipeline

(2019) Aran F. Labrijn et al.   NATURE REVIEWS DRUG DISCOVERY

Emicizumab: A Review in Haemophilia A

(2019) Hannah A. Blair   DRUGS

Probody Therapeutics: An Emerging Class of Therapies Designed to Enhance On-Target Effects with Reduced Off-Tumor Toxicity for Use in Immuno-Oncology

(2019) Karen A. Autio et al.   CLINICAL CANCER RESEARCH

Tuning the Hydrolytic Stability of Next Generation Maleimide Cross-Linkers Enables Access to Albumin-Antibody Fragment Conjugates and tri-scFvs

(2018) Nafsika Forte et al.   BIOCONJUGATE CHEMISTRY

Highly homogeneous antibody modification through optimisation of the synthesis and conjugation of functionalised dibromopyridazinediones

(2018) Calise Bahou et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Cell-type specific potent Wnt signaling blockade by bispecific antibody

(2018) Nam-Kyung Lee et al.   Scientific Reports

Expanding the Boundaries of Biotherapeutics with Bispecific Antibodies

(2018) Bushra Husain et al.   BIODRUGS

Preparation of bispecific antibody-protein adducts by site-specific chemo-enzymatic conjugation

(2018) Lina Bartels et al.   METHODS

Avidity-based binding to HER2 results in selective killing of HER2-overexpressing cells by anti-HER2/CD3

(2018) Dionysos Slaga et al.   Science Translational Medicine

Gemtuzumab ozogamicin in acute myeloid leukemia

(2017) C D Godwin et al.   LEUKEMIA

bisFabs: Tools for rapidly screening hybridoma IgGs for their activities as bispecific antibodies

(2017) Sanket Patke et al.   mAbs

The making of bispecific antibodies

(2017) Ulrich Brinkmann et al.   mAbs

Isolation of blood-brain barrier-crossing antibodies from a phage display library by competitive elution and their ability to penetrate the central nervous system

(2017) George Thom et al.   mAbs

Bispecific Antibodies and Antibody–Drug Conjugates (ADCs) Bridging HER2 and Prolactin Receptor Improve Efficacy of HER2 ADCs

(2017) Julian Andreev et al.   MOLECULAR CANCER THERAPEUTICS

Optimisation of the dibromomaleimide (DBM) platform for native antibody conjugation by accelerated post-conjugation hydrolysis

(2017) Maurício Morais et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

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

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

Pyridazinediones deliver potent, stable, targeted and efficacious antibody–drug conjugates (ADCs) with a controlled loading of 4 drugs per antibody

(2017) Eifion Robinson et al.   RSC Advances

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 antibody drug conjugates containing exatecan derivative-based cytotoxic payloads

(2016) Takashi Nakada et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Novel Bispecific Antibody Targeting EGFR and cMet Is Effective against EGFR Inhibitor–Resistant Lung Tumors

(2016) Sheri L. Moores et al.   CANCER RESEARCH

Enfortumab Vedotin Antibody-Drug Conjugate Targeting Nectin-4 Is a Highly Potent Therapeutic Agent in Multiple Preclinical Cancer Models

(2016) P. M. Challita-Eid et al.   CANCER RESEARCH

DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1

(2016) Y. Ogitani et al.   CLINICAL CANCER RESEARCH

Re-engineering therapeutic antibodies for Alzheimer’s disease as blood-brain barrier penetrating bi-specific antibodies

(2016) William M. Pardridge   EXPERT OPINION ON BIOLOGICAL THERAPY

Chemically Programmed Bispecific Antibodies in Diabody Format

(2016) Even Walseng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Recent advances in the construction of antibody–drug conjugates

(2016) Vijay Chudasama et al.   Nature Chemistry

Factor VIII–Mimetic Function of Humanized Bispecific Antibody in Hemophilia A

(2016) Midori Shima et al.   NEW ENGLAND JOURNAL OF MEDICINE

Processes for Constructing Homogeneous Antibody Drug Conjugates

(2016) David Y. Jackson   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Cell-type–restricted anti-cytokine therapy: TNF inhibition from one pathogenic source

(2016) Grigory A. Efimov et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Next-generation disulfide stapling: reduction and functional re-bridging all in one

(2016) Maximillian T. W. Lee et al.   Chemical Science

The use of 3,6-pyridazinediones in organic synthesis and chemical biology

(2016) Maximillian T. W. Lee et al.   JOURNAL OF CHEMICAL RESEARCH

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

(2016) Igor Dovgan et al.   Scientific Reports

Multiformat T-Cell-Engaging Bispecific Antibodies Targeting Human Breast Cancers

(2015) Yu Cao et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Exocyclic Olefinic Maleimides: Synthesis and Application for Stable and Thiol-Selective Bioconjugation

(2015) Dimpy Kalia et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A mild TCEP-based para-azidobenzyl cleavage strategy to transform reversible cysteine thiol labelling reagents into irreversible conjugates

(2015) Antoine Maruani et al.   CHEMICAL COMMUNICATIONS

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

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

A platform for efficient, thiol-stable conjugation to albumin's native single accessible cysteine

(2015) Mark E. B. Smith et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Sustained Brown Fat Stimulation and Insulin Sensitization by a Humanized Bispecific Antibody Agonist for Fibroblast Growth Factor Receptor 1/βKlotho Complex

(2015) Ganesh Kolumam et al.   EBioMedicine

Bridging Disulfides for Stable and Defined Antibody Drug Conjugates

(2014) George Badescu et al.   BIOCONJUGATE CHEMISTRY

Mild Method for Succinimide Hydrolysis on ADCs: Impact on ADC Potency, Stability, Exposure, and Efficacy

(2014) L. Nathan Tumey et al.   BIOCONJUGATE CHEMISTRY

Homogeneous Bispecifics by Disulfide Bridging

(2014) Elizabeth A. Hull et al.   BIOCONJUGATE CHEMISTRY

Selective Irreversible Chemical Tagging of Cysteine with 3-Arylpropiolonitriles

(2014) Oleksandr Koniev et al.   BIOCONJUGATE CHEMISTRY

Long-Term Stabilization of Maleimide–Thiol Conjugates

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

A Novel Glycoengineered Bispecific Antibody Format for Targeted Inhibition of Epidermal Growth Factor Receptor (EGFR) and Insulin-like Growth Factor Receptor Type I (IGF-1R) Demonstrating Unique Molecular Properties

(2014) Juergen M. Schanzer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2014) Robert P Lyon et al.   NATURE BIOTECHNOLOGY

Bispecific antibody generated with sortase and click chemistry has broad antiinfluenza virus activity

(2014) Koen Wagner et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Rapid, Stable, Chemoselective Labeling of Thiols with Julia-Kocieński-like Reagents: A Serum-Stable Alternative to Maleimide-Based Protein Conjugation

(2013) Narihiro Toda et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fab-PEG-Fab as a Potential Antibody Mimetic

(2013) Hanieh Khalili et al.   BIOCONJUGATE CHEMISTRY

A New Reagent for Stable Thiol-Specific Conjugation

(2013) George Badescu et al.   BIOCONJUGATE CHEMISTRY

Antibody–drug conjugates: current status and future directions

(2013) Heidi L. Perez et al.   DRUG DISCOVERY TODAY

Site-specific chemical modification of antibody fragments using traceless cleavable linkers

(2013) Gonçalo J L Bernardes et al.   Nature Protocols

Relative Amino Acid Composition Signatures of Organisms and Environments

(2013) Alexandra Moura et al.   PLoS One

Dual Targeting of EGFR and HER3 with MEHD7945A Overcomes Acquired Resistance to EGFR Inhibitors and Radiation

(2012) S. Huang et al.   CANCER RESEARCH

Synthesis of Bispecific Antibodies using Genetically Encoded Unnatural Amino Acids

(2012) Chan Hyuk Kim et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Self-Assembled Antibody Multimers through Peptide Nucleic Acid Conjugation

(2012) Stephanie A. Kazane et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Brentuximab vedotin

(2012) Niels W. C.J. van de Donk et al.   mAbs

Antitumor Activity of a Novel Bispecific Antibody That Targets the ErbB2/ErbB3 Oncogenic Unit and Inhibits Heregulin-Induced Activation of ErbB3

(2012) C. F. McDonagh et al.   MOLECULAR CANCER THERAPEUTICS

Conjugation site modulates the in vivo stability and therapeutic activity of antibody-drug conjugates

(2012) Ben-Quan Shen et al.   NATURE BIOTECHNOLOGY

A bispecific antibody to factors IXa and X restores factor VIII hemostatic activity in a hemophilia A model

(2012) Takehisa Kitazawa et al.   NATURE MEDICINE

Trastuzumab Emtansine for HER2-Positive Advanced Breast Cancer

(2012) Sunil Verma et al.   NEW ENGLAND JOURNAL OF MEDICINE

Reorienting the Fab Domains of Trastuzumab Results in Potent HER2 Activators

(2012) Justin M. Scheer et al.   PLoS One

Tunable Degradation of Maleimide–Thiol Adducts in Reducing Environments

(2011) Aaron D. Baldwin et al.   BIOCONJUGATE CHEMISTRY

Humanized Anti-Trop-2 IgG-SN-38 Conjugate for Effective Treatment of Diverse Epithelial Cancers: Preclinical Studies in Human Cancer Xenograft Models and Monkeys

(2011) T. M. Cardillo et al.   CLINICAL CANCER RESEARCH

Trastuzumab Emtansine: A Unique Antibody-Drug Conjugate in Development for Human Epidermal Growth Factor Receptor 2-Positive Cancer

(2011) P. M. LoRusso et al.   CLINICAL CANCER RESEARCH

Targeted Therapy With the T-Cell–Engaging Antibody Blinatumomab of Chemotherapy-Refractory Minimal Residual Disease in B-Lineage Acute Lymphoblastic Leukemia Patients Results in High Response Rate and Prolonged Leukemia-Free Survival

(2011) Max S. Topp et al.   JOURNAL OF CLINICAL ONCOLOGY

Site-Specific Incorporation ofp-Propargyloxyphenylalanine in a Cell-Free Environment for Direct Protein−Protein Click Conjugation

(2010) Bradley C. Bundy et al.   BIOCONJUGATE CHEMISTRY

Chemical generation of bispecific antibodies

(2010) V. R. Doppalapudi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

An efficient chemical approach to bispecific antibodies and antibodies of high valency

(2009) Julia I. Gavrilyuk et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Contribution of Linker Stability to the Activities of Anticancer Immunoconjugates

(2008) Stephen C. Alley et al.   BIOCONJUGATE CHEMISTRY

Antibody Conjugates of 7-Ethyl-10-hydroxycamptothecin (SN-38) for Targeted Cancer Chemotherapy

(2008) Sung-Ju Moon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Site-specific conjugation of a cytotoxic drug to an antibody improves the therapeutic index

(2008) Jagath R Junutula et al.   NATURE BIOTECHNOLOGY