LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 10 of total 301

Search options

  1. Article: Survival of enteric bacteria in seawater.

    Rozen, Y / Belkin, S

    FEMS microbiology reviews

    2001  Volume 25, Issue 5, Page(s) 513–529

    Abstract: Enteric bacteria exposed to the marine environment simultaneously encounter a variety of abiotic and biotic challenges. Among the former, light appears to be critical in affecting seawater survival; previous growth history plays a major part in ... ...

    Abstract Enteric bacteria exposed to the marine environment simultaneously encounter a variety of abiotic and biotic challenges. Among the former, light appears to be critical in affecting seawater survival; previous growth history plays a major part in preadaptation of the cells, and stationary phase cells are generally more resistant than exponentially growing ones. Predation, mostly by protozoa, is probably the most significant biotic factor. Using Escherichia coli as a model, a surprisingly small number of genes was found that, when mutated, significantly affect seawater sensitivity of this bacterium. Most prominent among those is rpoS, which was also dominant among genes induced upon transfer to seawater.
    MeSH term(s) Enterobacteriaceae/growth & development ; Seawater/microbiology
    Language English
    Publishing date 2001-12
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 283740-7
    ISSN 1574-6976 ; 0168-6445
    ISSN (online) 1574-6976
    ISSN 0168-6445
    DOI 10.1111/j.1574-6976.2001.tb00589.x
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 2165: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  2. Article: Improved method for the quality assurance of [C-11]choline.

    Mishani, E / Ben-David, I / Rozen, Y

    Nuclear medicine and biology

    2002  Volume 29, Issue 3, Page(s) 359–362

    Abstract: C-11]choline is a very promising radiomarker for the diagnosis of various human tumors using Positron Emission Tomography (PET). The existing quality control process for [C-11]choline is complicated and combines two HPLC methods with limited separation ... ...

    Abstract [C-11]choline is a very promising radiomarker for the diagnosis of various human tumors using Positron Emission Tomography (PET). The existing quality control process for [C-11]choline is complicated and combines two HPLC methods with limited separation and sensitivity which prevent the accurate determination of the specific activity. We have developed a new efficient single HPLC method for the detection of choline chloride and dimethylaminoethanol with high resolution and sensitivity using cation-exchange chromatography.
    MeSH term(s) Choline/chemistry ; Choline/standards ; Chromatography, High Pressure Liquid ; Chromatography, Ion Exchange ; Deanol/chemistry ; Quality Control ; Radiopharmaceuticals/chemistry ; Radiopharmaceuticals/standards ; Reference Standards ; Solutions
    Chemical Substances Radiopharmaceuticals ; Solutions ; Deanol (2N6K9DRA24) ; Choline (N91BDP6H0X)
    Language English
    Publishing date 2002-04
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1138098-6
    ISSN 1872-9614 ; 0969-8051 ; 0883-2897
    ISSN (online) 1872-9614
    ISSN 0969-8051 ; 0883-2897
    DOI 10.1016/s0969-8051(01)00311-0
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 1090: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  3. Article ; Online: Seawater Activation of Escherichia coli Gene Promoter Elements: Dominance of rpoS Control.

    Rozen, Y. / Dyk, T.K. / LaRossa, R.A. / Belkin, S.

    Microbial ecology

    2001  Volume 42, Issue 4, Page(s) 635–643

    Abstract: The release of non-disinfected wastewater into the marine environment is a common practice in many countries; nevertheless, the molecular mechanisms involved in determining the survival of enteric bacteria in seawater are poorly understood, in spite of ... ...

    Abstract The release of non-disinfected wastewater into the marine environment is a common practice in many countries; nevertheless, the molecular mechanisms involved in determining the survival of enteric bacteria in seawater are poorly understood, in spite of the obvious public health implications. In a methodological attempt to address this issue, a plasmid-based collection of 687 Escherichia coli distinct promoter::luxCDABE fusions was screened to identify promoters that are induced upon exposure to seawater. The luminescence driven by 22 out of these promoters reproducibly increased at least two-fold in an artificial seawater medium; only 9 of the corresponding genes have previously been assigned a function. The most prominent characteristic of the induced genes was that most (18 out of 22) were under rpoS control. The induction of these seawater-responsive promoters was evaluated in different media to identify the cause of the increased transcription. Salinity or osmolarity was instrumental in only four cases, and in three promoters, increased pH also seemed to play a role; however, the most significant environmental effector in inducing the majority of the seawater-induced promoters appeared to be nutrient limitation.
    Language English
    Publishing date 2001-12
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1462065-0
    ISSN 1432-184X ; 0095-3628
    ISSN (online) 1432-184X
    ISSN 0095-3628
    DOI 10.1007/s00248-001-1012-x
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  4. Article: Specific detection of p-chlorobenzoic acid by Escherichia coli bearing a plasmid-borne fcbA'::lux fusion.

    Rozen, Y / Nejidat, A / Gartemann, K H / Belkin, H

    Chemosphere

    2000  Volume 38, Issue 3, Page(s) 633–641

    Abstract: In this communication we report on a genetically engineered bacterium that reacts by light emission to the presence of 4-chlorobenzoic acid. To construct this strain, DNA fragment (1.7 kb) upstream from the 4-chlorobenzoic acid dehalogenase (fcb) operon ... ...

    Abstract In this communication we report on a genetically engineered bacterium that reacts by light emission to the presence of 4-chlorobenzoic acid. To construct this strain, DNA fragment (1.7 kb) upstream from the 4-chlorobenzoic acid dehalogenase (fcb) operon of Arthrobacter SU was fused to Vibriofischeri luxCDABE genes. An Escherichia coli strain transformed with a multi-copy plasmid (pASU) bearing this fusion responded to the presence of 4-chlorobenzoic acid and a few closely related compounds by increased luminescence, exhibiting a high specificity but a relatively low sensitivity. While it could be somewhat, improved by manipulating the experimental pH, sensitivity remained too low for real time applicability. Nevertheless, the principle of using dehalogenase promoters as environmental pollution sensor was demonstrated.
    MeSH term(s) Arthrobacter/enzymology ; Arthrobacter/genetics ; Benzoates/pharmacology ; Chlorobenzoates/analysis ; Chlorobenzoates/metabolism ; Chlorobenzoates/pharmacology ; Culture Media ; Escherichia coli/drug effects ; Escherichia coli/metabolism ; Hydrogen-Ion Concentration ; Hydrolases/genetics ; Indicators and Reagents ; Industrial Waste/adverse effects ; Industrial Waste/analysis ; Luminescent Measurements ; Photobacterium/drug effects ; Plasmids
    Chemical Substances Benzoates ; Chlorobenzoates ; Culture Media ; Indicators and Reagents ; Industrial Waste ; Hydrolases (EC 3.-) ; 4-chlorobenzoate dehalogenase (EC 3.8.1.6) ; 4-chlorobenzoic acid (IC7888DF4L)
    Language English
    Publishing date 2000-02-23
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120089-6
    ISSN 1879-1298 ; 0045-6535 ; 0366-7111
    ISSN (online) 1879-1298
    ISSN 0045-6535 ; 0366-7111
    DOI 10.1016/s0045-6535(98)00210-0
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 2540: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  5. Article: Seawater Activation of Escherichia coli Gene Promoter Elements: Dominance of rpoS Control

    Rozen, Y / R.A. LaRossa / S. Belkin / T.K. Dyk

    Microbial ecology. 2001 Dec., v. 42, no. 4

    2001  

    Abstract: The release of non-disinfected wastewater into the marine environment is a common practice in many countries; nevertheless, the molecular mechanisms involved in determining the survival of enteric bacteria in seawater are poorly understood, in spite of ...

    Abstract : The release of non-disinfected wastewater into the marine environment is a common practice in many countries; nevertheless, the molecular mechanisms involved in determining the survival of enteric bacteria in seawater are poorly understood, in spite of the obvious public health implications. In a methodological attempt to address this issue, a plasmid-based collection of 687 Escherichia coli distinct promoter::luxCDABE fusions was screened to identify promoters that are induced upon exposure to seawater. The luminescence driven by 22 out of these promoters reproducibly increased at least two-fold in an artificial seawater medium; only 9 of the corresponding genes have previously been assigned a function. The most prominent characteristic of the induced genes was that most (18 out of 22) were under rpoS control. The induction of these seawater-responsive promoters was evaluated in different media to identify the cause of the increased transcription. Salinity or osmolarity was instrumental in only four cases, and in three promoters, increased pH also seemed to play a role; however, the most significant environmental effector in inducing the majority of the seawater-induced promoters appeared to be nutrient limitation.
    Keywords Escherichia coli ; genes ; intestinal microorganisms ; luminescence ; marine environment ; osmolarity ; pH ; promoter regions ; public health ; salinity ; seawater ; wastewater
    Language English
    Dates of publication 2001-12
    Size p. 635-643.
    Publishing place Springer-Verlag
    Document type Article
    ZDB-ID 1462065-0
    ISSN 1432-184X ; 0095-3628
    ISSN (online) 1432-184X
    ISSN 0095-3628
    DOI 10.1007/s00248-001-1012-x
    Database NAL-Catalogue (AGRICOLA)

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  6. Article: Radiosynthesis of ML03, a novel positron emission tomography biomarker for targeting epidermal growth factor receptor via the labeling synthon: [11C]acryloyl chloride.

    Ben-David, Iris / Rozen, Yulia / Ortu, Giuseppina / Mishani, Eyal

    Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine

    2003  Volume 58, Issue 2, Page(s) 209–217

    Abstract: An automated procedure for the radiosynthesis of the labeling synthon [11C]acryloyl chloride was developed and applied for labeling several N-acryl amides with carbon-11. [11C]-6-acrylamido-4-(3,4-dichloro-6-fluoroanilino)quinazoline (ML03), a novel PET ... ...

    Abstract An automated procedure for the radiosynthesis of the labeling synthon [11C]acryloyl chloride was developed and applied for labeling several N-acryl amides with carbon-11. [11C]-6-acrylamido-4-(3,4-dichloro-6-fluoroanilino)quinazoline (ML03), a novel PET biomarker targeting the epidermal growth factor receptor tyrosine kinase (EGFr-TK) in cancer, was successfully prepared using this labeled synthon in a fully automated manner. Two other potential anticancer drugs were also labeled using the developed methodology. The potency of ML03 to inhibit autophosphorylation of EGFr-TK was evaluated by an ELISA assay indicating a low IC(50) of 0.037nM.
    MeSH term(s) Acrylamides/chemical synthesis ; Acrylamides/therapeutic use ; Acrylates ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/therapeutic use ; Carbon Radioisotopes ; ErbB Receptors/antagonists & inhibitors ; Humans ; Inhibitory Concentration 50 ; Phosphorylation/drug effects ; Quinazolines/chemical synthesis ; Quinazolines/therapeutic use ; Radiopharmaceuticals/chemical synthesis ; Tomography, Emission-Computed/methods ; Tumor Cells, Cultured
    Chemical Substances Acrylamides ; Acrylates ; Antineoplastic Agents ; Carbon Radioisotopes ; N-(4-((4,5-dichloro-2-fluorophenyl)amino)quinazolin-6-yl)acrylamide ; Quinazolines ; Radiopharmaceuticals ; acryloyl chloride (8K23O56TG5) ; ErbB Receptors (EC 2.7.10.1)
    Language English
    Publishing date 2003-01-28
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S.
    ZDB-ID 1142596-9
    ISSN 1872-9800 ; 0969-8043 ; 0883-2889
    ISSN (online) 1872-9800
    ISSN 0969-8043 ; 0883-2889
    DOI 10.1016/s0969-8043(02)00301-9
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Ue I Zs.279: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  7. Article: Potential (18)F-labeled biomarkers for epidermal growth factor receptor tyrosine kinase.

    Bonasera, T A / Ortu, G / Rozen, Y / Krais, R / Freedman, N M / Chisin, R / Gazit, A / Levitzki, A / Mishani, E

    Nuclear medicine and biology

    2001  Volume 28, Issue 4, Page(s) 359–374

    Abstract: As PET candidate tracers for EGFr-TK, five 4-(anilino)quinazoline derivatives, each fluorinated in the aniline moiety, were prepared. Each was tested in vitro for inhibition of EGFr autophosphorylation in A431 cell line. The leading compounds were then ... ...

    Abstract As PET candidate tracers for EGFr-TK, five 4-(anilino)quinazoline derivatives, each fluorinated in the aniline moiety, were prepared. Each was tested in vitro for inhibition of EGFr autophosphorylation in A431 cell line. The leading compounds were then radiolabeled with (18)F and cell binding experiments, biodistribution and PET studies in A431 tumor-bearing mice were performed. Metabolic studies were carried out in a mice control group. From our results, we concluded that while in vitro experiments indicates efficacy of 4-(anilino)quinazoline compounds, kinetic factors and rapid blood clearance make them unsuitable as tracers for nuclear medicine imaging of EGFr-TK.
    MeSH term(s) Animals ; Cell Division ; Chromatography, High Pressure Liquid ; Enzyme-Linked Immunosorbent Assay ; ErbB Receptors/metabolism ; Fluorine Radioisotopes ; Magnetic Resonance Spectroscopy ; Mice ; Phosphorylation ; Quinazolines ; Radiopharmaceuticals/pharmacokinetics ; Tissue Distribution ; Tomography, Emission-Computed
    Chemical Substances Fluorine Radioisotopes ; Quinazolines ; Radiopharmaceuticals ; ErbB Receptors (EC 2.7.10.1)
    Language English
    Publishing date 2001-05
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1138098-6
    ISSN 1872-9614 ; 0969-8051 ; 0883-2897
    ISSN (online) 1872-9614
    ISSN 0969-8051 ; 0883-2897
    DOI 10.1016/s0969-8051(01)00200-1
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 1090: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  8. Article: Novel iodine-124 labeled EGFR inhibitors as potential PET agents for molecular imaging in cancer.

    Shaul, Mazal / Abourbeh, Galith / Jacobson, Orit / Rozen, Yulia / Laky, Desideriu / Levitzki, Alexander / Mishani, Eyal

    Bioorganic & medicinal chemistry

    2004  Volume 12, Issue 13, Page(s) 3421–3429

    Abstract: The in vivo results with our previously reported irreversible labeled inhibitor [(11)C]-ML03 suggested that more chemically stable inhibitors, labeled with a longer-lived radioisotope, could be better candidates for molecular imaging of epidermal growth ... ...

    Abstract The in vivo results with our previously reported irreversible labeled inhibitor [(11)C]-ML03 suggested that more chemically stable inhibitors, labeled with a longer-lived radioisotope, could be better candidates for molecular imaging of epidermal growth factor receptor (EGFR) positive tumors. On the basis of this hypothesis we synthesized three new irreversible tyrosine kinase (TK) inhibitors with various chemical reactivities. The three new inhibitors were successfully labeled on the anilino moiety with [(124)I], starting with the 6-amino-4-[(3-tributylstannylphenyl)amino]-quinazoline (9) precursor. The cell-free results, obtained with these new irreversible inhibitors, indicated that compounds 5 (alpha-chloro-acetamide derivative) and 6 (4-dimethylamino-but-2-enoic amide derivative) possessed high potencies toward the EGFR with an irreversible inhibition effect. Compound 4 (alpha-methoxy-acetamide derivative) was found to be less potent, with only a partially irreversible effect. The high potency of compounds 5 and 6 toward the EGFR establishes their potential as PET agents for molecular imaging of EGFR positive tumors. Their prospect as PET biomarkers is further being investigated.
    MeSH term(s) Cell Line, Tumor ; Enzyme Inhibitors/analysis ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Humans ; Inhibitory Concentration 50 ; Iodine Radioisotopes ; Molecular Structure ; Neoplasms/diagnosis ; Neoplasms/metabolism ; Neoplasms/pathology ; Positron-Emission Tomography/instrumentation ; Receptor, Epidermal Growth Factor/antagonists & inhibitors ; Receptor, Epidermal Growth Factor/metabolism
    Chemical Substances Enzyme Inhibitors ; Iodine Radioisotopes ; Receptor, Epidermal Growth Factor (EC 2.7.10.1)
    Language English
    Publishing date 2004-07-01
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1161284-8
    ISSN 1464-3391 ; 0968-0896
    ISSN (online) 1464-3391
    ISSN 0968-0896
    DOI 10.1016/j.bmc.2004.04.044
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 3815: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  9. Article: Gene expression analysis of the response by Escherichia coli to seawater.

    Rozen, Yael / Larossa, Robert A / Templeton, Lori J / Smulski, Dana R / Belkin, Shimshon

    Antonie van Leeuwenhoek

    2002  Volume 81, Issue 1-4, Page(s) 15–25

    Abstract: Gene expression of Escherichia coli cells exposed to seawater for 20 h was compared to that of exponentially growing cells (mops-glucose 0.2%) using DNA microarray technology. The expression of most (ca. 3,000) of the 4,228 open reading frames on the ... ...

    Abstract Gene expression of Escherichia coli cells exposed to seawater for 20 h was compared to that of exponentially growing cells (mops-glucose 0.2%) using DNA microarray technology. The expression of most (ca. 3,000) of the 4,228 open reading frames on the microarray remained unchanged; the relative expression of about 320 genes decreased in seawater, whereas that of ca. one fourth (937) increased. Clearly coherent expression patterns were observed for several functional gene groups. Induced genes were numerous in groups specifying the degradation of small molecules (carbon compounds, amino acids and fatty acids), energy metabolism (aerobic and anaerobic respiration, pyruvate dehydrogenase and TCA cycle), chemotaxis and mobility, flagella biosynthesis, surface structures and phage related functions. Repressed genes were clustered in two groups, cell division and nucleotides biosynthesis, indicating a cessation of growth.
    MeSH term(s) Escherichia coli/genetics ; Escherichia coli/growth & development ; Escherichia coli/metabolism ; Escherichia coli Proteins/genetics ; Escherichia coli Proteins/metabolism ; Gene Expression Profiling ; Gene Expression Regulation, Bacterial ; Genome, Bacterial ; Oligonucleotide Array Sequence Analysis ; Seawater/microbiology
    Chemical Substances Escherichia coli Proteins
    Language English
    Publishing date 2002-10-01
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 214861-4
    ISSN 1572-9699 ; 0003-6072
    ISSN (online) 1572-9699
    ISSN 0003-6072
    DOI 10.1023/a:1020500821856
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Ud II Zs.94: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  10. Article: High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging agent candidates of EGFR overexpressing tumors.

    Mishani, Eyal / Abourbeh, Galith / Jacobson, Orit / Dissoki, Samar / Ben Daniel, Revital / Rozen, Yulia / Shaul, Mazal / Levitzki, Alexander

    Journal of medicinal chemistry

    2005  Volume 48, Issue 16, Page(s) 5337–5348

    Abstract: Previous studies with the anilinoquinazoline epidermal growth factor receptor (EGFR) irreversible inhibitor [(11)C]-ML03 demonstrated a rapid metabolism of the tracer, which led to its low in vivo accumulation in EGFR overexpressing tumors. To enhance ... ...

    Abstract Previous studies with the anilinoquinazoline epidermal growth factor receptor (EGFR) irreversible inhibitor [(11)C]-ML03 demonstrated a rapid metabolism of the tracer, which led to its low in vivo accumulation in EGFR overexpressing tumors. To enhance tumor uptake, the chemical structure of the compound was modified, and four new groups of EGFR inhibitors with a wide range of chemical reactivities were synthesized. Chemical reactivity assay of the compounds, performed with reduced glutathione (GSH), revealed that the group C (4-(dimethylamino)-but-2-enoic amide) derivative was the least chemically reactive against the nucleophilic attack of GSH. Nonetheless, it demonstrated a high inhibitory potency and bound irreversibly to the EGFR. Consequently, the blood stability of the group C compound (5a, ML04) labeled with (11)C was studied. In a time frame of 60 min, no radioactive metabolites were detected in blood. The stability of [(11)C]-5a, as indicated both from in vitro blood-stability assays and injection into nude rats, was significantly higher as compared to [(11)C]-ML03. Since group C presented a greater promise for tumor accumulation, it represents, to date, the most suitable candidate for radiolabeling with long-lived positron emission tomography (PET) radioisotopes.
    MeSH term(s) Animals ; Carbon Radioisotopes ; Cell Line ; Drug Stability ; Glutathione/chemistry ; Humans ; Male ; Mice ; Neoplasms/metabolism ; Phosphorylation ; Positron-Emission Tomography ; Quinazolines/chemical synthesis ; Quinazolines/chemistry ; Quinazolines/pharmacokinetics ; Quinazolines/pharmacology ; Radiopharmaceuticals/chemical synthesis ; Radiopharmaceuticals/chemistry ; Radiopharmaceuticals/pharmacokinetics ; Radiopharmaceuticals/pharmacology ; Rats ; Rats, Nude ; Receptor, Epidermal Growth Factor/antagonists & inhibitors ; Receptor, Epidermal Growth Factor/biosynthesis ; Structure-Activity Relationship
    Chemical Substances Carbon Radioisotopes ; Quinazolines ; Radiopharmaceuticals ; Receptor, Epidermal Growth Factor (EC 2.7.10.1) ; Glutathione (GAN16C9B8O)
    Language English
    Publishing date 2005-08-11
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/jm0580196
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

To top