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Incorporation of Fluorine into an OBOC Peptide Library by Copper-Free Click Chemistry toward the Discovery of PET Imaging Agents.

Abstract：

:A one-bead one-compound (OBOC) library of peptide-based imaging agents was developed where a 19F-containing moiety was added onto the N-terminus of octamer peptides through copper-free click chemistry prior to screening of the library. This created a library of complete imaging agents that was screened against CXCR4, a receptor of interest for cancer imaging. The screen directly resulted in the discovery of a peptide-based imaging agent with an IC50 of 138 μM. This proof-of-concept study describes a new type of OBOC peptide library design, where hits discovered from screening can be easily translated into their fluorine-18 counterpart for PET imaging without loss of affinity.

journal_name

ACS Comb Sci

journal_title

ACS combinatorial science

authors

Murrell E,Luyt LG

doi

10.1021/acscombsci.9b00146

subject

Has Abstract

pub_date

2020-03-09 00:00:00

pages

109-113

issue

3

eissn

2156-8952

issn

2156-8944

journal_volume

22

pub_type

杂志文章

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