دورية أكاديمية
أعرض في EDS

(99m)Tc-amitrole as a novel selective imaging probe for solid tumor: In silico and preclinical pharmacological study.

التفاصيل البيبلوغرافية
العنوان: (99m)Tc-amitrole as a novel selective imaging probe for solid tumor: In silico and preclinical pharmacological study.
المؤلفون: Essa BM; Radioactive Isotopes and Generator Department, Hot Laboratories Center, Atomic Energy Authority (EAEA), P.O. Box 13759, Cairo, Egypt., Sakr TM; Radioactive Isotopes and Generator Department, Hot Laboratories Center, Atomic Energy Authority (EAEA), P.O. Box 13759, Cairo, Egypt. Electronic address: Tamer_sakr78@yahoo.com., Khedr MA; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ein Helwan, Cairo 11795, Egypt., El-Essawy FA; Faculty of Science, Department of Chemistry, Menoufia University, Shebin El-Koam, Egypt., El-Mohty AA; Radioactive Isotopes and Generator Department, Hot Laboratories Center, Atomic Energy Authority (EAEA), P.O. Box 13759, Cairo, Egypt.
المصدر: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2015 Aug 30; Vol. 76, pp. 102-9. Date of Electronic Publication: 2015 May 05.
نوع المنشور: Journal Article; Validation Study
اللغة: English
بيانات الدورية: Publisher: Elsevier Science B.V Country of Publication: Netherlands NLM ID: 9317982 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1879-0720 (Electronic) Linking ISSN: 09280987 NLM ISO Abbreviation: Eur J Pharm Sci Subsets: MEDLINE
أسماء مطبوعة: Publication: Amsterdam : Elsevier Science B.V
Original Publication: Amsterdam ; New York : Elsevier, c1993-
مواضيع طبية MeSH: Computer-Aided Design* , Drug Design*, Amitrole/*pharmacokinetics , Antineoplastic Agents/*pharmacokinetics , Carcinoma, Ehrlich Tumor/*diagnostic imaging , Enzyme Inhibitors/*pharmacokinetics , Lactoperoxidase/*antagonists & inhibitors , Radiopharmaceuticals/*pharmacokinetics , Technetium/*pharmacokinetics, Amitrole/administration & dosage ; Amitrole/chemistry ; Animals ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/chemistry ; Carcinoma, Ehrlich Tumor/drug therapy ; Carcinoma, Ehrlich Tumor/enzymology ; Drug Stability ; Enzyme Inhibitors/administration & dosage ; Enzyme Inhibitors/chemistry ; Female ; Hydrogen-Ion Concentration ; Lactoperoxidase/metabolism ; Mice ; Molecular Docking Simulation ; Molecular Structure ; Radionuclide Imaging ; Radiopharmaceuticals/administration & dosage ; Radiopharmaceuticals/chemistry ; Structure-Activity Relationship ; Technetium/administration & dosage ; Technetium/chemistry ; Tissue Distribution
مستخلص: Lactoperoxidase (LPO) inhibitors are very selective for solid tumor due to their high binding affinity to the LPO enzyme. A computational study was used to select top-ranked LPO inhibitor (alone and in complex with (99m)Tc) with high in silico affinity. The novel prepared (99m)Tc-amitrole complex demonstrated both in silico and in vivo high affinity toward solid tumors.(99m)Tc-amitrole was radio-synthesized with a high radiochemical yield (89.7±3.25). It showed in vitro stability for up to 6h. Its preclinical evaluation in solid tumor-bearing mice showed high retention and biological accumulation in solid tumor cells with a high Target/Non-Target (T/NT) ratio equal to 4.9 at 60min post-injection. The data described previously could recommend (99m)Tc-amitrole as potential targeting scintigraphic probe for solid tumor imaging.
(Copyright © 2015 Elsevier B.V. All rights reserved.)
فهرسة مساهمة: Keywords: Amitrole; Hypoxia; Imaging; In silico; Lactoperoxidase enzyme; Technetium-99m; Tumor
المشرفين على المادة: 0 (Antineoplastic Agents)
0 (Enzyme Inhibitors)
0 (Radiopharmaceuticals)
7440-26-8 (Technetium)
EC 1.11.1.- (Lactoperoxidase)
ZF80H5GXUF (Amitrole)
تواريخ الأحداث: Date Created: 20150510 Date Completed: 20160308 Latest Revision: 20191210
رمز التحديث: 20240829
DOI: 10.1016/j.ejps.2015.05.002
PMID: 25956074
قاعدة البيانات: MEDLINE
الوصف
تدمد:1879-0720
DOI:10.1016/j.ejps.2015.05.002