Department of Chemistry, University of Western Ontario, 1151 Richmond Street, London, Ontario N6A 5B7, Canada.
Departments of Oncology and Medical Imaging, University of Western Ontario, 1151 Richmond Street, London, Ontario N6A 5B7, Canada.
ACS Comb Sci. 2020 Mar 9;22(3):109-113. doi: 10.1021/acscombsci.9b00146. Epub 2020 Feb 6.
A one-bead one-compound (OBOC) library of peptide-based imaging agents was developed where a F-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 IC 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.
开发了一种基于肽的单珠单化合物 (OBOC) 成像剂文库，在筛选文库之前，通过无铜点击化学将含氟部分添加到八聚肽的 N 端。这创建了一个完整的成像剂文库，针对 CXCR4 进行筛选，CXCR4 是癌症成像的感兴趣受体。该筛选直接发现了一种具有 IC 为 138 μM 的基于肽的成像剂。这项概念验证研究描述了一种新型的 OBOC 肽文库设计，其中筛选发现的命中物可以很容易地转化为其氟-18 对应物，用于 PET 成像，而不会损失亲和力。
