John A. Flygare

Design of Novel Exatecan-Amide Linker-Payloads for the Development of Stable, Low-Aggregating, and Highly Efficacious Antibody-Drug Conjugates

Ryan V. Quiroz, Simon B. Lang, Rebecca Johnson, Nancy Zepeda et autres

. These linker-payloads are promising new leads for the treatment of cancer and represent a generalizable, modular, and advantageous linker platform.

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Discovery of Novel N -Linked Camptothecin Linker-Payloads to Access Antibody–Drug Conjugates with High Target-Mediated In Vivo Efficacy

Vlad Bacauanu, Si-Jie Chen, Simon B. Lang, Christian L. Morales et autres

-aminobenzyl carbamate (PABC) linkers with a focus on stability and polarity leads to the discovery of promising α-amino-isobutyramido-exatecan constructs. The corresponding high-DAR ADCs showed low aggregation, good in vitro potency, and robust target-mediated efficacy in vivo across two antibody-antigen pairs. These results …

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Discovery of potent dihydro-oxazinoquinolinone inhibitors of GuaB for the treatment of tuberculosis

Yuebiao Zhou, Ignacio Aliagas, Shumei Wang, Chun Sing Li et autres

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Discovery and Evaluation of TLR-Targeted Immune Agonists

Natalia Chernyak, Bhagyashree Bhagwat, Saraswathi Naravula, Ying Chen et autres

Toll-like receptor (TLR) activation converts immunologically inactive tumors into immunologically active tumors by activating tumor residing antigen-presenting cells and recruitment of cytotoxic T lymphocytes. Targeted immune agonists (TIAs) are antibody drug conjugates with small-molecule TLR agonist payloads. The mechanism of action of …

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Design and Optimization of Selectivity-Tunable Toll-like Receptor 7/8 Agonists as Novel Antibody–Drug Conjugate Payloads

Akash M. Patel, Aarron T. Willingham, Alan C. Cheng, Daniela M. Tomazela et autres

Toll-like receptors 7 and 8 are involved in modulating the adaptive and innate immune responses, and their activation has shown promise as a therapeutic strategy in the field of immuno-oncology. While systemic exposure to TLR7/8 agonists can result in poor tolerance, combination …

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Impact of the first Hypersomnia Research Center in a public health service of Rio de Janeiro, Brazil - a participatory medicine model

Christianne Martins Corrêa da Silva Bahia, V. Mendes de Oliveira, Daniele Angst Secco, Romulo Vianna et autres

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In vivo bioluminescence imaging of labile iron in xenograft models and liver using FeAL-1, an iron-activatable form of D-luciferin

Ryan L. Gonciarz, Honglin Jiang, Linh Tram, Cedric L. Hugelshofer et autres

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

Thomas H. Pillow, Melissa M. Schutten, Shang‐Fan Yu, Rachana V. Ohri et autres

Supplementary Figures S1-S5, Supplementary Materials and Methods

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

Thomas H. Pillow, Melissa M. Schutten, Shang‐Fan Yu, Rachana V. Ohri et autres

Supplementary Figures S1-S5, Supplementary Materials and Methods

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

Thomas H. Pillow, Melissa M. Schutten, Shang‐Fan Yu, Rachana V. Ohri et autres

Abstract A novel disulfide linker was designed to enable a direct connection between cytotoxic pyrrolobenzodiazepine (PBD) drugs and the cysteine on a targeting antibody for use in antibody–drug conjugates (ADCs). ADCs composed of a cysteine-engineered antibody were armed with a PBD using …

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

Thomas H. Pillow, Melissa M. Schutten, Shang‐Fan Yu, Rachana V. Ohri et autres

Abstract A novel disulfide linker was designed to enable a direct connection between cytotoxic pyrrolobenzodiazepine (PBD) drugs and the cysteine on a targeting antibody for use in antibody–drug conjugates (ADCs). ADCs composed of a cysteine-engineered antibody were armed with a PBD using …

Supplementary 4 from A Novel Anti-CD22 Anthracycline-Based Antibody–Drug Conjugate (ADC) That Overcomes Resistance to Auristatin-Based ADCs

Shang‐Fan Yu, Bing Zheng, MaryAnn Go, Jeffrey Lau et autres

Supplementary 4. P-gp overexpressing BJAB.Luc cell line showed the similar resistance to anti-CD22-vc-MMAE