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  • DRUG  (6)
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  • 1
    Keywords: CELLS ; Germany ; THERAPY ; imaging ; SYSTEM ; TOOL ; GENOME ; DRUG ; MOLECULES ; DNA ; INTERVENTION ; molecular imaging ; RECOGNITION ; ACID ; PEPTIDE NUCLEIC-ACIDS ; TARGET ; REQUIRES ; DERIVATIVES ; DELIVERY ; STABILITY ; diagnostics ; sensitivity ; specificity ; FUTURE ; GENE DELIVERY ; CHEMISTRY ; OLIGONUCLEOTIDE ; development ; SUBSTRATE ; PERSPECTIVES ; DRUGS ; ANALOGS ; THYMINE ; antisense ; CLICK CHEMISTRY ; INTERVENTIONS ; LIGATION ; MODALITY ; Nucleic acids ; Click-Chemistry ; CELLULAR DELIVERY ; Diels Alder Reaction(invers) (DAR(inv)) ; Peptide Nucleic Acid (PNA) ; PNA building block functionalization
    Abstract: Progress in genome research led to new perspectives in diagnostic applications and to new promising therapies. On account of their specificity and sensitivity, nucleic acids (DNA/RNA) increasingly are in the focus of the scientific interest. While nucleic acids were a target of therapeutic interventions up to now, they could serve as excellent tools in the future, being highly sequence-specific in molecular diagnostics. Examples for imaging modalities are the representation of metabolic processes (Molecular Imaging) and customized therapeutic approaches ("Targeted Therapy"). In the individualized medicine nucleic acids could play a key role; this requires new properties of the nucleic acids, such as stability. Due to evolutionary reasons natural nucleic acids are substrates for nucleases and therefore suitable only to a limited extent as a drug. To use DNA as an excellent drug, modifications are required leading e.g. to a peptide nucleic acid (PNA). Here we show that an easy substitution of nucleobases by functional molecules with different reactivity like the Reppe anhydride and pentenoic acid derivatives is feasible. These derivatives allow an independent multi-ligation of functionalized compounds, e.g. pharmacologically active ones together with imaging components, leading to local concentrations sufficient for therapy and diagnostics at the same time. The high chemical stability and ease of synthesis could enhance nucleic chemistry applications and qualify PNA as a favourite for delivery. This system is not restricted to medicament material, but appropriate for the development of new and highly efficient drugs for a sustainable pharmacy
    Type of Publication: Journal article published
    PubMed ID: 20617125
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  • 2
    Keywords: BIOLOGY ; CHEMISTRY ; molecular biology ; DRUG ; USA
    Type of Publication: Meeting abstract published
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  • 3
    Keywords: PEPTIDE ; CELL ; Germany ; IN-VIVO ; DISEASE ; DISEASES ; GENE ; GENE-EXPRESSION ; PROTEIN ; transcription ; DRUG ; MOLECULES ; CONTRAST ; treatment ; DISCOVERY ; TRANSPORT ; MEMBRANE ; MODULATION ; NUCLEUS ; PEPTIDES ; TRANSFORMATION ; HUMAN-PAPILLOMAVIRUS ; MALIGNANT TRANSFORMATION ; C-MYC ; CHRONIC MYELOGENOUS LEUKEMIA ; CHRONIC MYELOID-LEUKEMIA ; DRUG-RESISTANCE ; ANTISENSE OLIGONUCLEOTIDES ; drug design,drug delivery,membrane transport,NLS,cancer treatment,radiation,peptide synthesis,solid- ; HUMAN PROSTATE-CANCER ; NEUTRON-CAPTURE THERAPY ; nuclear envelope ; NUCLEAR-ENVELOPE
    Abstract: The unique functions of biomolecules, including transport accross biological membranes (e.g. the cell membrane, the nuclear envelope), modulation of protein function, gene transcription, reconstitution of the malignant transformation, and viral, bacterial and fungal activities underlie a high pharmaceutical potential. The development of combinatorial functional peptide modules in this important area has been slow, in contrast to the rapid development in the synthesis of small biopolymers. The conjugation of a short transmembrane transport peptide module with a cell nucleus address peptide module and with any substance is attractive for preparation of BioShuttle-based peptides because of the well-established automated synthesis of peptides. Variation of the different functional modules for drug targeting and the choice of substances can be combined to create novel bioconjugates with unique properties. This article provides an overview of previous work on the BioShuttle technology and outlines the promising use of this approach in combinatorial peptide synthesis and drug discovery. Copyright (C) 2003 John Wiley Sons, Ltd
    Type of Publication: Journal article published
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  • 4
    Keywords: PEPTIDE ; CELLS ; tumor ; TUMOR-CELLS ; AGENTS ; Germany ; SYSTEM ; TOOL ; SITE ; DRUG ; TISSUE ; ACTIVATION ; SEQUENCE ; treatment ; CLEAVAGE ; TRANSPORT ; TUMOR PROGRESSION ; DELIVERY ; specificity ; LIVING CELLS ; TUMOR CELLS ; PRECURSORS ; CATHEPSIN-B ; RE ; GLIOMA ; GLIOMA-CELLS ; DRUG-DELIVERY ; TUMOR-CELL ; drug targeting ; glioblastoma multiforme ; TOOLS ; cathepsin B ; intracellular targeting ; METHYL-ESTER ; solid phase peptide synthesis ; SPPS ; transmembrane transport
    Abstract: Goal in pharmaceutical research is achievement of necessary drug concentrations in the target organ, effective treatment with safe delivery of genetic agents, while sparing normal tissue and minimizing side effects. A new "BioShuttle"-delivery system harbouring a cathepsin B cutting site, a nuclear address sequence and a functional Peptide was developed and tumor cells were treated. Transport and subcellular activation were determined by confocal laser scanning microscopy permitting the conclusion: BioShuttle-conjugates prove as efficient tools for genetic interventions by selective and topical activation of therapeutic peptide precursors by enzymatic cleavage. As shown here for glioma cells and the cathepsin B cleavable site, living cells can be treated with high specificity and selectivity for diagnostic and therapeutic purposes. (c) 2006 Elsevier B.V. All rights reserved
    Type of Publication: Journal article published
    PubMed ID: 16730647
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  • 5
    Keywords: PEPTIDE ; CANCER ; CANCER CELLS ; CELLS ; IN-VITRO ; radiotherapy ; AGENTS ; CELL ; Germany ; IN-VIVO ; PROSTATE ; VITRO ; VIVO ; GENERATION ; QUANTIFICATION ; SYSTEM ; DRUG ; EFFICIENCY ; ACTIVATION ; CONTRAST ; CONTRAST AGENT ; BIOLOGY ; MOLECULAR-BIOLOGY ; molecular imaging ; NUCLEI ; TARGET ; prostate cancer ; PROSTATE-CANCER ; CANCER-CELLS ; bioshuttle ; DELIVERY ; TARGET-CELLS ; CARRIERS ; CONTRAST AGENTS ; AGENT ; molecular biology ; molecular ; RE ; drug targeting ; DRUGS ; in vivo ; PLASMID ; transfer efficiency ; PLATFORM ; plasmid delivery
    Abstract: This paper presents the BioShuttle platform as a delivery vehicle for transfer of contrast agents and genetic material into target cells, which can be followed by activation of the BioShuttle inside the target cell. Here, we present a transporter system and summarize the findings on transporter use in vivo and in vitro. The results here are limited to examples where cargoes (drugs, genetically active materials or contrast agents) are covalently associated with the transporter module. A further example, in which the cargo is non-covalently attached to the BioShuttle, is also discussed. Finally, attempts have been made to solve some of the issues surrounding the efficiency of transfer of therapeutic or diagnostic agents and their later activity in the cell
    Type of Publication: Journal article published
    PubMed ID: 17635158
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  • 6
    Keywords: PEPTIDE ; SIMULATIONS ; CANCER ; CELLS ; INHIBITOR ; CELL ; Germany ; human ; LUNG ; MICROSCOPY ; DRUG ; DYNAMICS ; SIMULATION ; MOLECULE ; FORM ; TRANSPORT ; virus ; MEMBRANE ; LYMPHOCYTES ; bioshuttle ; DELIVERY ; MITOCHONDRIA ; PEPTIDES ; HUMAN IMMUNODEFICIENCY VIRUS ; LIVING CELLS ; 1 ; IMMUNODEFICIENCY-VIRUS ; MEMBRANES ; HUMAN-IMMUNODEFICIENCY-VIRUS ; MOLECULAR-DYNAMICS ; HIV-1 ; HUMAN-LYMPHOCYTES ; CAPACITY ; ASSEMBLIES ; assembly ; CLSM ; development ; structure ; solubility ; DRUG DEVELOPMENT ; docking ; anti-HIV ; CANDIDATE ; cancer research ; capsid ; TOXICOLOGY ; VICINITY ; DIVISION ; German ; molecular dynamics ; circular dichroism ; CIRCULAR-DICHROISM ; confocal laser scanning microscopy ; CD ; A ; AS ; Research ; DICHROISM ; HIV 1 ; HUMAN IMMUNODEFICIENCY ; IMMUNODEFICIENCY ; LA ; LASER ; LASER SCANNING MICROSCOPY ; Lead ; LYMPHOCYTE
    Abstract: The Human immunodeficiency virus 1 derived capsid assembly inhibitor peptide (HIV-1 CAI-peptide) is a promising lead candidate for anti-HIV drug development. Its drawback, however, is that it cannot permeate cells directly. Here we report the transport of the pharmacologically active CAI-peptide into human lymphocytes and Human Embryonic Lung cells (HEL) using the BioShuttle platform. Generally, the transfer of pharmacologically active substances across membranes, demonstrated by confocal laser scanning microscopy (CLSM), could lead to a loss of function by changing the molecule's structure. Molecular dynamics (MD) simulations and circular dichroism (CD) studies suggest that the CAI-peptide has an intrinsic capacity to form a helical structure, which seems to be critical for the pharmacological effect as revealed by intensive docking calculations and comparison with control peptides. This coupling of the CAI-peptide to a BioShuttle-molecule additionally improved its solubility. Under the conditions described, the HIV-1 CAI peptide was transported into living cells and could be localized in the vicinity of the mitochondria.
    Type of Publication: Journal article published
    PubMed ID: 18695744
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