PET and SPECT Molecular Imaging in Drug Development

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

Deadline for manuscript submissions: closed (10 November 2024) | Viewed by 1622

Special Issue Editor


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Guest Editor
Department of Molecular Medicine and Biopharmaceutical Sciences, Graduate School of Convergence Science and Technology, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 08826, Republic of Korea
Interests: PET pharmacokinetics; molecular imaging research
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Special Issue Information

Dear Colleagues,

Our forthcoming Special Issue of Pharmaceuticals, entitled “PET and SPECT Molecular Imaging in Drug Development”, will focus on the pivotal role of Positron Emission Tomography (PET) and SPECT (Single-photon emission computed tomography) in advancing drug development. Both, PET and SPECT imaging offer non-invasive insights into molecular processes, pharmacokinetics, and target engagement, enabling researchers to optimize drug candidates and predict clinical outcomes.

We are seeking contributions on topics such as novel tracers, preclinical and clinical applications, safety and efficacy assessments, quantitative data analysis, personalized medicine, and regulatory perspectives.

This Special Issue will serve as a platform for cutting-edge research, innovative methodologies, and case studies showcasing the impact of PET and SPECT imaging on drug development. We aim to create a bridge between academia and industry, fostering collaborations that translate PET- and SPECT-based discoveries into transformative therapies.

Dr. Hyun Soo Park
Guest Editor

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Published Papers (1 paper)

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Research

14 pages, 5448 KiB  
Article
Gallium-68-Labeled KISS1-54 Peptide for Mapping KISS1 Receptor via PET: Initial Evaluation in Human Tumor Cell Lines and in Tumor-Bearing Mice
by Ina Israel, Gabriele Riehl, Elke Butt, Andreas K. Buck and Samuel Samnick
Pharmaceuticals 2024, 17(1), 44; https://doi.org/10.3390/ph17010044 - 27 Dec 2023
Viewed by 1257
Abstract
Kisspeptins (KPs, KISS1) and their receptor (KISS1R) play a pivotal role as metastasis suppressor for many cancers. Low or lost KP expression is associated with higher tumor grade, increased metastatic potential, and poor prognosis. Therefore, KP expression has prognostic relevance and correlates with [...] Read more.
Kisspeptins (KPs, KISS1) and their receptor (KISS1R) play a pivotal role as metastasis suppressor for many cancers. Low or lost KP expression is associated with higher tumor grade, increased metastatic potential, and poor prognosis. Therefore, KP expression has prognostic relevance and correlates with invasiveness in cancers. Furthermore, KISS1R represents a very promising target for molecular imaging and therapy for KISS1R-expressing tumors. The goal of this study was to evaluate the developed KISS1-54 derivative, [68Ga]KISS1-54, as a PET-imaging probe for KISS1R-expressing tumors. The NODAGA-KISS1-54 peptide was labeled by Gallium-68, and the stability of the resulting [68Ga]KISS1-54 evaluated in injection solution and human serum, followed by an examination in different KISS1R-expressing tumor cell lines, including HepG2, HeLa, MDA-MB-231, MCF7, LNCap, SK-BR-3, and HCT116. Finally, [68Ga]KISS1-54 was tested in LNCap- and MDA-MB-231-bearing mice, using µ-PET, assessing its potential as an imaging probe for PET. [68Ga]KISS1-54 was obtained in a 77 ± 7% radiochemical yield and at a >99% purity. The [68Ga]KISS1-54 cell uptake amounted to 0.6–4.4% per 100,000 cells. Moreover, the accumulation of [68Ga]KISS1-54 was effectively inhibited by nonradioactive KISS1-54. In [68Ga]KISS1-54-PET, KISS1R-positive LNCap-tumors were clearly visualized as compared to MDA-MB-231-tumor implant with predominantly intracellular KISS1R expression. Our first results suggest that [68Ga]KISS1-54 is a promising candidate for a radiotracer for targeting KISS1R-expressing tumors via PET. Full article
(This article belongs to the Special Issue PET and SPECT Molecular Imaging in Drug Development)
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