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99mTc-labeled 19 amino acid containing peptide for use as phosphatidylethanolamine binding molecular probe and radiopharmaceutical

A technology of radiopharmaceuticals and amino acids, which can be used in radioactive carriers, in vivo radioactive preparations, peptide/protein components, etc., and can solve problems such as no treatment methods.

Active Publication Date: 2011-04-13
MCW RES FOUND INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although Tc-99 can be used in nuclear medicine imaging diagnostic methods, it is not used in any therapeutic methods

Method used

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  • 99mTc-labeled 19 amino acid containing peptide for use as phosphatidylethanolamine binding molecular probe and radiopharmaceutical
  • 99mTc-labeled 19 amino acid containing peptide for use as phosphatidylethanolamine binding molecular probe and radiopharmaceutical
  • 99mTc-labeled 19 amino acid containing peptide for use as phosphatidylethanolamine binding molecular probe and radiopharmaceutical

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Embodiment Construction

[0145] HPLC Method 1. At room temperature and a flow rate of 1.0ml / min, a Jupiter C 18 column( Aperture, 250×4.6 mm, Phenomenex). 90% buffer A (water with 0.1% trifluoroacetic acid, v / v) and 10% buffer B (acetonitrile with 0.1% trifluoroacetic acid, v / v) were run for 5 minutes for baseline, then for 35 minutes to 10 Linear gradient of % Buffer A and 90% Buffer B.

[0146] HPLC method 2. At room temperature and a flow rate of 1.0ml / min, Jupiter C 18 column( Aperture, 250×4.6mm). Baseline with 90% Buffer A (phosphate buffer, pH 6.7) and 10% Buffer B (acetonitrile) for 5 minutes, followed by a linear gradient to 10% Buffer A and 90% Buffer B over 30 minutes . Radioactivity levels in the HPLC eluate were monitored by gamma counting at an energy window of 140 ± 15 keV.

[0147] Radiolabeling of Duramycin. After HYNIC modification with 99m Tc labeled Duramycin. Specifically, HYNIC-coupled duramycin was synthesized by reacting succinimidyl 6-hydrazinonicotinic acid acet...

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Abstract

With only 19 amino acids, Duramycin is the smallest known polypeptide that has a defined 3-dimmensional binding structure. Duramycin binds Phosphatidylethanolamine (PtdE) at a 1:1 ratio with high affinity and exclusive specificity. As an abundant binding target, PtdE is a major phospholipid and accounts for about 20 % of the phospholipid content in mammalian cellular membranes. PtdE is externalized to the surface of apoptotic cells, and also becomes accessible in necrotic cells due to compromised plasma membrane integrity. Given the unique physicochemical properties of Duramycin and the availability of PtdE in acute cell death, the goal of this study is to develop and evaluate 99mTc-HYNIC-Duramycin as a novel molecular probe for imaging PtdE. 99mTc-HYNIC-Duramycin is a low-molecular weight, fast-clearing radiopharmaceutical that detects apoptosis / necrosis by binding to PtdE. The goal was to quantify the uptake of 99mTc-HYNIC-Duramycin in the area-at-risk after myocardial ischemia and reperfusion, and to determine the window of detection.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Patent Provisional Application No. 61 / 068,764, filed March 10,2008. [0003] Statement on Government Concerns [0004] none. Background of the invention [0005] Non-invasive imaging of acute cell death, including apoptosis and necrosis, has important implications in assessing degenerative disease and monitoring tumor therapy. To obtain better and earlier images, there must be a continuous effort to discover and develop uptake mechanisms and molecular probes that offer improved binding, pharmacokinetic and biodistribution properties. [0006] Technetium (technetium)-99m( 99m Tc) is a gamma-ray-emitting isotope used in radioisotope medical detection, eg, as a radiotracer detectable in vivo as a medical device. 99m Tc is well suited for this role as it readily emits detectable 140keV gamma rays. 99m The half-life of gamma rays emitted by Tc is 6.1 hours, which means that about 15...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/04
CPCA61K51/0474A61K51/088A61K38/04A61K38/10A61K38/03
Inventor M·赵
Owner MCW RES FOUND INC
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