Antibody-drug conjugates: recent advances in conjugation and linker chemistries

K Tsuchikama, Z An - Protein & cell, 2018 - academic.oup.com
… Boosted by the successes of FDA-approved Adcetris ® and Kadcyla ® , this drug class has
been rapidly growing along with about 60 ADCs currently in clinical trials. In this article, we …

[HTML][HTML] Rapid conjugation of antibodies to toxins to select candidates for the development of anticancer Antibody-Drug Conjugates (ADCs)

RM Hoffmann, S Mele, A Cheung… - Scientific reports, 2020 - nature.com
… the rapid conjugation and generation of antibody-drug combinations to facilitate early antibody
… of promising antibody-drug pairs for future ADC development. This methodology relies on …

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

BQ Shen, K Xu, L Liu, H Raab, S Bhakta… - Nature …, 2012 - nature.com
… To demonstrate that the Fc region per se was not responsible for the rapid drug loss
observed with the Fc-S396C conjugate, we selected two other accessible Fc region …

A rapid approach for characterization of thiol-conjugated antibodydrug conjugates and calculation of drugantibody ratio by liquid chromatography mass …

D Firth, L Bell, M Squires, S Estdale, C McKee - Analytical biochemistry, 2015 - Elsevier
… demonstration of a rapid “middle-up… conjugated maleimidocaproyl-monomethyl auristatin
F (mcMMAF) and valine-citrulline-monomethyl auristatin E (vcMMAE) antibodydrug conjugates

Ethynylphosphonamidates for the Rapid and Cysteine‐Selective Generation of Efficacious AntibodyDrug Conjugates

MA Kasper, A Stengl, P Ochtrop… - Angewandte Chemie …, 2019 - Wiley Online Library
conjugation method to reduce the number of drug equivalents needed for sufficient conjugation
Since Adcetris is modified with an average of four vedotin molecules per antibody, 28 we …

A rapid on-line method for mass spectrometric confirmation of a cysteine-conjugated antibody-drug-conjugate structure using multidimensional chromatography

RE Birdsall, H Shion, FW Kotch, A Xu, TJ Porter… - MAbs, 2015 - Taylor & Francis
… Cysteine-conjugated antibody-drug conjugates (ADCs) are manufactured using controlled
partial reduction and conjugation chemistry with drug payloads that typically occur in intervals …

Strategies and challenges for the next generation of antibodydrug conjugates

A Beck, L Goetsch, C Dumontet… - Nature reviews Drug …, 2017 - nature.com
… The highly solvent-accessible site rapidly lost conjugated thiol-reactive linkers in plasma
owing to maleimide exchange with reactive thiol groups in albumin, free cysteine or glutathione …

Rapid and Efficient Generation of Stable AntibodyDrug Conjugates via an Encoded Cyclopropene and an Inverse‐Electron‐Demand Diels–Alder Reaction

B Oller‐Salvia, G Kym, JW Chin - … Chemie International Edition, 2018 - Wiley Online Library
… the rapid production of stable therapeutic protein conjugates. … and rapid conjugation of
diverse therapeutic antibodies with … coupled to its rapid and quantitative conjugation to generate …

[HTML][HTML] Site-selective modification strategies in antibodydrug conjugates

SJ Walsh, JD Bargh, FM Dannheim… - Chemical Society …, 2021 - pubs.rsc.org
… It was hypothesised that pAMF would enable more rapid SPAAC conjugation compared to
pAzF, due to the azido group being further from the electron withdrawing phenyl ring, hence …

Antibodydrug conjugate sacituzumab govitecan drives efficient tissue penetration and rapid intracellular drug release

A Kopp, S Hofsess, TM Cardillo, SV Govindan… - Molecular cancer …, 2023 - AACR
Antibodydrug conjugates (ADC) are a rapidly growing class of targeted cancer treatments,
… We found that rapid release of the SN-38 payload from the hydrolysable linker inside cells …