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Stefania Neiva Lavorato Policarpo Ademar Sales Júnior Silvane Maria Fonseca Murta Alvaro José Romanha Ricardo José Alves/ 《Memórias do Instituto Oswaldo Cruz》2015,110(4):566-568
We describe herein the antitrypanosomal activity of 20 novel
1,3-bis(aryloxy)propan-2-amine derivatives. Compounds 2, 4, 6, 12, 15, 16 and 19 were
significantly active against amastigote and trypomastigote forms, with half maximal
inhibitory concentrationvalues in the range of 6-18 µM. In the cytotoxicity tests
against L929 cells, only compound 4 presented selectivity index value above 10,
indicating low toxicity. 相似文献
176.
Eric?R. Henry Andrea Mozzarelli Cristiano Viappiani Stefania Abbruzzetti Stefano Bettati Luca Ronda Stefano Bruno William?A. Eaton 《Biophysical journal》2015,109(6):1264-1272
Trapping quaternary structures of hemoglobin in single crystals or by encapsulation in silica gels has provided a demanding set of data to test statistical mechanical models of allostery. In this work, we compare the results of those experiments with predictions of the four major allosteric models for hemoglobin: the quaternary two-state model of Monod, Wyman, and Changeux; the tertiary two-state model of Henry et al., which is the simplest extension of the Monod-Wyman-Changeux model to include pre-equilibria of tertiary as well as quaternary conformations; the structure-based model of Szabo and Karplus; and the modification of the latter model by Lee and Karplus. We show that only the tertiary two-state model can provide a near quantitative explanation of the single-crystal and gel experimental results. 相似文献
177.
Kazuo Yamasaki Takashi Daiho Stefania Danko Hiroshi Suzuki 《The Journal of biological chemistry》2015,290(46):27868-27879
The mechanism whereby events in and around the catalytic site/head of Ca2+-ATPase effect Ca2+ release to the lumen from the transmembrane helices remains elusive. We developed a method to determine deoccluded bound Ca2+ by taking advantage of its rapid occlusion upon formation of E1PCa2 and of stabilization afforded by a high concentration of Ca2+. The assay is applicable to minute amounts of Ca2+-ATPase expressed in COS-1 cells. It was validated by measuring the Ca2+ binding properties of unphosphorylated Ca2+-ATPase. The method was then applied to the isomerization of the phosphorylated intermediate associated with the Ca2+ release process E1PCa2 → E2PCa2 → E2P + 2Ca2+. In the wild type, Ca2+ release occurs concomitantly with EP isomerization fitting with rate-limiting isomerization (E1PCa2 → E2PCa2) followed by very rapid Ca2+ release. In contrast, with alanine mutants of Leu119 and Tyr122 on the cytoplasmic part of the second transmembrane helix (M2) and Ile179 on the A domain, Ca2+ release in 10 μm Ca2+ lags EP isomerization, indicating the presence of a transient E2P state with bound Ca2+. The results suggest that these residues function in Ca2+ affinity reduction in E2P, likely via a structural rearrangement at the cytoplasmic part of M2 and a resulting association with the A and P domains, therefore leading to Ca2+ release. 相似文献
178.
Gene Expression Changes in Progression of Cervical Neoplasia Revealed by Microarray Analysis of Cervical Neoplastic Keratinocytes
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179.
Francesco Fazio Stefania Casella Claudia Giannetto Elisabetta Giudice Giuseppe Piccione 《Experimental Animals》2015,64(1):19-24
Haptoglobin (Hp), serum amyloid A (SAA), C-reactive protein (CRP), white blood cells
(WBC), reactive oxygen metabolites (ROMs), the antioxidant barrier (Oxy-adsorbent) and
thiol groups of plasma compounds (SHp) were measured in ten dogs that had been transported
a distance of about 230 km within 2 h (experimental group) and in ten dogs that had not
been subjected to road transportation (control group). Blood was collected via cephalic
venipuncture before road transportation (T0), after road transportation (T1), and more
than 6 (T6) and 24 (T24) hours after road transportation in the experimental group (Group
A) and at the same time points in the control group (Group B). The GLM (general linear
model) Repeated Measures procedure showed a significant difference between the two groups
(P<0.0001) and a significant rise (P<0.0001) in
the concentrations of Hp, SAA, CRP, WBC, ROMs, Oxy-adsorbent and SHp after road
transportation in Group A, underlining that physiological and homeostatic mechanisms are
modified differently at various sampling times. 相似文献
180.
Cameron C Scott Stefania Vossio Fabrizio Vacca Berend Snijder Jorge Larios Olivier Schaad Nicolas Guex Dmitry Kuznetsov Olivier Martin Marc Chambon Gerardo Turcatti Lucas Pelkmans Jean Gruenberg 《EMBO reports》2015,16(6):741-752
The Wnt pathway, which controls crucial steps of the development and differentiation programs, has been proposed to influence lipid storage and homeostasis. In this paper, using an unbiased strategy based on high-content genome-wide RNAi screens that monitored lipid distribution and amounts, we find that Wnt3a regulates cellular cholesterol. We show that Wnt3a stimulates the production of lipid droplets and that this stimulation strictly depends on endocytosed, LDL-derived cholesterol and on functional early and late endosomes. We also show that Wnt signaling itself controls cholesterol endocytosis and flux along the endosomal pathway, which in turn modulates cellular lipid homeostasis. These results underscore the importance of endosome functions for LD formation and reveal a previously unknown regulatory mechanism of the cellular programs controlling lipid storage and endosome transport under the control of Wnt signaling. 相似文献