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Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging.

ABSTRACT: Over the last 20 years, intensive investigation and multiple clinical successes targeting protein kinases, mostly for cancer treatment, have identified small molecule kinase inhibitors as a prominent therapeutic class. In the course of those investigations, radiolabeled kinase inhibitors for positron emission tomography (PET) imaging have been synthesized and evaluated as diagnostic imaging probes for cancer characterization. Given that inhibitor coverage of the kinome is continuously expanding, in vivo PET imaging will likely find increasing applications for therapy monitoring and receptor density studies both in- and outside of oncological conditions. Early investigated radiolabeled inhibitors, which are mostly based on clinically approved tyrosine kinase inhibitor (TKI) isotopologues, have now entered clinical trials. Novel radioligands for cancer and PET neuroimaging originating from novel but relevant target kinases are currently being explored in preclinical studies. This article reviews the literature involving radiotracer design, radiochemistry approaches, biological tracer evaluation and nuclear imaging results of radiolabeled kinase inhibitors for PET reported between 2010 and mid-2015. Aspects regarding the usefulness of pursuing selective vs. promiscuous inhibitor scaffolds and the inherent challenges associated with intracellular enzyme imaging will be discussed.

SUBMITTER: Bernard-Gauthier V

PROVIDER: S-EPMC6332294 | biostudies-literature | 2015 Dec

REPOSITORIES: biostudies-literature

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Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging.

Bernard-Gauthier Vadim V Bailey Justin J JJ Berke Sheldon S Schirrmacher Ralf R

Molecules (Basel, Switzerland) 20151209 12

Over the last 20 years, intensive investigation and multiple clinical successes targeting protein kinases, mostly for cancer treatment, have identified small molecule kinase inhibitors as a prominent therapeutic class. In the course of those investigations, radiolabeled kinase inhibitors for positron emission tomography (PET) imaging have been synthesized and evaluated as diagnostic imaging probes for cancer characterization. Given that inhibitor coverage of the kinome is continuously expanding, ...[more]

PMID: 26690113

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Project description:PurposePrinting technology, capable of producing three-dimensional (3D) objects, has evolved in recent years and provides potential for developing reproducible and sophisticated physical phantoms. 3D printing technology can help rapidly develop relatively low cost phantoms with appropriate complexities, which are useful in imaging or dosimetry measurements. The need for more realistic phantoms is emerging since imaging systems are now capable of acquiring multimodal and multiparametric data. This review addresses three main questions about the 3D printers currently in use, and their produced materials. The first question investigates whether the resolution of 3D printers is sufficient for existing imaging technologies. The second question explores if the materials of 3D-printed phantoms can produce realistic images representing various tissues and organs as taken by different imaging modalities such as computer tomography (CT), positron emission tomography (PET), single-photon emission computed tomography (SPECT), magnetic resonance imaging (MRI), ultrasound (US), and mammography. The emergence of multimodal imaging increases the need for phantoms that can be scanned using different imaging modalities. The third question probes the feasibility and easiness of "printing" radioactive or nonradioactive solutions during the printing process.MethodsA systematic review of medical imaging studies published after January 2013 is performed using strict inclusion criteria. The databases used were Scopus and Web of Knowledge with specific search terms. In total, 139 papers were identified; however, only 50 were classified as relevant for this paper. In this review, following an appropriate introduction and literature research strategy, all 50 articles are presented in detail. A summary of tables and example figures of the most recent advances in 3D printing for the purposes of phantoms across different imaging modalities are provided.ResultsAll 50 studies printed and scanned phantoms in either CT, PET, SPECT, mammography, MRI, and US-or a combination of those modalities. According to the literature, different parameters were evaluated depending on the imaging modality used. Almost all papers evaluated more than two parameters, with the most common being Hounsfield units, density, attenuation and speed of sound.ConclusionsThe development of this field is rapidly evolving and becoming more refined. There is potential to reach the ultimate goal of using 3D phantoms to get feedback on imaging scanners and reconstruction algorithms more regularly. Although the development of imaging phantoms is evident, there are still some limitations to address: One of which is printing accuracy, due to the printer properties. Another limitation is the materials available to print: There are not enough materials to mimic all the tissue properties. For example, one material can mimic one property-such as the density of real tissue-but not any other property, like speed of sound or attenuation.

Dataset Information

Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging.

Publications

Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging.

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