In this section
@article{Aboagye:2023:10.3390/pharmaceutics15071915,
author = {Aboagye, E and Teh, JH and Amgheib, A and Fu, R and Barnes, C and Abrahams, J and Ashek, A and Wang, N and Yang, Z and Mansoorudeen, M and Long, NJ and Aboagye, E},
doi = {10.3390/pharmaceutics15071915},
journal = {Pharmaceutics},
pages = {1--13},
title = {Evaluation of [18F]AlF-EMP-105 for molecular imaging of 2 C-Met},
url = {http://dx.doi.org/10.3390/pharmaceutics15071915},
volume = {15},
year = {2023}
}
TY - JOUR
AB - C-Met is a receptor tyrosine kinase that is overexpressed in a range of different cancer types, and has been identified as a potential biomarker for cancer imaging and therapy. Previously, a 68Ga-labelled peptide, [68Ga]Ga-EMP-100, has shown promise for imaging c-Met in renal cell carcinoma in humans. Herein, we report the synthesis and preliminary biological evaluation of an [18F]AlF-labelled analogue, [18F]AlF-EMP-105, for c-Met imaging by positron emission tomography. EMP-105 was radiolabelled using the aluminium-[18F]fluoride method with 46 ± 2% RCY and >95% RCP in 35–40 min. In vitro evaluation showed that [18F]AlF-EMP-105 has a high specificity for c-Met-expressing cells. Radioactive metabolite analysis at 5 and 30 min post-injection revealed that [18F]AlF-EMP-105 has good blood stability, but undergoes transformation—transchelation, defluorination or demetallation—in the liver and kidneys. PET imaging in non-tumour-bearing mice showed high radioactive accumulation in the kidneys, bladder and urine, demonstrating that the tracer is cleared predominantly as [18F]fluoride by the renal system. With its high specificity for c-Met expressing cells, [18F]AlF-EMP-105 shows promise as a potential diagnostic tool for imaging cancer.
AU - Aboagye,E
AU - Teh,JH
AU - Amgheib,A
AU - Fu,R
AU - Barnes,C
AU - Abrahams,J
AU - Ashek,A
AU - Wang,N
AU - Yang,Z
AU - Mansoorudeen,M
AU - Long,NJ
AU - Aboagye,E
DO - 10.3390/pharmaceutics15071915
EP - 13
PY - 2023///
SN - 1999-4923
SP - 1
TI - Evaluation of [18F]AlF-EMP-105 for molecular imaging of 2 C-Met
T2 - Pharmaceutics
UR - http://dx.doi.org/10.3390/pharmaceutics15071915
UR - https://www.mdpi.com/1999-4923/15/7/1915
UR - http://hdl.handle.net/10044/1/105352
VL - 15
ER -
Professor Nick Long
Email: n.long@imperial.ac.uk
Telephone: +44 (0)20 7594 5781
501J
Molecular Sciences Research Hub
White City Campus
