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    Wyświetlanie 1-4 z 4
    Tytuł:
    Areny jako proleki
    Arenes as prodrugs
    Autorzy:
    Guzik, U.
    Hupert-Kocurek, K.
    Nieć, A.
    Wojcieszyńska, D.
    Powiązania:
    https://bibliotekanauki.pl/articles/171928.pdf
    Data publikacji:
    2015
    Wydawca:
    Polskie Towarzystwo Chemiczne
    Tematy:
    prolek
    związki aromatyczne
    aktywacja proleku
    prodrug
    aromatic compounds
    prodrugs activation
    Opis:
    Nowadays, improvement of physicochemical, biopharmaceutical and pharmacokinetic properties of pharmacologically active compounds is connected with development of prodrugs. Prodrugs are defined as pharmaceutical compounds inactive in their parent form and converted either chemically or enzymatically to the active derivative in the organism. A lot of prodrugs are aromatic compounds because of benzene ring reactivity. There are two main classes of prodrugs. In the carrier-linked prodrugs, the active drug is linked to a carrier through bioreversible covalent bond removed by enzymatic or chemical reactions. The second class comprises bioprecursor prodrugs that are modified in the body to induce the functional groups. Additionally, based on the site of prodrugs conversion into their active forms, they are classified into two groups: prodrugs metabolized intracellulary and prodrugs metabolized extracellulary. Chemical or enzymatic transformation of prodrugs may occur through their reduction, decarboxylation, oxidative deamination, cyclization, phosphorylation and/or hydrolysis. These reactions enable to overcome different barriers in drug delivery through changes in aqueous solubility, chemical instability and insufficient oral adsorption. It may also cause prolonged duration of drug action. Moreover, the prodrugs strategy allows achieving brain and tumor specific targeting. Summarizing, the designing of the prodrugs seems to be one of the most promising strategies to enhance the therapeutic effect of drugs and reduction of their negative side effects.
    Źródło:
    Wiadomości Chemiczne; 2015, 69, 3-4; 255-269
    0043-5104
    2300-0295
    Pojawia się w:
    Wiadomości Chemiczne
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    CEA-negative glioblastoma and melanoma cells are sensitive to cytosine deaminase/5-fluorocytosine therapy directed by the carcinoembryonic antigen promoter.
    Autorzy:
    Dąbrowska, Anna
    Szary, Jarosław
    Kowalczuk, Małgorzata
    Szala, Stanisław
    Ugorski, Maciej
    Powiązania:
    https://bibliotekanauki.pl/articles/1041550.pdf
    Data publikacji:
    2004
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    CEA promoter
    E. coli cytosine deaminase
    gene-directed enzyme prodrug therapy
    Opis:
    Recent studies have suggested that carcinoembryonic antigen (CEA)-promoter sequences are active only in CEA-positive cells, filing in the criteria for tumor specific targeting of suicide genes. However, the present study on gene therapy of colon cancer and cell-specificity of CEA promoter, provide evidence that CEA-positive and CEA-negative cells transfected with E. coli cytosine deaminase (CD) gene under the control of CEA promotor sequence are sensitive to enzyme/pro-drug therapy with 5-fluorocytosine (5-FC). Individual clones derived from the CEA-negative cell lines: melanoma Hs294T and glioblastoma T98G after transfection with CD differed profoundly in their sensitivity to 5-FC. The IC50 values for several clones of the CEA-negative cells were almost the same as for CEA-positive colon cancer cells. Such 5-FC-sensitive clones derived from the population of CEA-negative cells, present even in small number, because of the very effective bystender effect of this enzyme/pro-drug system can cause severe problems during therapy by efficiently killing surrounding normal cells. Safety is the major issue in gene therapy. Our data suggest that the safety of gene-directed enzyme pro-drug therapy (GDEPT) with CEA promoter driven expression of therapeutic genes is not so obvious as it has originally been claimed.
    Źródło:
    Acta Biochimica Polonica; 2004, 51, 3; 723-732
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Pronukleotydy o strukturze amidofosforanów i ich wewnątrzkomórkowy mechanizm aktywacji
    Phosphoramidate pronucleotides and their intracellular activation mechanism
    Autorzy:
    Kulik, K.
    Baraniak, J.
    Powiązania:
    https://bibliotekanauki.pl/articles/171604.pdf
    Data publikacji:
    2014
    Wydawca:
    Polskie Towarzystwo Chemiczne
    Tematy:
    pronukleotydy
    amidofosforany
    aktywność fosforoamidazowa
    Hint
    białko triady histydynowej wiążącej nukleotyd
    prolek
    pronucleotides
    phosphoramidates
    phosphoramidase activity
    histidine triad nucleotide binding protein
    prodrug
    Opis:
    Nucleoside analogues have great therapeutic potential for the treatment of cancer and viral diseases. Once inside the cell, they are activated by a series of intracellular phosphorylation steps to produce 5’-triphosphate derivatives, which can be incorporated to DNA or RNA and act as terminators of growing polynucleotide chains [1c]. In many cases, nucleoside analogues are poor substrates for the cellular kinases needed for their activation [5]. It is clear that intracellular introduction of nucleoside analogues as phosphorylated metabolites (so called pronucleotides) could circumvent difficulties associated with the use of non-phosphorylated nucleoside analogues and could even activate inactive compounds or could increase the activity of the nucleoside analogues. However, polarity and a ready degradation by phosphatases make the use of free nucleotide analogues impractical. Therefore, much of the recent efforts have been focused on finding suitable prodrugs of nucleoside analogue monophosphates. Among the current diverse prodrug approaches, nucleoside phosphoramidate derivatives appear to be an interesting class of antiviral and anticancer agents [1c]. These prodrugs, as are devoid of negative charge, should be able to cross the cell membrane either by diffusion or utilizing transport protein [1c]. Conducted cell extract studies have provided evidence of a bioactivation mechanism that relies on enzyme-catalyzed P-N bond hydrolysis in phosphoramidate pronucleotides [1a,b]. It was assumed that phosphoramidate derivatives should generate nucleoside monophosphates inside the cell at rates that are influenced by both the nature of the amino group and the pH of the medium. Then nucleoside monophosphates should be phosphorylated in two different steps to the corresponding 5’-O-triphosphates (NTP) which can inhibit polymerase or be incorporated into the DNA strand being synthesized in the cell. Over the last decade extensive studies has been carried out to establish the mechanism of action of phosphoramidates and identification of enzymes responsible for bioactivation this pronucleotides to phosphorylated nucleosides [7, 21, 24]. Investigation of metabolism pathways provided evidence that phosphoramidase activity of Hint (histidine triad nucleotide-binding proteins) play a key role in the activation of phosphoramidate pronucleotides [23–27].
    Źródło:
    Wiadomości Chemiczne; 2014, 68, 9-10; 811-831
    0043-5104
    2300-0295
    Pojawia się w:
    Wiadomości Chemiczne
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synteza biodegradowalnych poliestrów z zastosowaniem katalizatorów i inicjatorów naturalnych
    Synthesis of biodegradable polyesters using natural catalysts and initiators
    Autorzy:
    Sawicka, A.
    Oledzka, E.
    Sobczak, M.
    Kołodziejski, W.
    Powiązania:
    https://bibliotekanauki.pl/articles/947524.pdf
    Data publikacji:
    2017
    Wydawca:
    Sieć Badawcza Łukasiewicz - Instytut Chemii Przemysłowej
    Tematy:
    polimer biodegradowalny
    koniugat wielkocząsteczkowy
    prolek wielkocząsteczkowy
    polimeryzacja z otwarciem pierścienia (ROP)
    katalizator
    naturalny inicjator
    biodegradable polymer
    macromolecular conjugate
    macromolecular prodrug
    ring-opening polymerization (ROP)
    catalyst
    natural initiator
    Opis:
    Artykuł stanowi przegląd literatury dotyczącej wykorzystania związków pochodzenia naturalnego i nietoksycznych jako inicjatorów i/lub katalizatorów polimeryzacji z otwarciem pierścienia (ROP) cyklicznych estrów prowadzącej do otrzymania biodegradowalnych i bioresorbowalnych poliestrów stosowanych w medycynie i farmacji. Dokonano klasyfikacji naturalnych inicjatorów ROP na zawierające funkcyjne grupy aminowe lub hydroksylowe. Opisano również możliwość zastosowania związków naturalnych jako kokatalizatorów ROP oraz naturalnych katalizatorów organicznych tego procesu.
    The paper is a review of the literature concerning the application of non-toxic and natural compounds, as initiators and/or catalysts of ring-opening polymerization (ROP) of cyclic esters in the synthesis of biodegradable and bioresorbable polymers for medical and pharmaceutical purposes. The classification of natural ROP initiators as those containing functional amino and hydroxyl groups has been presented. The possibility of using natural compounds as ROP cocatalysts and organocatalysts was also described.
    Źródło:
    Polimery; 2017, 62, 9; 633-641
    0032-2725
    Pojawia się w:
    Polimery
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-4 z 4

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