Evaluation of the pharmacokinetic effects of various linking group using the 111In-DOTA-X-BBN(7-14)NH2 structural paradigm in a prostate cancer model.

Bioconjugate Chemistry
Jered C GarrisonTimothy J Hoffman

Abstract

The high incidence of BB2 receptor (BB2r) expression in various cancers has prompted investigators to pursue the development of BB2r-targeted agents for diagnostic imaging, chemotherapy, and radiotherapy. Development of BB2r-targeted agents, based on the bombesin (BBN) peptide, has largely involved the use of the bifunctional chelate approach in which the linking group serves several key roles including pharmacokinetic modification. Understanding the in vivo properties of the various pharmacokinetic modifying linking groups is crucial for developing BB2r-targeted agents with improved targeting and clearance characteristics. The goal of this study was to systematically evaluate the pharmacokinetic profile of aliphatic hydrocarbon, aromatic, and poly(ethylene glycol) (ether) functional groups in order to obtain a better understanding of the in vivo properties of these pharmacokinetic modifiers. Specifically, we synthesized six radioconjugates with the structure 111In-DOTA- X-BBN(7-14)NH2, where X = 8-aminooctanoic acid (8-AOC), 5-amino-3-oxapentyl-succinamic acid (5-ADS), 8-amino-3,6-dioxaoctyl-succinamic acid (8-AOS), p-aminobenzoic acid (AMBA), Gly-AMBA, and Gly- p-aminomethylbenzoic acid (Gly-AM2BA). All of the (nat)In-conjuga...Continue Reading

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Citations

Mar 6, 2012·European Journal of Nuclear Medicine and Molecular Imaging·Melpomeni Fani, Helmut R Maecke
Jun 30, 2011·Cancer Biotherapy & Radiopharmaceuticals·Seyed Pezhman ShirmardiMojtaba Shamsaei
Oct 2, 2012·PloS One·Hanwen ZhangHelmut R Maecke
Mar 23, 2011·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Haixun GuoYubin Miao
Mar 8, 2014·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Ajay ShrivastavaMichael F Tweedle
Jun 11, 2011·Journal of Biomedicine & Biotechnology·Chung-Li HoChih-Hsien Chang
Mar 13, 2012·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·P B PujattiE B de Araújo
Aug 3, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Anna Lucia TorneselloFranco Maria Buonaguro
Jan 1, 2020·Anti-cancer Agents in Medicinal Chemistry·Arezou M FarahaniNourollah Sadeghzadeh
Feb 4, 2021·Journal of Medicinal Chemistry·Rajendra P BandariCharles J Smith
Dec 31, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Nurmaya EffendiKazuma Ogawa
Dec 3, 2014·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Haixun Guo, Yubin Miao
Oct 12, 2019·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Wenting ZhangJered C Garrison
Jul 31, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Zhengyuan ZhouJered C Garrison
Jun 16, 2009·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Zhaofei LiuXiaoyuan Chen
Nov 8, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Yang LiuZhen Cheng
Sep 4, 2010·Bioconjugate Chemistry·Joeri KuilFijs W B van Leeuwen
Nov 1, 2018·Chemical Reviews·Thomas I Kostelnik, Chris Orvig
Oct 11, 2011·Nuclear Medicine and Biology·Simone DäppRoger Schibli

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