A New 4-Nitrobenzyl Carbonate Prodrug of Methyl 5-Benzyl-2-hydroxy-11-methylene-6-oxo-5H-benzo [b]carbazole-1-carboxylate for Potential Use with Nitroreductase-Based Gene-Directed Enzyme Prodrug Therapy (GDEPT).

ChemInform ◽  
2006 ◽  
Vol 37 (28) ◽  
Author(s):  
C. Asche ◽  
U. Kucklaender
Keyword(s):  
Enzyme Prodrug Therapy ◽  
Potential Use

scholarly journals Cell-Penetrating Peptides as a Tool for the Cellular Uptake of a Genetically Modified Nitroreductase for use in Directed Enzyme Prodrug Therapy

2019 ◽  
Vol 10 (4) ◽  
pp. 45 ◽  
Author(s):  
Anderson ◽  
Hobbs ◽  
Gwenin ◽  
Ball ◽  
Bennie ◽  
...  
Keyword(s):  
Magnetic Nanoparticle ◽  
Genetically Modified ◽  
Cell Penetrating Peptides ◽  
Target Cells ◽  
Tumour Site ◽  
Enzyme Prodrug Therapy ◽  
Delivery Vector ◽  
Cell Penetrating ◽  
Subsequent Activation ◽  
Potential Use

Directed enzyme prodrug therapy (DEPT) involves the delivery of a prodrug-activating enzyme to a solid tumour site, followed by the subsequent activation of an administered prodrug. One of the most studied enzyme–prodrug combinations is the nitroreductase from Escherichia coli (NfnB) with the prodrug CB1954 [5-(aziridin-1-yl)-2,4-dinitro-benzamide]. One of the major issues faced by DEPT is the ability to successfully internalize the enzyme into the target cells. NfnB has previously been genetically modified to contain cysteine residues (NfnB-Cys) which bind to gold nanoparticles for a novel DEPT therapy called magnetic nanoparticle directed enzyme prodrug therapy (MNDEPT). One cellular internalisation method is the use of cell-penetrating peptides (CPPs), which aid cellular internalization of cargo. Here the cell-penetrating peptides: HR9 and Pep-1 were tested for their ability to conjugate with NfnB-Cys. The conjugates were further tested for their potential use in MNDEPT, as well as conjugating with the delivery vector intended for use in MNDEPT and tested for the vectors capability to penetrate into cells.

Nitrobenzylcarbamate Prodrugs of Cytotoxic Acridines for Potential Use with Nitroreductase Gene Directed Enzyme Prodrug Therapy.

ChemInform ◽  
2006 ◽  
Vol 37 (29) ◽  
Author(s):  
Christian Asche ◽  
Pascal Dumy ◽  
Daniele Carrez ◽  
Alain Croisy ◽  
Martine Demeunynck
Keyword(s):  
Enzyme Prodrug Therapy ◽  
Potential Use

Novel Inhibitors of Carboxypeptidase G2(CPG2):  Potential Use in Antibody-Directed Enzyme Prodrug Therapy

1999 ◽  
Vol 42 (6) ◽  
pp. 951-956 ◽  
Author(s):  
Tariq H. Khan ◽  
Ebun A. Eno-Amooquaye ◽  
Frances Searle ◽  
Pat J. Browne ◽  
Helen M. I. Osborn ◽  
...  
Keyword(s):  
Enzyme Prodrug Therapy ◽  
Carboxypeptidase G2 ◽  
Potential Use

Nitrobenzylcarbamate prodrugs of cytotoxic acridines for potential use with nitroreductase gene-directed enzyme prodrug therapy

2006 ◽  
Vol 16 (7) ◽  
pp. 1990-1994 ◽  
Author(s):  
Christian Asche ◽  
Pascal Dumy ◽  
Danièle Carrez ◽  
Alain Croisy ◽  
Martine Demeunynck
Keyword(s):  
Enzyme Prodrug Therapy ◽  
Potential Use

scholarly journals The YfkO Nitroreductase from Bacillus Licheniformis on Gold-Coated Superparamagnetic Nanoparticles: Towards a Novel Directed Enzyme Prodrug Therapy Approach

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 517
Author(s):  
Patrick Ball ◽  
Robert Hobbs ◽  
Simon Anderson ◽  
Emma Thompson ◽  
Vanessa Gwenin ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Bacillus Licheniformis ◽  
Maximum Dosage ◽  
Superparamagnetic Nanoparticles ◽  
Enzyme Prodrug Therapy ◽  
Hydroxylamine Derivative ◽  
Therapy Approach ◽  
Potential Use

The bacterial nitroreductase NfnB has been the focus of a great deal of research for its use in directed enzyme prodrug therapy in combination with the nitroreductase prodrug CB1954 with this combination of enzyme and prodrug even entering clinical trials. Despite some promising results, there are major limitations to this research, such as the fact that the lowest reported Km for this enzyme far exceeds the maximum dosage of CB1954. Due to these limitations, new enzymes are now being investigated for their potential use in directed enzyme prodrug therapy. One such enzyme that has proved promising is the YfkO nitroreductase from Bacillus Licheniformis. Upon investigation, the YfkO nitroreductase was shown to have a much lower Km (below the maximum dosage) than that of NfnB as well as the fact that when reacting with the prodrug it produces a much more favourable ratio of enzymatic products than NfnB, forming more of the desired 4-hydroxylamine derivative of CB1954.

The growth of mica polytypes as studied by conventional and high-resolution TEM

1983 ◽  
Vol 41 ◽  
pp. 174-177
Author(s):  
A. Baronnet ◽  
M. Amouric
Keyword(s):  
Water Pressure ◽  
Point Of View ◽  
Temperature Fields ◽  
Natural Occurrence ◽  
Growth Mechanisms ◽  
Long Period ◽  
High Resolution Tem ◽  
Layer Stacking ◽  
Experimental Works ◽  
Potential Use

The origin of mica polytypes has long been a challenging problem for crystal- lographers, mineralogists and petrologists. From the petrological point of view, interest in this field arose from the potential use of layer stacking data to furnish further informations about equilibrium and/or kinetic conditions prevailing during the crystallization of the widespread mica-bearing rocks. From the compilation of previous experimental works dealing with the occurrence domains of the various mica "polymorphs" (1Mr, 1M, 2M1, 2M2 and 3T) within water-pressure vs temperature fields, it became clear that most of these modifications should be considered as metastable for a fixed mica species. Furthermore, the natural occurrence of long-period (or complex) polytypes could not be accounted for by phase considerations. This highlighted the need of a more detailed kinetic approach of the problem and, in particular, of the role growth mechanisms of basal faces could play in this crystallographic phenomenon.

An atomic-resolution microscope study of Al contracts on GaAs

1986 ◽  
Vol 44 ◽  
pp. 726-727
Author(s):  
Z. Liliental-Weber ◽  
C. Nelson ◽  
R. Ludeke ◽  
R. Gronsky ◽  
J. Washburn
Keyword(s):  
High Speed ◽  
Schottky Contacts ◽  
Detailed Knowledge ◽  
The Past ◽  
Semiconductor Interfaces ◽  
Deposited Metal ◽  
Microwave Applications ◽  
Free Interfaces ◽  
Potential Use

The properties of metal/semiconductor interfaces have received considerable attention over the past few years, and the Al/GaAs system is of special interest because of its potential use in high-speed logic integrated optics, and microwave applications. For such materials a detailed knowledge of the geometric and electronic structure of the interface is fundamental to an understanding of the electrical properties of the contact. It is well known that the properties of Schottky contacts are established within a few atomic layers of the deposited metal. Therefore surface contamination can play a significant role. A method for fabricating contamination-free interfaces is absolutely necessary for reproducible properties, and molecularbeam epitaxy (MBE) offers such advantages for in-situ metal deposition under UHV conditions

The potential use of short chain peptides in parenteral nutrition

1985 ◽  
Vol 4 ◽  
pp. 116-123 ◽  
Author(s):  
P STEHLE ◽  
S ALBERS ◽  
I AMBERGER ◽  
P PFAENDER ◽  
P FURST
Keyword(s):  
Parenteral Nutrition ◽  
Short Chain ◽  
Potential Use
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