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81.
Stabilized α-helices and nonpeptidic helix mimetics have emerged as powerful molecular scaffolds for the discovery of protein-protein interaction inhibitors. Protein-protein interactions often involve large contact areas, which are often difficult for small molecules to target with high specificity. The hypothesis behind the design of stabilized helices and helix mimetics is that these medium-sized molecules may pursue their targets with higher specificity because of a larger number of contacts. This protocol describes an optimized synthetic strategy for the preparation of stabilized α-helices that feature a carbon-carbon linkage in place of the characteristic N-terminal main-chain hydrogen bond of canonical helices. Formation of the carbon-carbon bond is enabled by a microwave-assisted ring-closing metathesis reaction between two terminal olefins on the peptide chain. The outlined strategy allows the synthesis and purification of a hydrogen bond surrogate (HBS) α-helix in ~ 1 week. 相似文献
82.
Estimates of (co)variance components and genetic parameters for body weights and first greasy fleece weight in Bharat Merino sheep 总被引:2,自引:0,他引:2
Gowane GR Chopra A Prince LL Paswan C Arora AL 《Animal : an international journal of animal bioscience》2010,4(3):425-431
(Co)variance components and genetic parameters of weight at birth (BWT), weaning (3WT), 6, 9 and 12 months of age (6WT, 9WT and 12WT, respectively) and first greasy fleece weight (GFW) of Bharat Merino sheep, maintained at Central Sheep and Wool Research Institute, Avikanagar, Rajasthan, India, were estimated by restricted maximum likelihood, fitting six animal models with various combinations of direct and maternal effects. Data were collected over a period of 10 years (1998 to 2007). A log-likelihood ratio test was used to select the most appropriate univariate model for each trait, which was subsequently used in bivariate analysis. Heritability estimates for BWT, 3WT, 6WT, 9WT and 12WT and first GFW were 0.05 ± 0.03, 0.04 ± 0.02, 0.00, 0.03 ± 0.03, 0.09 ± 0.05 and 0.05 ± 0.03, respectively. There was no evidence for the maternal genetic effect on the traits under study. Maternal permanent environmental effect contributed 19% for BWT and 6% to 11% from 3WT to 9WT and 11% for first GFW. Maternal permanent environmental effect on the post-3WT was a carryover effect of maternal influences during pre-weaning age. A low rate of genetic progress seems possible in the flock through selection. Direct genetic correlations between body weight traits were positive and ranged from 0.36 between BWT and 6WT to 0.94 between 3WT and 6WT and between 6WT and 12WT. Genetic correlations of 3WT with 6WT, 9WT and 12WT were high and positive (0.94, 0.93 and 0.93, respectively), suggesting that genetic gain in post-3WT will be maintained if selection age is reduced to 3 months. The genetic correlations of GFW with live weights were 0.01, 0.16, 0.18, 0.40 and 0.32 for BWT, 3WT, 6WT, 9WT and 12WT, respectively. Correlations of permanent environmental effects of the dam across different traits were high and positive for all the traits (0.45 to 0.98). 相似文献
83.
Choudhary S Vathulya M Mantri R Arora P Triparty SS 《Plastic and reconstructive surgery》2010,126(6):2297-8; author reply 2298
84.
85.
The study is aimed at exploring the utility of thermoanalytical methods in the solid-state characterization of various crystalline
forms of nevirapine. The different forms obtained by recrystallization of nevirapine from various solvents were identified
using differential scanning calorimetry and thermogravimetric analysis (TGA). The appearance of desolvation peak accompanied
by weight loss in TGA indicated the formation of solvates: hemi-ethanolate (Form I), hemi-acetonitrilate (Form II), hemi-chloroformate
(Form III), hemi-THF solvate (Form IV), mixed hemi-ethanolate hemi-hydrate (Form V), and hemi-toluenate (Form VI). The higher
desolvation temperatures of all the solvates except toluenate than their respective boiling point indicate tighter binding
of solvent. Emphasis has been laid on the determination of heat capacity and heat of solution utilizing microreaction calorimeter
to further distinguish the various forms. The enthalpy of solution (ΔH
sol), an indirect measure of the lattice energy of a solid, was well correlated with the crystallinity of all the solid forms
obtained. The magnitude of ΔH
sol was found to be −14.14 kJ/mol for Form I and −2.83 kJ/mol for Form V in phosphate buffer of pH 2, exhibiting maximum ease
of molecular release from the lattice in Form I. The heat capacity for solvation (ΔC
p) was found to be positive, providing information about the state of solvent molecules in the host lattice. The solubility
and dissolution rate of the forms were also found to be in agreement with their enthalpy of solution. Form (I), being the
most exothermic, was found to be the most soluble of all the forms. 相似文献
86.
Renu Bhardwaj Sukhbir Kaur Pramodh Kumar Nagar Hardesh Kumar Arora 《Plant Growth Regulation》2007,53(1):1-5
Brassinosteroids play an important role in growth and development of plants. They have been reported universally in all the
plants. The present study deals with the presence of these compounds in immature tea seeds. Five brassinosteroids, i.e. 6-deoxo-28-norcathasterone,
6-deoxo-28-norteasterone, 3-dehydro-6-deoxo-28-norteasterone, 6-deoxo-28-nortyphasterol and 6-deoxo-28-norcastasterone have
been isolated and identified by GC–MS. The identified brassinosteroids and their derivatives are active constituents of late
C-6 oxidation pathway, thereby suggesting the biosynthesis of brassinosteroids in tea seeds by late C-6 oxidation pathway. 相似文献
87.
Arora V Cheung HH Plenchette S Micali OC Liston P Korneluk RG 《The Journal of biological chemistry》2007,282(36):26202-26209
X-linked inhibitor of apoptosis (XIAP)-associated factor 1 (XAF1) is a putative tumor suppressor in which expression is significantly reduced in human cancer cell lines and primary tumors. The proapoptotic effects of XAF1 have been attributed to both caspase-dependent and -independent means. In particular, XAF1 reverses the anti-caspase activity of XIAP, a physiological inhibitor of apoptosis. We further investigated the function of XAF1 by examining its relationship with other IAPs. Immunoprecipitation studies indicate that XAF1 binds to XIAP, cIAP1, cIAP2, Livin, TsIAP, and NAIP but not Survivin, an IAP that prevents mitotic catastrophe and in which antiapoptotic activity is exerted through direct XIAP interaction and stabilization. We found that overexpressed XAF1 down-regulates the protein expression of Survivin. Under these conditions, Survivin expression was restored in the presence of the proteasome inhibitor MG132 or a XIAP RING mutant that is defective in ubiquitin-protein isopeptide ligase (E3) activity, suggesting that XAF1 interaction activates E3 activity of XIAP and targets Survivin by direct ubiquitination. In addition, RNA interference targeting endogenous XIAP protected Survivin degradation by XAF1. Furthermore, interferon-beta-mediated XAF1 induction promoted formation of an endogenous XIAP-XAF1-Survivin complex. This complex facilitated Survivin degradation, which was prevented in XAF1(-/-) stable clones. Altogether, our study demonstrates that XAF1 mediates Survivin down-regulation through a complex containing XIAP, supporting dual roles for XAF1 in apoptosis and mitotic catastrophe. 相似文献
88.
Puri SC Amna T Khajuria A Gupta A Arora R Spiteller M Qazi GN 《Acta microbiologica et immunologica Hungarica》2007,54(3):237-260
A novel camptothecin-producing endophytic fungus viz., Entrophospora infrequens was isolated from an important Indian medicinal plant Nothapodytes foetida. The present study reports evaluation ofbioactivities of two novel extracts viz., chloroform (CEEI) and methanolic (MEEI) extracts of Entrophospora infrequens with respect to their immunomodulatory potential in vitro and in vivo (in Balb/c mice). The endophyte E. infrequens was found to synthesize camptothecin, which tested positive in CEEI. The immunomodulatory potential of CEEI and MEEI was compared with standard camptothecin (CPT). Doses of the chloroform extract (CEEI) ranging from 12.5-100 mg/kg body weight, significantly (p < 0.05) stimulated the humoral and cell-mediated immune responses in a dose-dependent manner. MEEI on the other hand significantly (p < 0.05) stimulated the delayed type hypersensitivity (DTH) reaction (by nearly 80%), plaque forming cell (PFC) assay (33%), phagocytic response (38%) and haemagglutination antibody (HA) titre [IgM by 79.07% and IgG by 62.05%] at a dose of 12.5 mg/kg body weight. The present study is the first report of the immunomodulatory potential of this neoteric camptothecin-producing endophyte from Nothapodytes foetida. 相似文献
89.
The Indian pygmy field mouse, Mus terricolor, is a tiny, yet economically and ecologically important crop pest found throughout South-East Asia. There are no systematic reports exploring its reproductive physiology. We report the presence of distinct periods of annual reproductive activity and quiescence in M. terricolor. Body weight in males and females, relative weights of testis, epididymis and seminal vesicle in males, ovarian and uterine weight in females, gonadal histomorphic changes, testicular and ovarian cholesterol, sialic acid in epididymis, fructose in seminal vesicle, uterine protein content, melatonin in males and females, testosterone in males, estradiol, and progesterone in females were studied over a period of three years in both wild-caught and lab-acclimated mice. The number of Graafian follicles and corpora lutea, and plasma estradiol and progesterone, along with relative weights of ovary and uterus in females exhibited a peak in the months of October–January, compared to June. Based on histomorphic and hormonal status, the major reproductively active season is the winter (short-day breeding). There is a brief period of sub-maximal reproductive activity in April. M. terricolor is reproductively inactive in the summer, monsoons, and autumn. The results establish M. terricolor as a seasonal breeder in the field, with interesting implications for pest management. 相似文献
90.
Shikha Verma Anamika Sharma Raj Kumar Charanjit Kaur Anju Arora Raghubir Shah Lata Nain 《Saudi Journal of Biological Sciences》2015,22(3):256-264
Nutrient management practices play a significant role in improving the nutritional quality of tomato. The present study deals with the evaluation of compost prepared using Effective Microorganisms (EM), on antioxidant and defense enzyme activities of Tomato (Lycopersicon esculentum). A field experiment with five treatments (control, chemical fertilizer and EM compost alone and in combination) was conducted in randomized block design. An increment of 31.83% in tomato yield was recorded with the combined use of EM compost and half recommended dose of chemical fertilizers (N50P30K25 + EM compost at the rate of 5 t ha−1). Similarly, fruit quality was improved in terms of lycopene content (35.52%), antioxidant activity (24–63%) and defense enzymes activity (11–54%), in tomatoes in this treatment as compared to the application of recommended dose of fertilizers. Soil microbiological parameters also exhibited an increase of 7–31% in the enzyme activities in this treatment. Significant correlation among fruit quality parameters with soil microbiological activities reveals the positive impact of EM compost which may be adopted as an eco-friendly strategy for production of high quality edible products. 相似文献