排序方式: 共有22条查询结果,搜索用时 31 毫秒
1.
2.
Introducing Glycolinkers for the Functionalization of Cytotoxic Drugs and Applications in Antibody–Drug Conjugation Chemistry
下载免费PDF全文
![点击此处可从《ChemMedChem》网站下载免费的PDF全文](/ch/ext_images/free.gif)
Dr. Filip S. Ekholm Henna Pynnönen Anja Vilkman Virve Pitkänen Dr. Jari Helin Juhani Saarinen Tero Satomaa 《ChemMedChem》2016,11(22):2501-2505
Antibody–drug conjugates (ADCs) are promising alternatives to naked antibodies for selective drug‐delivery applications and treatment of diseases such as cancer. Construction of ADCs relies upon site‐selective, efficient and mild conjugation technologies. The choice of a chemical linker is especially important, as it affects the overall properties of the ADC. We envisioned that hydrophilic bifunctional chemical linkers based on carbohydrates would be a useful class of derivatization agents for the construction of linker–drug conjugates and ADCs. Herein we describe the synthesis of carbohydrate‐based derivatization agents, glycolinker–drug conjugates featuring the tubulin inhibitor monomethyl auristatin E and an ADC based on an anti‐EGFR antibody. In addition, an initial in vitro cytotoxicity evaluation of the individual components and the ADC is provided against EGFR‐positive cancer cells. 相似文献
3.
Brian R. Gibson Erna Storgårds Kristoffer Krogerus Virve Vidgren 《Yeast (Chichester, England)》2013,30(7):255-266
Two distinct genetic groups (Saaz and Frohberg) exist within the hybrid Saccharomyces pastorianus (S. cerevisiae × S. eubayanus) taxon. However, physiological/technological differences that exist between the two groups are not known. Fermentative capability of the parental S. eubayanus has likewise never been studied. Here, 58 lager strains were screened to determine which hybrid group they belonged to, and selected strains were characterized to determine salient characteristics. In 15 °P all‐malt wort fermentations at 22 °C, Frohberg strains showed greater growth and superior fermentation (80% apparent attenuation, 6.5% alcohol by volume in 3–4 days) compared to all other strains and maintained highest viability values (>93%). Fermentation with S. eubayanus was poor at the same temperature (33% apparent attenuation, 2.7% alcohol by volume at 6 days and viability reduced to 75%). Saaz strains and S. eubayanus were the least sensitive to cold (10 °C), though this did not translate to greater fermentation performance. Fermentation with S. eubayanus was poor at 10 °C but equal to or greater than that of the Saaz strains. Performance of Saaz yeast/S. eubayanus was limited by an inability to use wort maltotriose. [14C]‐Maltotriose transport assays also showed negligible activity in these strains (≤0.5 µmol min?1 g?1 dry yeast). Beers from Saaz fermentations were characterized by two‐ to sixfold lower production of the flavour compounds methyl butanol, ethyl acetate and 3‐methylbutyl acetate compared to Frohberg strains. Higher alcohol and ester production by S. eubayanus was similar to that of Frohberg strains. Copyright © 2013 John Wiley & Sons, Ltd. 相似文献
4.
M. Vidgren M. Silvasti P. Vidgren H. Sormunen K. Laurikainen P. Korhonen 《Aerosol science and technology》2013,47(4):335-345
Due to the depletion of ozone layer linked to CFf propellants used in metered-dose inhalers (MDIs), alternative drug delivery systems for inhalation therapy of bronchial asthma is required. Dry powder inhalers have become a remarkable alternative to the MDIs. The research of powder delivery systems has strongly been focused on developing portable, preloaded multiple-dose powder inhalers, from which patients can reliably inhale several drug doses. Recently, a novel multiple-dose powder inhaler (Easyhaler®) has been developed. Easyhaler® is a suitable drug delivery system for various drugs already available or still under development. Optimum patient compliance is achieved by a design similar to the dose delivery system of the conventional MDI. In addition, the construction of the device allows high dose reproducibility and good in vitro and in vivo deposition of inhaled drug particles. Consequently, equal therapeutic efficacy, safety and tolerability with an MDI is documented in clinical trials. Thus the pharmaceutical, biopharmaceutical, and clinical features as well as the similar mode of use would facilitate a smooth transition from the freon based MDIs to the Easyhaler® multiple-dose powder inhaler. 相似文献
5.
Variation in α‐acetolactate production within the hybrid lager yeast group Saccharomyces pastorianus and affirmation of the central role of the ILV6 gene
下载免费PDF全文
![点击此处可从《Yeast (Chichester, England)》网站下载免费的PDF全文](/ch/ext_images/free.gif)
6.
Hagren V von Lode P Syrjälä A Korpimäki T Tuomola M Kauko O Nurmi J 《International journal of food microbiology》2008,125(2):158-161
We describe a system consisting of rapid sample enrichment and homogeneous end-point PCR analysis that enables the detection of Salmonella in various food matrices in 8 h. Sample preparation starts with 6 h enrichment step in supplemented broth, after which Salmonella cells are collected with immunomagnetic particles. The particles are washed and dispensed to ready-to-use PCR reaction vessels, which contain dried assay-specific reagents and an internal amplification control. PCR is performed with a novel instrument platform utilising the sensitive label technology of time-resolved fluorometry. Qualitative assay results are automatically interpreted and available in 45 min after sample addition. The overall accuracy, sensitivity and specificity of the Magda CA Salmonella system were 99.1%, 98.4% and 100.0%, respectively, based on the evaluation of 107 samples (beef, pork, poultry and ready-to-eat meals) artificially contaminated with sub-lethally injured Salmonella cells. 相似文献
7.
Helvi M. Vidgren Jyrki J. Ågren Ursula Schwab Tiina Rissanen Osmo Hänninen Matti I. J. Uusitupa 《Lipids》1997,32(7):697-705
The effects of n-3 fatty acid supplementation in the form of fresh fish, fish oil, and docosahexaenoic acid (DHA) oil on the
fatty acid composition of plasma lipid fractions, and platelets and erythrocyte membranes of young healthy male students were
examined. Altogether 59 subjects (aged 19–32 yr, body mass index 16.8–31.3 kg/m2) were randomized into the following diet groups: (i) control group; (ii) fish diet group eating fish meals five times per
week [0.38±0.04 g eicosapentaenoic acid (EPA) and 0.67±0.09 g DHA per day]; (iii) DHA oil group taking algae-derived DHA oil
capsules (1.68 g/d DHA oil group taking algae-derived DHA oil capsules (1.68 g/d DHA in triglyceride form); and (iv) fish
oil group (1.33 g EPA and 0.95 g DHA/d as free fatty acids) for 14 wk. The fatty acid composition of plasma lipids, platelets,
and erythrocyte membranes was analyzed by gas chromatography. The subjects kept 4-d food records four times during the study
to estimate the intake of nutrients. In the fish diet, in DHA oil, and in fish oil groups, the amounts of n-3 fatty acids
increased and those of n-6 fatty acids decreased significantly in plasma lipid fractions and in platelets and erythrocyte
membranes. A positive relationship was shown between the total n-3 polyunsaturated fatty acids (PUFA) and EPA and DHA intake
and the increase in total n-3 PUFA and EPA and DHA in all lipid fractions analyzed. DHA was preferentially incorporated into
phospholipid (PL) and triglyceride (TG) and there was very little uptake in cholesterol ester (CE), while EPA was preferentially
incorporated into PL and CE. The proportion of EPA in plasma lipids and platelets and erythrocyte membranes increased also
by DHA supplementation, and the proportion of linoleic acid increased in platelets and erythrocyte membranes in the DHA oil
group as well. These results suggest retroconversion of DHA to EPA and that DHA also interferes with linoleic acid metabolism. 相似文献
8.
9.
Sulfa antibiotics (sulfonamides) are used in veterinary and human medicine for therapeutic and prophylactic purposes. Veterinary use can result in foodstuffs derived from animals being contaminated with residual sulfonamides. Current sulfonamide-screening methods (mainly based on bacterial growth inhibition) are slow and inaccurate, since sensitivities of bacteria to different sulfonamides vary a lot. Therefore, a rapid immunoassay that was able to detect at least 18 different sulfonamides at the MRL level (100 microg/kg) from food samples in a single reaction was developed. The assay was reproducible and adequately accurate for screening purposes. The presence of sulfonamide metabolites did not cause major assay interference. We also demonstrated reliable detection of sulfonamides from a panel of meat, milk, and serum samples with the assay. 相似文献
10.