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Pharmaceuticals
Special Issues
Radiolabelling for Tracking Drug Delivery System
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Radiolabelling for Tracking Drug Delivery System

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Radiopharmaceutical Sciences".

Deadline for manuscript submissions: closed (31 March 2023) | Viewed by 2250

Special Issue Editor

Dr. Yihsiu Chung

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Guest Editor
Department of Medical Research and Development, Linkou Chang Gung Memorial Hospital, Taoyuan, Taiwan
Interests: molecular imaging and image analysis; nanomedicine and drug delivery; translational oncological animal model; radiolabeling PET and SPECT

Special Issue Information

Dear Colleagues,

Drug delivery systems (nanoparticles) are a prosperous, exciting research field. The drugs or pharmaceuticals in a drug delivery system can enhance drug targeting and efficacy. Interestingly, tracking drug delivery systems by radiolabeling the radionuclides allows us to understand the pharmacokinetics of nanoparticle-based drugs in a living body. Herein, we would like to cover the radiolabeling chemistry, their PK/PD and efficacy in treatment in the successful development of drug delivery systems for PET or SPECT imaging. Furthermore, labeled drug delivery systems with alpha- or beta-emitted radionuclides as a promising synergistic treatment for cancer will be covered.

In summary, the Special Issue aims to highlight the tracking of drug delivery systems in PET and SPECT imaging and application.

Dr. Yihsiu Chung
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • drug delivery system
  • nanoparticles
  • radiolabeling
  • PET Imaging
  • SPECT Imaging
  • in vivo study
  • clinical study

Published Papers (1 paper)

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Research

9 pages, 1833 KiB  
Article
Characterization of Sigma-2 Receptor—Specific Binding Sites Using [3H]DTG and [125I]RHM-4
by Chi-Chang Weng, Aladdin Riad, Brian P. Lieberman, Kuiying Xu, Xin Peng, John L. Mikitsh and Robert H. Mach
Pharmaceuticals 2022, 15(12), 1564; https://doi.org/10.3390/ph15121564 - 15 Dec 2022
Cited by 2 | Viewed by 1941
Abstract
The sigma-2 receptor/transmembrane protein 97 (σ2R/TMRM97) is a promising biomarker of tumor proliferation and a target for cancer therapy. [3H]DTG has been used to evaluate σ2R/TMEM97 binding affinity in compound development studies. However, [3H]DTG has equal and moderate binding [...] Read more.
The sigma-2 receptor/transmembrane protein 97 (σ2R/TMRM97) is a promising biomarker of tumor proliferation and a target for cancer therapy. [3H]DTG has been used to evaluate σ2R/TMEM97 binding affinity in compound development studies. However, [3H]DTG has equal and moderate binding affinities to both sigma 1 receptor (σ1R) and σ2R/TMEM97. Furthermore, co-administration with the σ1R masking compound (+)-pentazocine may cause bias in σ2R/TMEM97 binding affinity screening experiments. We have developed a radioiodinated ligand, [125I]RHM-4, which has high affinity and selectivity for σ2R/TMEM97 versus σ1R. In this study, a head-to-head comparison between [3H]DTG and [125I]RHM-4 on the binding affinity and their effectiveness in σ2R/TMEM97 compound screening studies was performed. The goal of these studies was to determine if this radioiodinated ligand is a suitable replacement for [3H]DTG for screening new σ2R/TMEM97 compounds. Furthermore, to delineate the binding properties of [125I]RHM-4 to the σ2R/TMEM97, the structure of RHM-4 was split into two fragments. This resulted in the identification of two binding regions in the σ2R, the “DTG” binding site, which is responsible for binding to the σ2R/TMEM97, and the secondary binding site, which is responsible for high affinity and selectivity for the σ2R/TMEM97 versus the σ1R. The results of this study indicate that [125I]RHM-4 is an improved radioligand for in vitro binding studies of the σ2R/TMEM97 versus [3H]DTG. Full article
(This article belongs to the Special Issue Radiolabelling for Tracking Drug Delivery System)
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