Impact of dipeptide on ADC physicochemical properties and efficacy identifies Ala–Ala as the optimal dipeptide-Reference-Cited by-同舟云学术

Impact of dipeptide on ADC physicochemical properties and efficacy identifies Ala–Ala as the optimal dipeptide

Published:2024 Issue:1 Volume:15 Page:355-365
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Wang Lu¹^ORCID,Hobson Adrian D.¹^ORCID,Fitzgibbons Julia¹^ORCID,Hernandez Axel¹,Jia Ying¹,Xu Zhou²,Wang Zhongyuan²,Yu Yajie²,Li Xiang²

Affiliation:

1. AbbVie Bioresearch Center, 381 Plantation Street, Worcester, Massachusetts 01605, USA

2. WuXi AppTec, 168 Nanhai Road, Tianjin Economic-Technological Development Area TEDA, TJS 300457, China

Abstract

A glucocorticoid receptor modulator (GRM) was conjugated to a mouse anti-TNF antibody using various dipeptide linkers. Impact of dipeptide linkers on ADC physical properties, including solubility, hydrophobicity, and aggregation were evaluated.

Funder

AbbVie

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2024/MD/D3MD00473B

Reference30 articles.

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5. Cathepsin B-Labile Dipeptide Linkers for Lysosomal Release of Doxorubicin from Internalizing Immunoconjugates: Model Studies of Enzymatic Drug Release and Antigen-Specific In Vitro Anticancer Activity

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1. Anti-TNF Thioester Glucocorticoid Antibody–Drug Conjugate Fully Inhibits Inflammation with Minimal Effect on Systemic Corticosterone Levels in a Mouse Arthritis Model;Journal of Medicinal Chemistry;2024-05-23

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