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

被引：11

作者：

Zana, Aureliano ^{[1
]}

Puig-Moreno, Claudia ^{[1
,2
]}

Bocci, Matilde ^{[1
]}

Gilardoni, Ettore ^{[1
]}

Di Nitto, Cesare ^{[1
]}

Principi, Lucrezia ^{[1
]}

Ravazza, Domenico ^{[1
]}

Rotta, Giulia ^{[1
]}

Prodi, Eleonora ^{[1
]}

De Luca, Roberto ^{[1
]}

Neri, Dario ^{[1
,2
,3
]}

Cazzamalli, Samuele ^{[1
]}

机构：

[1] R&D Dept, Philochem AG, CH-8112 Zurich, Switzerland

[2] Swiss Fed Inst Technol, Dept Chem & Appl Biosci, CH-8093 Zurich, Switzerland

[3] Philogen SpA, I-53100 Siena, Italy

来源：

BIOCONJUGATE CHEMISTRY | 2023年 / 34卷 / 07期

关键词：

Compendex;

D O I：

10.1021/acs.bioconjchem.3c00244

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Wepresent the first in vivo comparative evaluationof chemically defined antibody-drug conjugates (ADCs), smallmolecule-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 potentantitumor activity in a preclinical cancer model.

引用

页码：1205 / 1211

页数：7

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