@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}
}

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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  - 

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