Next Article in Journal
Efficient Synthesis of β-Aryl-γ-lactams and Their Resolution with (S)-Naproxen: Preparation of (R)- and (S)-Baclofen
Next Article in Special Issue
Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives
Previous Article in Journal
Identification of Hydrophobic Interfaces in Protein-Ligand Complexes by Selective Saturation Transfer NMR Spectroscopy
Previous Article in Special Issue
The Guareschi Pyridine Scaffold as a Valuable Platform for the Identification of Selective PI3K Inhibitors
Article Menu

Export Article

Open AccessReview
Molecules 2015, 20(12), 22000-22027; doi:10.3390/molecules201219816

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

Division of Oncological Imaging, Department of Oncology, University of Alberta, 11560 University Ave., Edmonton, AB T6G 1Z2, Canada
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: James W. Leahy
Received: 22 October 2015 / Revised: 18 November 2015 / Accepted: 1 December 2015 / Published: 9 December 2015
(This article belongs to the Special Issue Kinase Inhibitor Chemistry)
View Full-Text   |   Download PDF [7839 KB, uploaded 9 December 2015]   |  

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. View Full-Text
Keywords: positron emission tomography; tyrosine kinase inhibitors; protein kinases; nuclear imaging; cancer imaging; neuroimaging; fluorine-18; carbon-11 positron emission tomography; tyrosine kinase inhibitors; protein kinases; nuclear imaging; cancer imaging; neuroimaging; fluorine-18; carbon-11
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Bernard-Gauthier, V.; Bailey, J.J.; Berke, S.; Schirrmacher, R. Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging. Molecules 2015, 20, 22000-22027.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top