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

当前位置： X-MOL 学术 › ACS Comb. Sci. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Incorporation of Fluorine into an OBOC Peptide Library by Copper-Free Click Chemistry toward the Discovery of PET Imaging Agents.
ACS Combinatorial Science Pub Date : 2020-02-03 , DOI: 10.1021/acscombsci.9b00146
Emily Murrell ₁ , Leonard G Luyt _{1,

2,

3}

Affiliation

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.

中文翻译：

通过无铜点击化学将氟掺入OBOC肽库中，以发现PET成像剂。

开发了一种基于肽的成像剂的单珠单化合物（OBOC）库，其中在筛选该库之前，通过无铜点击化学将含19F的基团添加到八聚体肽的N端。这创建了一个完整的成像剂库，该库针对CXCR4（针对癌症成像的目标受体）进行了筛选。该筛选直接导致发现基于肽的显像剂，IC50为138μM。这项概念验证研究描述了一种新型的OBOC肽文库设计，在此设计中，从筛选中发现的命中可以轻松翻译成对应的18氟对应物，用于PET成像而不会失去亲和力。

更新日期：2020-02-06

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11