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排序方式: 共有341条查询结果,搜索用时 10 毫秒
1.
Jonas G. Barlind Linda K. Buckett Sharon G. Crosby Öjvind Davidsson Hans Emtenäs Anne Ertan Ulrik Jurva Malin Lemurell Pablo Morentin Gutierrez Karolina Nilsson Gavin O’Mahony Annika U. Petersson Alma Redzic Fredrik Wågberg Zhong-Qing Yuan 《Bioorganic & medicinal chemistry letters》2013,23(9):2721-2726
[Acyl CoA]monoacylglycerol acyltransferase 2 (MGAT2) is of interest as a target for therapeutic treatment of diabetes, obesity and other diseases which together constitute the metabolic syndrome. In this Letter we report our discovery and optimisation of a novel series of MGAT2 inhibitors. The development of the SAR of the series and a detailed discussion around some key parameters monitored and addressed during the lead generation phase will be given. The in vivo results from an oral lipid tolerance test (OLTT) using the MGAT2 inhibitor (S)-10, shows a significant reduction (68% inhibition relative to na?ve, p <0.01) in plasma triacylglycerol (TAG) concentration. 相似文献
2.
Ulrik Røen 《Hydrobiologia》1987,145(1):125-130
Chydorus arcticus n.sp. (Cladocera: Chydoridae: Chydorinae) is described, figured, and differentiated from the closely relatedC. sphaericus (O.F. Müller, 1785). The known distribution of the species is given, and some aspects of speciation of arctic crustaceans
are pointed out. 相似文献
3.
Ulrik Pedersen-Bjergaard Lars B geskov Nielsen Kai Jensen Lars Edvinsson Inger Jansen Jes Olesen 《Peptides》1989,10(6):1147-1152
Neurokinin A (NKA), substance P (SP) and the two peptides combined (SP + NKA) were injected intracutaneously on the forearm and into the temporal muscle of healthy volunteers. Pain intensity, cutaneous wheal and flare responses and tenderness of the temporal muscle were quantitated. SP but not NKA induced cutaneous pain. This relates the algesic effect of SP to the specific N-terminal amino acid sequence of the peptide, not shared by NKA. NKA, however, potentiated the algesic effect of SP as SP + NKA induced a significantly prolonged cutaneous pain sensation. Both peptides induced wheals, but only SP induced flare. These results confirm previous studies relating wheal formation to the identical C-terminal amino acid sequence of the two peptides and flare reaction to the N-terminal part of SP. Injections into the temporal muscle did not cause pain or tenderness. 相似文献
4.
Filtration rate capacities in 6 species of European freshwater bivalves 总被引:12,自引:0,他引:12
Summary Filtration rate capacities in undisturbed freshwater bivalves were determined by means of two different methods (indirect clearance and suction methods) in Anodonta anatina (L.), Unio tumidus Philipsson, Unio pictorum (L.), Unio crassus Philipsson, Dreissena polymorpha (Pallas) and Sphaerium corneum (L.). In A. anatina, D. polymorpha, and S. corneum the filtration rate (FR, 1 h-1) at 19–20°C as a function of dry tissue weight (DW, g) or ash-free dry weight (AFDW, g) could be expressed by the equations: 1.10 DW0.78, 6.82 DW0.88, and 2.14 AFDW0.92, respectively. In U. tumidus, U. pictorum, and U. crassus filtration rates were comparable with those of A. anatina. In D. polymorpha the b value of the corresponding regression of gill area on dry weight was 0.87. The rates of water transport in freshwater bivalves are 2–8 times lower than in marine bivalves of comparable size. A corresponding difference in the filtration rate per gill area unit is found. The measured filtration rates in undisturbed bivalves are substantially higher (at least 4 times) than previously reported. This indicates that the impact of bivalve water processing on freshwater ecosystems is greater than hitherto suggested. 相似文献
5.
6.
K M Osiecki-Newman D Fabbro T Dinur S Boas S Gatt G Legler R J Desnick G A Grabowski 《Enzyme》1986,35(3):147-153
Two sepharose-bound 1-deoxynojirimycin N-alkyl derivatives, N-(9-carboxynonyl)- and N-(11-carboxyundecyl)-deoxynojirimycin, were used for the affinity purification of acid beta-glucosidase (beta-Glc) from normal and type-1 Ashkenazi Jewish Gaucher disease (AJGD) sources. The capacities of these nondegradable inhibitor supports were 0.5 and 0.75 mg of normal beta-Glc/ml of settled gel, respectively. The purified normal enzyme (14-18% yield) had a specific activity of 1.6 X 10(6) nmol/h/mg protein and was homogeneous as evidenced by a single protein species of Mr = 67,000 on sodium dodecylsulfate-polyacrylamide gel electrophoresis and reverse phase high-performance liquid chromatography (HPLC). Microsequencing demonstrated a single N terminus, and the sequence of the first 22 N-terminal amino acids was colinear with that predicted from the beta-Glc cDNA. Amino acid composition analyses of beta-Glc revealed a high content (35%) of hydrophobic amino acids. The N-decyl-deoxynojirimycin support facilitated the purification of the residual enzyme from type-1 AJGD spleen to about 7,500-fold in four steps with a yield of about 11%. These new affinity supports provided improved stability, capacity and/or specificity compared to other affinity or HPLC methods for purifying this lysosomal glycosidase. 相似文献
7.
Ca2+ efflux from sarcoplasmic reticulum vesicles was studied by measurements of net Ca2+ uptake, 45Ca2+ flux and hydrolysis of energy-rich phosphate. The maximal Ca2+ uptake capacity (150–200 nmol/mg protein at pH 6.7, 10 mM MgCl2 and μ=0.26) was independent of the nature and concentration of the energy-donating substrate (ATP or carbamyl phosphate) and of temperature (15–35°C), suggesting coupling between influx and efflux of Ca2+. In the presence of high concentrations of ATP, this efflux of Ca2+ was much higher than the passive Ca2+ permeation, measured after ATP or Ca2+ depletion of the reaction medium. Ca2+ efflux was imperceptible at vesicle filling levels below 35–40 nmol Ca2+/mg protein, and uncorrelated to the inhibition of the Ca2+-ATPase by high intravesicular Ca2+ concentrations. Analysis of the data indicated that Ca2+ efflux under our conditions probably is associated with one of the Ca2+-ATPase partial reactions occurring after dephosphorylation, rather than with a reversal of the Ca2+ translocation step in the phosphorylated state of the enzyme. Furthermore, passive Ca2+ permeation may be concurrently reduced during the enzymatically active state. It is proposed that both Ca2+ efflux and passive Ca2+ permeation (Ca2+ outflow) proceed via the same channels which are closed (occluded) during part of the Ca2+-ATPase reaction cycle. 相似文献
8.
Ulrik Merrild Vibeke Schiøler Flemming Christensen Ewald Wolny Carl Johan Edeling 《Human genetics》1978,45(1):85-88
Summary Elevated levels of alpha-1-fetoprotein (AFP) were found in the amniotic fluid of a 36-year-old woman in the 15th week of gestation. Because of this and the results of repeated ultrasonography, abortion was induced. An anencephalic fetus with trisomy 18 was delivered. The possible correlation among neural-tube defects, chromosomal abnormalities, and level of AFP is discussed. 相似文献
9.
Nakul Mandal Steffen Heegaard Jan Ulrik Prause Bent Honoré Henrik Vorum 《Biological procedures online》2010,12(1):56-88
The intention of this review is to provide an overview of current methodologies employed in the rapidly developing field of
ocular proteomics with emphasis on sample preparation, two-dimensional polyacrylamide gel electrophoresis (2D-PAGE) and mass
spectrometry (MS). Appropriate sample preparation for the diverse range of cells and tissues of the eye is essential to ensure
reliable results. Current methods of protein staining for 2D-PAGE, protein labelling for two-dimensional difference gel electrophoresis,
gel-based expression analysis and protein identification by MS are summarised. The uses of gel-free MS-based strategies (MuDPIT,
iTRAQ, ICAT and SILAC) are also discussed. Proteomic technologies promise to shed new light onto ocular disease processes
that could lead to the discovery of strong novel biomarkers and therapeutic targets useful in many ophthalmic conditions. 相似文献
10.
Peter Hammershøj Mikkel Jessing Anders Ø. Madsen Knud J. Jensen Jørn B. Christensen Ulrik Boas 《International journal of peptide research and therapeutics》2007,13(1-2):209-212
The development of new linkers (handles) for solid-phase synthesis provides new chemical opportunities for peptide synthesis.
To understand the chemical properties of a recently developed backbone amide linker from a structural perspective, the crystal
structure of S-((5-formyl-3,4-ethylenedioxy)thiophene-2-yl)-3-thiopropionic acid (T-BAL2) was studied. Specifically, we wished
to address whether this highly substituted thiophene retained planarity in the aromatic ring as well as between the aromatic
ring and the aldehyde carbonyl. Furthermore, we sought an explanation for the relatively low reactivity in reductive aminations
of the thienylaldehyde with amines in solution and on solid phase. Based on the crystal structure of T-BAL2, the thienyl-C
(aldehyde) and C–O (aldehyde) bond lengths were applied as measures for the electron-deficiency (electrophilicity) of the
aldehyde and compared to similar bond lengths found in previously reported formylated homo- and hetero-aromatic systems, which
show significantly higher reactivity towards imine formation. The bond lengths found in the present structure are in accordance
with normal C–C single bond and C–O double bond lengths. The high similarity in aldehyde bond lengths in the present system
and in the reported systems indicates similar electron distribution in these systems. The lower reactivity of the present
system may therefore not be attributed to electronic factors. 相似文献