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Stability of Maleimide-PEG and Mono-Sulfone-PEG Conjugation to a Novel Engineered Cysteine in the Human Hemoglobin Alpha Subunit

In order to use a Hemoglobin Based Oxygen Carrier as an oxygen therapeutic or blood substitute, it is necessary to increase the size of the hemoglobin molecule to prevent rapid renal clearance. A common method uses maleimide PEGylation of sulfhydryls created by the reaction of 2-iminothiolane at surface lysines. However, this creates highly heterogenous mixtures […]... Read more

Addressing the Challenges of Bioconjugate Medicines

The continuing advancements in bioconjugate medicines from delivery of potent cytotoxins to vaccine-, oligonucleotide-, radionuclide-, immunomodulator- and check-point inhibitor-conjugates, can start to address the large unmet medical need currently unattainable from current therapeutic approaches. As the field of bioconjugation develops, and the recent spate of antibody-drug conjugates (ADCs) approvals continues, the resulting knock-on effects for delivering a wider […]... Read more

Antibody-Drug Conjugates

This volume looks at key methodologies that are commonly used across antibody drug conjugates (ADCs) programs. The chapters in this book cover topics such as conjugations to endogenous cysteine residues; click chemistry conjugations; antibody conjugations via glycosyl remodeling; analysis of ADCs by native mass spectrometry; characterization of ADCs by capillary electrophoresis; LC/MS methods for studying […]... Read more

Integrating ADC Manufacturing for the Future

Antibody–drug conjugates (ADCs) in development target many indications beyond cancer and consist of a multitude of different types of components. Integrated development and manufacturing capabilities are essential to bringing these promising yet complex therapeutics to market.... Read more

Antibody Drug Conjugates of Cleavable Amino-alkyl and Aryl Maytansinoids

Natural products have been used for many medicinal purposes for centuries. Antibody drug conjugates (ADCs) have utilized this rich source of small molecule therapeutics to produce several clinically useful treatments. ADCs based on the natural product maytansine have been successful clinically. The authors further the utility of the anti-cancer natural product maytansine by developing efficacious payloads and linker-payloads for […]... Read more

Antibody drug conjugates of cleavable amino-alkyl and aryl maytansinoids

Natural products have been used for many medicinal purposes for centuries. Antibody drug conjugates (ADCs) have utilized this rich source of small molecule therapeutics to produce several clinically useful treatments. ADCs based on the natural product maytansine have been successful clinically. The authors further the utility of the anti-cancer natural product maytansine by developing efficacious […]... Read more

Design and Synthesis of Isoquinolidinobenzodiazepine Dimers, a Novel Class of Antibody–Drug Conjugate Payload

Antibody–drug conjugates (ADCs) represent an important class of emerging cancer therapeutics. Recent ADC development efforts highlighted the use of pyrrolobenzodiazepine (PBD) dimer payload for the treatment of several cancers. We identified the isoquinolidinobenzodiazepine (IQB) payload (D211), a new class of PBD dimer family of DNA damaging payloads. We have successfully synthesized all three IQB stereoisomers, […]... Read more

Design and Synthesis of Isoquinolidinobenzodiazepine Dimers, a Novel Class of Antibody-Drug Conjugate Payload

Antibody–drug conjugates (ADCs) represent an important class of emerging cancer therapeutics. Recent ADC development efforts highlighted the use of pyrrolobenzodiazepine (PBD) dimer payload for the treatment of several cancers. We identified the isoquinolidinobenzodiazepine (IQB) payload (D211), a new class of PBD dimer family of DNA damaging payloads. We have successfully synthesized all three IQB stereoisomers, […]... Read more

Modulation of drug-linker design to enhance in vivo potency of homogeneous antibody-drug conjugates

Antibody-drug conjugates (ADCs) are a promising class of anticancer agents which have undergone substantial development over the past decade and are now achieving clinical success. The development of novel site-specific conjugation technologies enables the systematic study of architectural features within the antibody conjugated drug linker that may affect overall therapeutic indices. Here we describe the […]... Read more

Stable and Homogeneous Drug Conjugation by Sequential Bis-Alkylation at Disulphide Bonds Using Bis-Sulphone Reagents

Antibody drug conjugates (ADCs) have begun to have a tremendous impact on the treatment of cancer and other pathological conditions. A current limitation in ADC development is that much effort and time is needed to fully optimise the combination of antibody, linker and drug. New linker strategies are required to ensure that more homogeneous and […]... Read more

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