- Multivalent Siderophore–DOTAM Conjugates as Theranostics for Imaging and Treatment of Bacterial Infections
-
There is a strong need to better diagnose infections at deep body sites through noninvasive molecular imaging methods. Herein, we describe the synthesis and characterization of probes based on siderophore conjugates with catechol moieties and a central DO
- Ferreira, Kevin,Hu, Hai-Yu,Fetz, Verena,Prochnow, Hans,Rais, Bushra,Müller, Peter P.,Br?nstrup, Mark
-
-
Read Online
- Ligand taking indocyanine green derivative as carrier as well as preparation method and application of ligand
-
The invention discloses a ligand taking an indocyanine green derivative as a carrier as well as a preparation method and application of the ligand. When the ligand is chelated with paramagnetic metal ions, an NIR/MRI multi-mode contrast agent is obtained, when the ligand is chelated with radioactive metal ions, an NIR/PET multi-mode contrast agent is obtained, and the obtained contrast agents can be used for diagnosis of various tumors, especially liver cancer. Meanwhile, the contrast agents are good in water solubility and low in toxicity, mutual verification of multiple contrast modes is achieved, diagnosis information is enriched, diagnosis precision is improved, and a feasible novel contrast agent is provided for early diagnosis of tumors clinically.
- -
-
-
- NIR/PET bimodal contrast agent, and preparation method and application thereof
-
The invention discloses a near infrared and positron emission computed tomography (NIR)/positron emission tomography (PET) bimodal contrast agent, and a preparation method and application thereof. The NIR/PET bimodal contrast agent is obtained by taking an optimized indocyanine green derivative as a carrier and connecting a PET signal molecule. The contrast agent can be used for near-infrared imaging and has PET imaging capability; and meanwhile, the contrast agent is good in water solubility and low in toxicity, near-infrared and PET images verify each other, diagnosis information is enriched, and the contrast agent has the potential of becoming a novel tumor contrast agent.
- -
-
-
- NIR/MRI bimodal contrast agent, and preparation method and application thereof
-
The invention discloses a near infrared imaging and nuclear magnetic resonance imaging (NIR)/MRI bimodal contrast agent, and a preparation method and application thereof. The NIR/MRI bimodal contrast agent is obtained by taking an optimized indocyanine green derivative as a carrier and connecting an MRI signal molecule. The contrast agent can be used for near-infrared imaging and also has an MRI imaging capability; and meanwhile, water solubility is good, toxicity is low, near-infrared and MRI images verify each other, diagnosis information is enriched, and the contrast agent has the potential of becoming a novel tumor contrast agent.
- -
-
-
- Time-Resolved Terbium-Based Probe for the Detection of Zinc(II) Ions: Investigation of the Formation of a Luminescent Ternary Complex
-
Because of their unique photochemical and photophysical properties, luminescent lanthanide-based complexes have long captivated chemists. In recent years, the number of reports of luminescent lanthanide complex-based probes for monitoring of biological an
- Winnett, Matthew R.,Mini, Parvathy,Grace, Michael R.,Tuck, Kellie L.
-
supporting information
p. 118 - 127
(2019/09/30)
-
- Method for preparing DOTA derivative organic ligand which is a precursor DOTA-tris(tBu ester) of hypoxic tissue contrast agent DOTA-Ni with significant cost advantage in the preparation
-
The present invention relates to a method for preparing DOTA derivative organic ligand, which uses benzyl bromoacetate as one of the reactants in the synthesis process. Firstly, the starting materials 1,4,7,10-tetrazacyclododecane, sodium acetate and tert
- -
-
-
- 1,4,7,10-TETRAZACYCLODODECANE BASED AGENTS TO TARGET BACTERIA AND ITS USE
-
The present invention relates to new compounds comprising a siderophore moiety as well as a core structure able to chelate a metal ion. Optionally, the compounds may have additionally a moiety with a functional element including a marker molecule, a bioactive agent, an activity based probe suitable to monitor the aberrant expression or activity of proteins involved in the initiation and progression of bacterial infection, or a compound useful for bacterial inhibition. In a further aspect, the present invention provides a pharmaceutical composition containing said compound, for example, said pharmaceutical composition is an antibiotic. Additionally, the present invention relates to the use of said compounds in diagnostic methods, in particular, imaging methods including SPEC, PET or MRI. In an embodiment of the present invention, the compound is part of a theranostic composition having both, therapeutic as well as diagnostic activities.
- -
-
-
- DOTAM DERIVATIVES FOR THERAPEUTIC USE
-
The present invention relates to A compound of the formula I, in any of their stereoisomeric forms or a mixture of stereoisomeric forms in any ratio, and the pharmaceutically acceptable salts thereof, (I) wherein M is absent or present and a positively ch
- -
-
Page/Page column 50
(2015/06/08)
-
- Design, synthesis, and in vitro evaluation of a binary targeting MRI contrast agent for imaging tumor cells
-
A binary targeting vector that consists of peptide sequences of Arg-Gly-Asp (RGD) and Asn-Gly-Arg (NGR) motifs has been designed and synthesized using solid-phase peptide synthesis procedure. The vector is then coupled with Gd-DOTA to work as a targeting
- Yang, Yuping,Zhou, Jinlan,Yu, Kaichao
-
p. 449 - 457
(2014/03/21)
-
- CANCER IMAGING AND TREATMENT
-
A compound, or a pharmaceutically acceptable salt or ester thereof, comprises the structure: [in-line-formulae][(P1-S1j)p-L-(S2q-P2)r]t [/in-line-formulae] wherein: P1 and P2, which may be the same or
- -
-
-
- Conjugates of the B-subunit of shiga toxin for use as contrasting agents for imaging and therapy
-
Multivalent conjugates comprising the following formula: (STxB-linker A-S)x-GNS-(S-linker B-T)y wherein STxB is the B-subunit of Shiga toxin; linker A is a noncleavable linker; linker B is a cleavable linker used to release at least
- -
-
-
- CONJUGATES OF THE B-SUBUNIT OF SHIGA TOXIN FOR USE AS CONTRASTING AGENTS FOR IMAGING AND THERAPY
-
Multivalent conjugates comprising the following formula: (STxB-linker A-S)x-GNS-(S-linker B-T)y wherein STxB is the B-subunit of Shiga toxin; linker A is a noncleavable linker; linker B is a cleavable linker used to release at least
- -
-
-
- SELF-ASSEMBLING MOLECULES THAT ACCUMULATE IN ACIDIC TUMOR MICROENVIRONMENTS
-
Disclosed are compositions that contain a plurality of biocompatible self-assembling molecules that transform from isolated molecules or spherical micelles in the circulation into cylindrical nanofibers in the acidic extracellular environment of tumors wh
- -
-
-
- MRI CONTRAST AGENTS
-
The present invention relates to MRI based imaging. In particular, the present invention provides MRI contrast agents targeted to a HaloTag protein with tunable relaxation properties thereby providing optimal relaxivity for low field strength imaging and the other optimal relaxivity for high field strength imaging. Moreover, the MRI contrast agents are used to detect gene expression (of a gene of interest) in real time in vivo, to detect changes in gene expression (of a gene of interest) over time in, for example, an individual organism, to detect gene expression changes (of a gene of interest) in response to therapeutics, in cell labeling for MR imaging, in clinical diagnostics, and in theranostics.
- -
-
Paragraph 0114; 0115; 0116; 0117
(2013/11/19)
-
- Development of a dual functional luminescent sensor for zinc ion based on a peptidic architecture
-
A synthetic peptide bearing a lanthanide complex, TbOTZ exhibits a decrease of chromophore fluorescence and a concomitant luminescence enhancement due to sensitized Tb3+ upon Zn2+ binding. Thus, TbOTZ can be a valuable tool for ratiometric sensing of Zn2+ as well as for time-resolved fluorescence detection with a single molecule.
- Hirayama, Tasuku,Taki, Masayasu,Akaoka, Kazushi,Yamamoto, Yukio
-
p. 7410 - 7413
(2013/02/23)
-
- Reporter protein-targeted probes for magnetic resonance imaging
-
Contrast agents for magnetic resonance imaging are frequently employed as experimental and clinical probes. Drawbacks include low signal sensitivity, fast clearance, and nonspecificity that limit efficacy in experimental imaging. In order to create a bioresponsive MR contrast agent, a series of four Gd(III) complexes targeted to the HaloTag reporter were designed and synthesized. HaloTag is unique among reporter proteins for its specificity, versatility, and the covalent interaction between substrate and protein. In similar systems, these properties produce prolonged in vivo lifetimes and extended imaging opportunities for contrast agents, longer rotational correlation times, and increases in relaxivity (r1) upon binding to the HaloTag protein. In this work we report a new MR contrast probe, 2CHTGd, which forms a covalent bond with its target protein and results in a dramatic increase in sensitivity. A 6-fold increase in r1, from 3.8 to 22 mM-1s-1, is observed upon 2CHTGd binding to the target protein. This probe was designed for use with the HaloTag protein system which allows for a variety of substrates (specific for MRI, florescence, or protein purification applications) to be used with the same reporter.
- Strauch, Renee C.,Mastarone, Daniel J.,Sukerkar, Preeti A.,Song, Ying,Ipsaro, Jonathan J.,Meade, Thomas J.
-
supporting information; experimental part
p. 16346 - 16349
(2011/12/14)
-
- LDL-based nanoparticles for contrast enhanced MRI of atheroplaques in mouse models
-
A LDL particle functionalized with a GdDO3A-monoamide chelate with a long alkenyl anchor (GdDO3A-OA) was prepared for in vivo detection of atheroplaques. The GdDO3A-OA, when successfully intercalated into the lipid layer of LDL particles, led to a signifi
- Yamakoshi, Yoko,Qiao, Hui,Lowell, Andrew N.,Woods, Mark,Paulose, Betty,Nakao, Yuka,Zhang, Hualei,Liu, Ting,Lund-Katz, Sissel,Zhou, Rong
-
supporting information; experimental part
p. 8835 - 8837
(2011/09/21)
-
- Paramagnetic relaxation-based 19F MRI probe to detect protease activity
-
A novel design principle for 19F MRI probes detecting protease activity was developed. This principle is based on 19F MRI signal quenching by the intramolecular paramagnetic effect from Gd3+. The intramolecular Gd3+/
- Mizukami, Shin,Takikawa, Rika,Sugihara, Fuminori,Hori, Yuichiro,Tochio, Hidehito,Waelchli, Markus,Shirakawa, Masahiro,Kikuchi, Kazuya
-
p. 794 - 795
(2008/09/19)
-
- Improved syntheses and applicability of different DOTA building blocks for multiply derivatized scaffolds
-
DOTA (1,4,7,10-tetraazacyclodocecane-N,N′,N″,N?-tetraacetic acid), which forms extremely stable complexes with a large number of metal ions, is one of the most important and most commonly used chelators for in vivo applications such as cancer diagnosis an
- Waengler,Waengler,Eisenhut,Haberkorn,Mier
-
p. 2606 - 2616
(2008/12/22)
-
- CASCADE MACROMOLECULAR CONTRAST AGENTS FOR MEDICAL IMAGING
-
The present invention provides macromolecular contrast media for diagnostic imaging modalities.
- -
-
Page/Page column 22
(2010/11/28)
-
- A luminescent probe containing a tuftsin targeting vector coupled to a terbium complex
-
Orthogonal protection strategies have been used to prepare a series of luminescent and MRI active lanthanide complexes containing a tuftsin targeting vector that are internalised by macrophage cells. The Royal Society of Chemistry 2006.
- Aarons, Rebecca J.,Notta, Jatinder K.,Meloni, Marco M.,Feng, Jianghua,Vidyasagar, Rishma,Narvainen, Johanna,Allan, Stuart,Spencer, Neil,Kauppinen, Risto A.,Snaith, John S.,Faulkner, Stephen
-
p. 909 - 911
(2008/02/08)
-
- Pharmaceuticals for the imaging of angiogenic disorders
-
The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present
- -
-
-
- Synthesis and evaluation of a monoreactive DOTA derivative for indium-111-based residualizing label to estimate protein pharmacokinetics
-
The purpose of this study was to develop an indium-111 (111In)-based residualizing label for estimating the pharmacokinetics of proteins. 1,4,7,10-Tetraazacyclododecane-N,N′,N″,N?-tetraacetic acid (DOTA), which produced a highly stable and hydrophilic 111In chelate, was selected as the chelating site, and the monoreactive DOTA derivative with a tetrafluorophenyl group as the protein binding site (mDOTA) was designed to avoid cross-linkings of proteins. mDOTA was synthesized with an overall yield of 11%. The stability in murine plasma, the radioactivity retention in the catabolic sites of proteins and the radiochemical yields of 111In-labelled proteins via mDOTA were investigated using human serum albumin (HSA), galactosyl-neoglycoalbumin (NGA) and cytochrome c (cyt c) as model proteins. 111In-labelled HSA via mDOTA was highly stable for 5 days after incubation in murine plasma. Long retention of radioactivity in the catabolic sites was observed after injection of 111In-DOTA-NGA in mice, due to the slow elimination of the radiometabolite from the lysosome. At a chelator concentration of 42.2 μM, 111In-DOTA-cyt c was produced with over 91 % radiochemical yield. On the other hand, 111In-DOTA-lysine and 111In-DOTA were obtained with high radiochemical yields at lower chelator concentrations. These findings indicated that mDOTA would be an appropriate 111In-labelling agent for estimating protein pharmacokinetics. These findings also suggested that the introduction of a protein binding site at a position distal from the unmodified DOTA structure would be preferable to preparing 111In-DOTA-labelled proteins with higher specific activity.
- Mukai,Namba,Arano,Ono,Fujioka,Uehara,Ogawa,Konishi,Saji
-
p. 1073 - 1081
(2008/12/21)
-
- Simultaneous imaging of cardiac perfusion and a vitronectin receptor targeted imaging agent
-
The present invention describes a method of concurrent imaging in a mammal comprising: a) administering to said mammal a vitronectin receptor targeted imaging agent and a perfusion imaging agent; and b) concurrently detecting the vitronectin target imagin
- -
-
-
- Radiometal-labelled macrocyclic chelator-derivatised somatostatin analogue with superb tumour-targeting properties and potential for receptor-mediated internal radiotherapy
-
A monoreactive DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) prochelator (4,7,10-tricarboxymethyl-tert-butyl ester 1,4,7,10-tetraazacyclododecane-1-acetate) was synthesised which is useful in solid-phase and solution-phase peptide synthe
- Heppeler,Froidevaux,Maecke,Jermann,Behe,Powell,Hennig
-
p. 1974 - 1981
(2007/10/03)
-
- Cascade polymer complexes, process for their production and pharmaceutical agents containing said complexes
-
Cascade polymer complexes that contain a) complexing ligands of general formula I in which A stands for a nitrogen-containing cascade nucleus of base multiplicity a, X and Y, independently of one another, stand for a direct bond or a cascade reproduction
- -
-
-