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排序方式: 共有150条查询结果,搜索用时 46 毫秒
141.
Gil Fridkin Shai Rahimipour Nurit Ben-Aroya Aviva Kapitkovsky Susanna Di-Segni Masha Rosenberg Irina Kustanovich Yitzhak Koch Chaim Gilon Mati Fridkin 《Journal of peptide science》2006,12(2):106-115
Five linear analogs of GnRH containing a p-aminophenylalanine (Pap) residue in their sequence and their six corresponding azo-bridged cyclic derivatives were synthesized. The precyclic peptides were prepared on solid-support, while azo-cyclization was performed in solution by diazotization of the p-aminophenylalanine residue followed by intramolecular coupling of the formed diazo salt with either tyrosine or histidine side chains present in the sequence. All peptides were examined for their binding ability to the GnRH receptor expressed on rat pituitary membranes and for their LH-release activity from dispersed rat pituitary cells. Linear analogs 1 i.e [Pap(5)] GnRH and 3, i.e. [Tyr(3), Pap(5)] GnRH, were found to bind to the GnRH receptors only slightly less avidly than native GnRH. Their cyclization, however, led to a marked reduction in the binding capacity, i.e. from IC(50) of 10(-9) M to the 10(-7) M range, and in biopotency, i.e. LH-release. All other linear and cyclic peptides were found to bind selectively to the GnRH receptor only in the low microM range. Only peptide 1 was found comparable to native GnRH in respect to LH-release activity and thus may potentially be a good agonist of the parent peptide. Peptides 1-4, the most potent GnRH receptor binders, were examined for their conformational properties using CD. Cyclic-azo peptides 2 and 4 were further evaluated by NMR spectroscopy in solution combined with molecular modeling. The structural information obtained explains in part the GnRH-like biological activity observed. 相似文献
142.
Eran J. Yavin Oren Rosen Michel Pontet Enid G. Shephard Mati Fridkin 《Letters in Peptide Science》1995,2(1):7-16
Summary Proteolysis of human C-reactive protein (CRP) by lysosomal enzymes derived from human neutrophils is shown to yield short peptides capable of modulating the production of superoxide ions by stimulated human neutrophils. Thus, fractionation of trichloroacetic acid-soluble digestion mixtures by HPLC yielded the following peptides: Ser-Tyr (1), Gly-Tyr (2), Phe-Glu-Val-Pro-Glu-Val-Thr (3), Trp-Asp-Phe-Val (4), Asn-Met-Trp-Asp-Phe-Val (5) and Gln-Leu-Trp-Pro (6). These peptides, corresponding to CRP sequences 18–19, 48–49 and/or 72–73, 84–90, 162–165, 160–165 and 203–206, respectively, have been synthesized and peptides 2, 3 and in particular peptide 6 were found to significantly inhibit neutrophilic function. The results suggest that CRP-derived peptides may be capable of regulating superoxide ion production by neutrophils in vivo during the acute phase response as part of a complex protective mechanism. 相似文献
143.
The synthesis of poly(L -leucyl-L -ornithyl-L -leucine) and of poly(L -leucyl-L -arginyl-L -leucine) is reported. The antibacterial action of the two copolymers was checked by growth inhibition experiments on Staphylococcus aureus. The activity was found to be identical with that of a disordered 1:1 copolymer of L -ornithine and L -leucine. Conversion of 75% of the ornithine residues to arginine had no effect on the antibacterial activity. 相似文献
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R Levy Z Kain C Chaimovitz M Fridkin S Segal M Alkan 《Journal of biological regulators and homeostatic agents》1989,3(2):71-78
A major complication of continuous ambulatory peritoneal dialysis (CAPD) is peritonitis caused by Candida albicans. Increasing the activity of the peritoneal macrophages, the predominant cell type found in the peritoneal cavity, may be a promising treatment for this infection. Tuftsin was found to increase thioglycollate-elicited mouse peritoneal macrophage activity. 2x10(-7) M tuftsin enhanced two-fold cell association with radiolabelled candida, superoxide aniom production, and killing activity. Thus, a model consisting of mice undergoing peritoneal dialysis was developed in order to study the use of tuftsin as a therapeutic drug against peritoneal candidiasis. Administration of tuftsin (50 micrograms/mouse) before candidiasis induction with a lethal dose of candida (7x10(8) candida per mouse) improved mouse survival up to 70%, compared with 10% in the control group. The potential of tuftsin as a treatment for candidiasis was shown when the infection was induced with a sublethal dose of candida. Daily intraperitoneal injections of tuftsin (50 micrograms) to the sublethally infected mice caused a significant decrease in the number of candida recovered from the peritoneal cavity and from the blood (from 700 +/- 190 to 110 +/- 26 CFU/ml and from 100 +/- 26 CFU/ml to 17 +/- 8 CFU/ml, respectively). In addition, a larger number of peritoneal macrophages with greater phagocytic and killing activity were found in the tuftsin-treated mice. The effect of tuftsin may promote its potential use in the therapy of peritonitis in patients undergoing chronic peritoneal dialysis. 相似文献
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149.
Y Stabinsky M Fridkin V Zakuth Z Spirer 《International journal of peptide and protein research》1978,12(3):130-138
The cyclization, under alkaline conditions, of N-benzyloxycarbonyl-L-threonine and of N-benzyloxycarbonyl-L-serine to produce 5-methyl-2-oxo-oxazolidine-4-carboxylic acid (O = C Thr1 and 2-oxo-oxazolidine-4-carboxylic acid (O = C Ser), respectively, was investigated and found to be efficient and racemization-free. Similar was the cyclization which accompanied the basic hydrolysis of N-benzyl-oxycarbonyl-L-threonyl-L-phenylalanine methyl ester and of N-benzyloxy-carbonyl-L-seryl-DL-valine ethyl ester, and which resulted in the formation of L - O = C Thr-L-Phe and L - O = C Ser-DL-Val, respectively. The reaction was applied to the synthesis of [O = C Thr1] tuftsin, an active analog of the phagocytosis stimulating peptide tuftsin. A new synthetic route to tuftsin is also described. 相似文献
150.
Lea Eisenbach Ofer Mandelboim Erez Bar-Haim Lior Carmon Hernan Copcow Khaled El-Shami Adrian Paz Dan Popovic Ezra Vadai Esther Tzehoval Michael Feldman Mati Fridkin 《Letters in Peptide Science》1998,5(5-6):323-328
Cytotoxic T-lymphocytes (CTLs) kill abnormal cells. CTLs recognize major histocompatibility complex class I molecules in complex with peptides derived from relevant antigens. The identification of tumor associated antigen peptides enabled the design of anti-tumor and anti-metastatic vaccines in a murine lung carcinoma. 相似文献