Synthesis of specific SPECT-radiopharmaceutical for tumor imaging based on methionine: 99mTc-DTPA-bis(methionine)

Bioconjugate Chemistry
Puja Panwar HazariAnil K Mishra

Abstract

Methionine-diethylenetriaminepentaaceticacid-methionine [DTPA-bis(Met)] was synthesized by covalently conjugating two molecules of methionine (Met) to DTPA and was labeled with (99m)Tc in high radiochemical purity and specific activity (166-296 MBq/micromol). Kinetic analysis showed K(m) of 12.95 +/- 3.8 nM and a maximal transport rate velocity (V(max)) of 80.35 +/- 0.42 pmol microg protein(-1) min(-1) of (99m)Tc-DTPA-bis(Met) in U-87MG cells. DTPA-bis(Met) had dissociation constants (K(d)) of 0.067 and 0.077 nM in U-87MG and BMG, respectively. (35)S-methionine efflux was trans-stimulated by (99m)Tc-labeled DTPA conjugate demonstrating concentrative transport. The blood kinetic studies showed fast clearance with t(1/2) (F) = 36 +/- 0.5 min and t(1/2) (S) = 5 h 55 min +/- 0.85 min. U-87MG and BMG tumors saturated at approximately 2000 +/- 280 nmol/kg of (99m)Tc-DTPA-bis(Met). Initial rate of transport of (99m)Tc-DTPA-bis(Met) in U-87MG tumor was found to be 4.68 x 10(-4) micromol/kg/min. The tumor (BMG cell line, malignant glioma) grafted in athymic mice were readily identifiable in the gamma images. Semiquantitative analysis from region of interest (ROI) placed over areas counting average counts per pixel with maximum radiotrac...Continue Reading

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Citations

May 4, 2012·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Didel M MahoungaYueqing Gu
Oct 23, 2014·Therapeutic Delivery·Shubhra Chaturvedi, Anil Kumar Mishra
Apr 20, 2016·Cancer Biotherapy & Radiopharmaceuticals·Raghuvir H GaonkarMita C Debnath
Feb 27, 2017·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Caroline Mari Ramos OdaElaine Amaral Leite
Oct 16, 2015·Nuclear Medicine and Biology·Xiaotian XiaXiaoli Lan
Apr 23, 2013·Chemical Biology & Drug Design·Pooja SinghAnil K Mishra
Nov 20, 2020·Journal of Pharmaceutical Sciences·Anshul GuptaGaurav K Jain
Jun 14, 2018·Molecular Pharmaceutics·Chen WeiHaiyan Chen

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