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  • 1
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    A specific inhibitor of the epidermal growth factor receptor tyrosine kinase (1994)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1994-08-19
    Description: A small molecule called PD 153035 inhibited the epidermal growth factor (EGF) receptor tyrosine kinase with a 5-pM inhibition constant. The inhibitor was specific for the EGF receptor tyrosine kinase and inhibited other purified tyrosine kinases only at micromolar or higher concentrations. PD 153035 rapidly suppressed autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocked EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. PD 153035 demonstrates an increase in potency over that of other tyrosine kinase inhibitors of four to five orders of magnitude for inhibition of isolated EGF receptor tyrosine kinase and three to four orders of magnitude for inhibition of cellular phosphorylation.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Fry, D W -- Kraker, A J -- McMichael, A -- Ambroso, L A -- Nelson, J M -- Leopold, W R -- Connors, R W -- Bridges, A J -- New York, N.Y. -- Science. 1994 Aug 19;265(5175):1093-5.〈br /〉〈span class="detail_caption"〉Author address: 〈/span〉Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/8066447" target="_blank"〉PubMed〈/a〉
    Keywords: 3T3 Cells ; Animals ; Cell Transformation, Neoplastic/drug effects ; Epidermal Growth Factor/pharmacology ; Fibroblast Growth Factor 2/pharmacology ; Gene Expression/drug effects ; Humans ; Kinetics ; Mice ; Mitosis/drug effects ; Phosphorylation/drug effects ; Platelet-Derived Growth Factor/pharmacology ; Protein-Tyrosine Kinases/antagonists & inhibitors ; Quinazolines/*antagonists & inhibitors ; Receptor, Epidermal Growth Factor/*antagonists & inhibitors ; Tumor Cells, Cultured ; Tyrosine/metabolism
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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  • 2
    Electronic Resource
    Electronic Resource
    Alterations of the carrier-mediated transport of an anionic solute, methotrexate, by charged liposomes in Ehrlich ascites tumor cells (1979)
    Springer
    The journal of membrane biology 50 (1979), S. 123-140 
    Details
    ISSN: 1432-1424
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Interaction of positively charged liposomes with Ehrlich ascites tumor cells increases the bidirectional transmembrane fluxes of the anionic folic acid analog, methotrexate. Negative liposomes reduce methotrexate influx. Stimulation of methotrexate influx by positively charged liposomes is time and concentration dependent, requiring at least a 5-min incubation with 2.5mm phosphatidylcholine containing 20% stearylamine for maximum effect. Stimulation is not appreciably reversed by washing the cells. Similar increases are observed for influx and efflux so that there is no change in the steady-state methotrexate electrochemical-potential difference across the cell membrane. The increase in influx appears to be a stimulation of the carrier-mediated transport process for methotrexate since both control and stimulated influx are abolished by the competitive inhibitor, 5-formyltetrahydrofolate or the sulfhydryl group inhibitor,p-chloromercuriphenylsulfonic acid and the Q10 of the system remains unchanged. Influx of 5-methyltetrahydrofolate, which shares the same transport carrier as methotrexate, is also stimulated. However, the transport of folic acid, which is structurally similar to methotrexate but does not utilize the carrier, is unaffected. The kinetic change induced by positively charged liposomes is an increase in theV ma in , while theK t in remains unchanged. Trans-stimulation of methotrexate influx by 5-formyltetrahydrofolate occurs to the same extent in the presence or absence of positively charged liposomes. The liposomes have no apparent effect on the intracellular water, the extracellular space, or the chloride distribution ratio. The data suggest that interaction of positively charged liposomes with Ehrlich ascites tumor cells accelerates the rate of transposition of the membrane carrier system for methotrexate, altering the kinetics of transport without a change in transport thermodynamics.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01868944
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  • 3
    Electronic Resource
    Electronic Resource
    Further studies on the charge-related alterations of methotrexate transport in Ehrlich ascites tumor cells by ionic liposomes: Correlation with liposome-cell association (1982)
    Springer
    The journal of membrane biology 66 (1982), S. 87-95 
    Details
    ISSN: 1432-1424
    Keywords: methotrexate ; liposome ; transport ; Ehrlich ; tumor ; cell
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Interaction of positively (phosphatidylcholine/stearylamine 5∶1) or negatively (phosphatidylcholine/stearic acid 5∶1) charged liposomes with Ehrlich ascites tumor cells for 1–5 min increases or decreases, respectively, the bidirectional fluxes of the folic acid analog, methotrexate. These effects on influx and efflux appear to be symmetrical since the liposomes do not change the intracellular level of methotrexate at the steady state. Influx kinetics show that these alterations result from an increase or decrease in theV max with no change in theK m in . These effects appear to be specific for the methotrexate-tetrahydrofolate carrier system since the transport of other compounds which utilize this carrier, aminopterin, 5-methyltetrahydrofolate, and 5-formyltetrahydrofolate, is affected similarly to methotrexate, whereas, the transport of folic acid, a compound similar in structure and charge but not significantly transported by this carrier is unaffected by liposomes. Once cells are exposed to charged liposomes, the effects on methotrexate transport cannot be reversed by washing the cells free of the extracellular liposomes. If, however, cells are exposed to liposomes of one charge, washed and then exposed to liposomes of the opposite charge, methotrexate influx is reversed to control rates. The effects of charged liposomes on methotrexate influx were not abolished by treating the cells with neuraminidase, metabolic inhibitors or lowering the temperature to 4°C. Studies on the uptake of [14C] liposomes show that these effects are not proportional to the total amount of lipid associated with the cell but result from an initial rapid liposome-cell association that is not dependent on temperature or energy metabolism nor related to cell surface charge.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01868485
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  • 4
    Electronic Resource
    Electronic Resource
    Controlled Release of Thermonuclear Energy: Production of High Temperatures and Nuclear Reactions in a Gas Discharge (1958)
    [s.l.] : Nature Publishing Group
    Nature 181 (1958), S. 217-220 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Introduction The basic conditions which must be established before a thermonuclear reactor is possible are, first, the containment of a high-temperature gas so that it is isolated from the walls of the surrounding vessel, and second, the attainment of temperatures sufficiently high for nuclear ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/181217a0
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  • 5
    Electronic Resource
    Electronic Resource
    A Travelling-Wave Linear Accelerator for 4-MeV. Electrons (1948)
    [s.l.] : Nature Publishing Group
    Nature 162 (1948), S. 859-861 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] THE basic principles of this type of accelerator and the details of a first model producing 0-5-MeV. electrons have already been described in Nature1. The accelerator here described follows the same general design, and as the phase velocity approaches the velocity of light the ratio of the inner ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/162859a0
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  • 6
    Electronic Resource
    Electronic Resource
    30-Mev. Electron Synchrotron (1948)
    [s.l.] : Nature Publishing Group
    Nature 161 (1948), S. 504-506 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] FOLLOWING earlier work on the conversion of a betatron to a synchrotron1, a 30-MeV. electron synchrotron has been constructed and was first operated in October 1947. The machine is shown in Fig. 1, and employs a rectangular-yoke magnet, designed to give maximum space for experimental work. A more ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/161504a0
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  • 7
    Electronic Resource
    Electronic Resource
    Travelling-Wave Linear Accelerator for Electrons (1947)
    [s.l.] : Nature Publishing Group
    Nature 160 (1947), S. 351-353 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] THE linear accelerator principle as used in the Sloan and Lawrence positive ion accelerator1 has received a new stimulus from the advent of radar magnetrons giving high peak powers under pulse operation at short wave-lengths. These new techniques are particularly suitable for the acceleration of ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/160351a0
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  • 8
    Electronic Resource
    Electronic Resource
    Dezaguanine mesylate: a new antipurine antimetabolite (1985)
    Springer
    Investigational new drugs 3 (1985), S. 223-231 
    Details
    ISSN: 1573-0646
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 3-Deazaguanine (dezaguanine, USAN; CI-908) is a new antipurine antimetabolite which is entering Phase I studies in the USA. This compound differs from guanine only in the substitution of a carbon for the 3-nitrogen of guanine. Dezaguanine has an unusual spectrum of activity against experimental rodent tumors; its activity against transplantable rodent leukemias is only modest, but it has significant activity against transplantable rodent solid tumors, particularly mammary adenocarcinomas. Mammary adenocarcinoma models against which this compound is active include slow and fast-growing tumors, hormone sensitive and hormone insensitive tumors, and the subrenal capsule implanted human breast cancer xenograft, MX-1. Dezaguanine must be converted to its nucleotides to be active. Dezaguanine nucleotides inhibit synthesis of guanine nucleotides, and can be incorporated into nucleic acids in place of guanine nucleotides; incorporation into DNA may be particularly important in the cytotoxicity of this compound. Addition of certain purines or purine nucleosides can prevent dezaguanine cytotoxicity in vitro. Preclinical studies suggest that dezaguanine does not undergo deamination to 3-deazaxanthine, and is not metabolized by xanthine oxidase. Therefore, this compound may not be subject to metabolic inactivation in vivo, and active metabolites may have a prolonged half-life. This concept is supported by the prolonged half-life of radiolabelled dezaguanine in rats. Finally, dezaguanine can cross the blood-brain barrier. In summary, the novel biochemical and experimental antitumor properties of dezaguanine indicate that this compound could have better activity against some human solid tumors than currently used purine antimetabolites. Preclinical formulation and toxicology studies are now complete, and Phase I human studies are being initiated.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00179426
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  • 9
    Electronic Resource
    Electronic Resource
    Biological and biochemical activities of the novel antitumor antibiotic PD 114,759 and related derivatives (1986)
    Springer
    Investigational new drugs 4 (1986), S. 3-10 
    Details
    ISSN: 1573-0646
    Keywords: antitumor ; antibiotic ; DNA scission
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A complex of novel and exceptionally potent antibiotics has been evaluated for antitumor activity in vitro and in vivo and characterized with regard to their ability to cause DNA strand scission. The major component, PD 114,759, was quite active against all in vitro tumor systems including the human tumors, MCF-7 breast, HCT-8 colon, and A549 lung and the murine tumors M16/c mammary, Lewis lung, Pan 02 pancreas and L1210 leukemia. ID50 values ranged from 2–57 pg/ml. In vivo this agent produced significant increases of host life spans in mice bearing L1210 leukemia, B16 melanoma and the M5076 sarcoma. Further, it inhibited growth of subcutaneous implants of the Ridgway osteogenic sarcoma by 80% and growth of the MX-1 human mammary xenograft by 90–95%. PD 114, 759, however, had no activity against the colon adenocarcinoma 11a or mammary adenocarcinoma 16c. Chinese hamster ovary cells exposed for 24 hours to concentrations of PD 114,759 ranging from 18 to 37 pg/ml accumulated in the S and G2 + M phases of the cell cycle with a corresponding decrease in G1. Higher concentrations of drug apparently stopped any progression through the cell cycle. PD 114,759 caused significant DNA single strand breaks in L1210 cells exposed for 1 hour to drug concentrations as low as 20 pg/ml and the frequency of these lesions increased in proportion to the drug concentration. A portion of these DNA breaks appeared to be associated with protein. In contrast, no double strand DNA breaks were detected at the highest drug concentration tested (100 pg/ml).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00172009
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  • 10
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    Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor (1998)
    National Academy of Sciences
    Details
    Publication Date: 1998-09-29
    Print ISSN: 0027-8424
    Electronic ISSN: 1091-6490
    Topics: Biology , Medicine , Natural Sciences in General
    Published by National Academy of Sciences
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