Site-specific antibody–drug conjugates: the nexus of bioorthogonal chemistry, protein engineering, and drug development

P Agarwal, CR Bertozzi - Bioconjugate chemistry, 2015 - ACS Publications
Antibody–drug conjugates (ADCs) combine the specificity of antibodies with the potency of
small molecules to create targeted drugs. Despite the simplicity of this concept, generation of …

Stepping forward in antibody-drug conjugate development

Y Jin, MA Schladetsch, X Huang, MJ Balunas… - Pharmacology & …, 2022 - Elsevier
Antibody-drug conjugates (ADCs) are cancer therapeutic agents comprised of an antibody,
a linker and a small-molecule payload. ADCs use the specificity of the antibody to target the …

Site-specific antibody drug conjugates for cancer therapy

S Panowski, S Bhakta, H Raab, P Polakis, JR Junutula - MAbs, 2014 - Taylor & Francis
Antibody therapeutics have revolutionized the treatment of cancer over the past two
decades. Antibodies that specifically bind tumor surface antigens can be effective …

Antibody drug conjugates: design and selection of linker, payload and conjugation chemistry

JR McCombs, SC Owen - The AAPS journal, 2015 - Springer
Antibody drug conjugates (ADCs) have emerged as an important pharmaceutical class of
drugs designed to harness the specificity of antibodies with the potency of small molecule …

Synthesis of site-specific antibody-drug conjugates using unnatural amino acids

JY Axup, KM Bajjuri, M Ritland… - Proceedings of the …, 2012 - National Acad Sciences
Antibody-drug conjugates (ADCs) allow selective targeting of cytotoxic drugs to cancer cells
presenting tumor-associated surface markers, thereby minimizing systemic toxicity …

ARX788, a site-specific anti-HER2 antibody–drug conjugate, demonstrates potent and selective activity in HER2-low and T-DM1–resistant breast and gastric cancers

L Skidmore, S Sakamuri, NA Knudsen, AG Hewet… - Molecular cancer …, 2020 - AACR
First-generation antibody–drug conjugates (ADC) are heterogeneous mixtures that have
shown clinical benefit, but generally exhibited safety issues and a narrow therapeutic …

Transglutaminase-based chemo-enzymatic conjugation approach yields homogeneous antibody–drug conjugates

P Dennler, A Chiotellis, E Fischer… - Bioconjugate …, 2014 - ACS Publications
Most chemical techniques used to produce antibody–drug conjugates (ADCs) result in a
heterogeneous mixture of species with variable drug-to-antibody ratios (DAR) which will …

Marine-Sourced Anti-Cancer and Cancer Pain Control Agents in Clinical and Late Preclinical Development

DJ Newman, GM Cragg - Marine drugs, 2014 - mdpi.com
The marine habitat has produced a significant number of very potent marine-derived agents
that have the potential to inhibit the growth of human tumor cells in vitro and, in a number of …

Drugs and drug candidates from marine sources: An assessment of the current “state of play”

DJ Newman, GM Cragg - Planta medica, 2016 - thieme-connect.com
The potential of the marine environment to produce candidate compounds (structures) as
leads to, or even direct drugs from, has been actively discussed for the last 50 or so years …

Aldehyde tag coupled with HIPS chemistry enables the production of ADCs conjugated site-specifically to different antibody regions with distinct in vivo efficacy and …

PM Drake, AE Albers, J Baker, S Banas… - Bioconjugate …, 2014 - ACS Publications
It is becoming increasingly clear that site-specific conjugation offers significant advantages
over conventional conjugation chemistries used to make antibody–drug conjugates (ADCs) …