Exner Rüdiger M, Paisey Stephen J, Redman James E, Pascu Sofia I
Department of Chemistry, University of Bath, Claverton Down, Bath BA2 7AY, United Kingdom.
Wales Research & Diagnostic Positron Emission Tomography Imaging Centre (PETIC), School of Medicine, Cardiff University, University Hospital of Wales, Heath Park, Cardiff CF14 4XN, United Kingdom.
ACS Omega. 2021 Oct 19;6(43):28455-28462. doi: 10.1021/acsomega.1c03994. eCollection 2021 Nov 2.
Peptide nucleic acids (PNAs, nucleic acid analogues with a peptide backbone rather than a phosphoribosyl backbone) have emerged as promising chemical agents in antigene or antisense therapeutics, as splicing modulators or in gene editing. Their main benefits, compared to DNA or RNA agents, are their biochemical stability and the lack of negative charges throughout the backbone, leading to negligible electrostatic interaction with the strand with which they are hybridizing. As a result, hybridization of PNA strands with DNA or RNA strands leads to higher binding energies and melting temperatures. A lack of natural transporters, however, necessitates the formation of PNA-containing chimeras or the formulation of nanoparticular cell delivery methods. Here, we set out to explore the progress made in using imaging agents based on PNAs in diagnostic applications and highlight selected developments and challenges.
肽核酸（PNA，一种具有肽主链而非磷酸核糖主链的核酸类似物）已成为反基因或反义治疗、剪接调节剂或基因编辑领域中颇具前景的化学试剂。与DNA或RNA试剂相比，它们的主要优势在于生化稳定性以及整个主链缺乏负电荷，这使得它们与杂交链的静电相互作用可忽略不计。因此，PNA链与DNA或RNA链的杂交会产生更高的结合能和熔解温度。然而，由于缺乏天然转运体，需要形成含PNA的嵌合体或采用纳米颗粒细胞递送方法。在此，我们着手探索基于PNA的成像剂在诊断应用方面取得的进展，并重点介绍一些选定的进展和挑战。
