# Imaging of Chemokine Receptors

> **NIH NIH P41** · WASHINGTON UNIVERSITY · 2022 · $261,097

## Abstract

TR&D 2 Project Summary
Via their cognate receptors, chemokines orchestrate the migration and activation of various classes of immune
cells and, thus, play a central role in the pathogenesis of cellular inflammation that underlies a host of common
diseases such as atherosclerosis, Alzheimer's disease, various forms of inflammatory lung disease and
numerous cancers. As a consequence, there is intense interest in clarifying the roles of various chemokines
and their receptors in human diseases and in the development of novel therapeutics and imaging approaches
directed at this system. Currently, it is unclear whether broad spectrum or individually targeted therapeutics
should be employed. Consequently, it is also uncertain whether imaging a panel of key chemokine receptors
or targeting a specific receptor would be most useful as a diagnostic agent to determine disease activity,
progression or assess drug treatment efficiency. However, what is clear is that the chemokine receptor imaging
agents are underdeveloped. Given the constant evolution in human disease pathogenesis, it is critical the
imaging methods that are developed are widely applicable in humans.
Building upon our expertise in synthesizing various chemokine receptor targeted PET radiotracers for vascular
injury, atherosclerosis and cancer applications, our objective is to first translate a broad spectrum chemokine
receptor imaging agent using viral inflammatory macrophage protein-II (vMIP-II) to determine the overall
expression of chemokine receptors in head and neck cancer patients and then focus a chemokine CC receptor
2 (CCR2) targeted PET radiotracer using a peptide ECL1 inverso (ECL1i). Information from these studies will
guide further radiotracer optimization and assess potential for human imaing. To achieve this objective, we will
pursue the following Specific Aims:
Aim 1. Translate the broad spectrum chemokine receptor PET radiotracer [64Cu]DOTA-vMIP-II for human
imaging. We have developed a [64Cu]DOTA-vMIP-II peptide-based radiotracer to detect numerous chemokine
receptors and have demonstrated its potential in multiple animal disease models and ex-vivo human tissue. In
Aim 1A, we will optimize our radiotracer cell binding assay to screen potentially alternative radiotracer candidates
and in parallel, evaluate radiotracer performance by one of our Collaborative Projects (CPs) in a non-human
primate model of disease. If successful, we will then perform the necessary tasks to obtain approval for an
Exploratory Investigational New Drug Application from the US Food and Drug Administration (Aim 1B). In Aim
1C we will perform a first-in-man evaluation of [64Cu]DOTA-vMIP-II in head and neck cancer patients to: 1) Assess
its safety, biodistribution and radiation dosimetry and; 2) To evaluate its ability to detect chemokine receptor
expression.
Aim 2. Translate the CCR2 targeted radiotracer [64Cu]DOTA-ECL1i for human imaging. We have prepared
a [64Cu]DOTA-ECL1i peptide tracer for specific ...

## Key facts

- **NIH application ID:** 10480878
- **Project number:** 5P41EB025815-05
- **Recipient organization:** WASHINGTON UNIVERSITY
- **Principal Investigator:** Yongjian Liu
- **Activity code:** P41 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $261,097
- **Award type:** 5
- **Project period:** 2018-09-01 → 2023-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10480878

## Citation

> US National Institutes of Health, RePORTER application 10480878, Imaging of Chemokine Receptors (5P41EB025815-05). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10480878. Licensed CC0.

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