A Comparative Analysis of Fibroblast Activation Protein-Targeted Small Molecule–Drug, Antibody–Drug, and Peptide–Drug Conjugates

IF 3.9 2区化学 Q1 BIOCHEMICAL RESEARCH METHODS

Bioconjugate Chemistry Pub Date : 2023-07-03 DOI:10.1021/acs.bioconjchem.3c00244

Aureliano Zana, Claudia Puig-Moreno, Matilde Bocci, Ettore Gilardoni, Cesare Di Nitto, Lucrezia Principi, Domenico Ravazza, Giulia Rotta, Eleonora Prodi, Roberto De Luca, Dario Neri* and Samuele Cazzamalli*,

引用次数: 0

Abstract

We present the first in vivo comparative evaluation of chemically defined antibody–drug conjugates (ADCs), small molecule–drug conjugates (SMDCs), and peptide–drug conjugates (PDCs) targeting and activated by fibroblast activation protein (FAP) in solid tumors. Both the SMDC (OncoFAP-Gly-Pro-MMAE) and the ADC (7NP2-Gly-Pro-MMAE) candidates delivered high amounts of active payload (i.e., MMAE) selectively at the tumor site, thus producing a potent antitumor activity in a preclinical cancer model.

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成纤维细胞活化蛋白靶向小分子药物、抗体药物和肽药物偶联物的比较分析

我们首次在实体肿瘤中对化学定义的抗体-药物偶联物(adc)、小分子-药物偶联物(SMDCs)和肽-药物偶联物(PDCs)进行了体内比较评价，这些偶联物靶向并被成纤维细胞激活蛋白(FAP)激活。SMDC (OncoFAP-Gly-Pro-MMAE)和ADC (7NP2-Gly-Pro-MMAE)候选药物在肿瘤部位选择性地提供大量活性有效载荷(即MMAE)，从而在临床前癌症模型中产生有效的抗肿瘤活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Bioconjugate Chemistry 生物-化学综合

CiteScore

9.00

自引率

2.10%

发文量

236

审稿时长

1.4 months

期刊介绍： Bioconjugate Chemistry invites original contributions on all research at the interface between man-made and biological materials. The mission of the journal is to communicate to advances in fields including therapeutic delivery, imaging, bionanotechnology, and synthetic biology. Bioconjugate Chemistry is intended to provide a forum for presentation of research relevant to all aspects of bioconjugates, including the preparation, properties and applications of biomolecular conjugates.