NDLI: Trastuzumab Labeled to High Specific Activity with $^{111}$In by Conjugation to G4 PAMAM Dendrimers Derivatized with Multiple DTPA Chelators Exhibits Increased Cytotoxic Potency on HER2-Positive Breast Cancer Cells

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Trastuzumab Labeled to High Specific Activity with $^{111}$In by Conjugation to G4 PAMAM Dendrimers Derivatized with Multiple DTPA Chelators Exhibits Increased Cytotoxic Potency on HER2-Positive Breast Cancer Cells

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Trastuzumab Labeled to High Specific Activity with $^{111}$In by Conjugation to G4 PAMAM Dendrimers Derivatized with Multiple DTPA Chelators Exhibits Increased Cytotoxic Potency on HER2-Positive Breast Cancer Cells

Content Provider	Springer Nature Link
Author	Chan, Conrad Cai, Zhongli Reilly, Raymond M.
Copyright Year	2013
Abstract	To conjugate trastuzumab with/without NLS peptides to G4 PAMAM dendrimers derivatized with DTPA and determine the specific radioactivity (SA) for $^{111}$In labeling, HER2 immunoreactivity and cytotoxicity on breast cancer (BC) cells.G4 dendrimers were reacted with DTPA then conjugated through a thiol to maleimide-derivatized trastuzumab. The SA achievable was determined by incubating 2 to 20 μg with 60 MBq of $^{111}$In. HER2 immunoreactivity, internalization and nuclear importation were measured. The effect of $^{111}$In-DTPA-G4-trastuzumab (5.9 MBq/μg) on the clonogenic survival (CS) of SK-Br-3 or MDA-MB-231 cells with high or low HER2 density, respectively was compared to $^{111}$In-DTPA-NLS-trastuzumab (0.5 MBq/μg). DNA double-strand breaks (DSBs) were measured.DTPA-G4-trastuzumab was labeled with $^{111}$In to a SA (23.6 MBq/μg) which was 100-fold higher than $^{111}$In-DTPA-NLS-trastuzumab. $^{111}$In-DTPA-G4-trastuzumab and $^{111}$In-DTPA-G4-NLS-trastuzumab retained HER2 immunoreactivity and were internalized and imported into the nucleus of BC cells. G4-radioimmunoconjugates were 2–4 fold and 9-fold more cytotoxic to SK-Br-3 and MDA-MB-231 cells, respectively than $^{111}$In-DTPA-NLS-trastuzumab which was associated with an increase in DNA DSBs.Conjugation of trastuzumab to G4 PAMAM dendrimers modified with 30 DTPA permitted high SA $^{111}$In labeling which increased their cytotoxic potency for BC cells with high or low HER2 density.
Starting Page	1999
Ending Page	2009
Page Count	11
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	30
Issue Number	8
e-ISSN	1573904X
Language	English
Publisher	Springer US
Publisher Date	2013-04-25
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Breast cancer HER2 Indium-111 PAMAM dendrimers Trastuzumab Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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Trastuzumab Labeled to High Specific Activity with $^{111}$In by Conjugation to G4 PAMAM Dendrimers Derivatized with Multiple DTPA Chelators Exhibits Increased Cytotoxic Potency on HER2-Positive Breast Cancer Cells