- Synthesis of the Tripeptides Tyr-Thr-Lys Phosphorylated with Isopropyl Methyl- and (Deuteromethyl)phosphonochloridates as Reference Standards for the Analysis of Biomedical Samples
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A procedure for the phosphorylation of the tripeptide Tyr-Thr-Lys with isopropyl methyl- or (deuteromethyl)phosphonochloridate is developed. The phosphorylated tripeptides are intended for use as reference standards in the analysis of blood samples of people suspected to have been exposed to acetylcholinesterase inhibitors. Conditions of hromatographic separation and purification of the synthesized compounds are determined and optimized, which ensures the preparation of high-purity phosphorylated tripeptides.
- Rodin,Baygildiev,Krylov,Osipov,Krylov,Yashkir,Rybalchenko
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p. 2103 - 2107
(2019/11/29)
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- A new class of β-carboline alkaloid-peptide conjugates with therapeutic efficacy in acute limb ischemia/reperfusion injury
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We describe a novel class of β-carboline alkaloid-peptide conjugates that possess both free radical scavenging and thrombolytic activity. These conjugates demonstrate therapeutic efficacy in a rat arterial thrombosis assay, as well as free radical scavenging capacity as evaluated in a PC12 cell survival assay. Our results indicate that β-carboline alkaloid-peptide conjugate 26a exerts a significant protective effect against local and remote organ injury induced by limb I/R injury in the rat.
- Bi, Wei,Bi, Yue,Xue, Ping,Zhang, Yanrong,Gao, Xiang,Wang, Zhibo,Li, Meng,Baudy-Floc'H, Michle,Ngerebara, Nathaniel,Michael Gibson,Bi, Lanrong
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experimental part
p. 1453 - 1462
(2011/05/06)
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- A class of novel carboline intercalators: Their synthesis, in vitro anti-proliferation, in vivo anti-tumor action, and 3D QSAR analysis
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Based on DOCK scores 18 N-(3-benzyloxycarbonylcarboline-1-yl)ethylamino acid benzylesters (6a-r) were synthesized as anti-tumor agents. Their IC 50 values against five human carcinoma cell lines ranged from 11.1 μM to more than 100 μM. The in vivo assay identified five derivatives of them had no anti-tumor action, the anti-tumor activity of nine derivatives of them equaled that of cytarabine, and the anti-tumor activity of three derivatives of them was higher than that of cytarabine. The UV and fluorescence spectra, as well as the relative viscosity and melting temperature measurements of calf thymus DNA (CT DNA) with and without the representative compound suggested that DNA intercalation could be their action mechanism. The 3D QSAR analysis of N-(3-benzyloxycarbonylcarboline-1-yl)ethylamino acid benzylesters (6a-r) revealed that their in vivo anti-tumor activity significantly depends on the molecular electrostatic and steric fields of the side chain of the amino acid residue.
- Wu, Jianhui,Li, Chunyu,Zhao, Ming,Wang, Wenjing,Wang, Yuji,Peng, Shiqi
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experimental part
p. 6220 - 6229
(2010/10/04)
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- Synthesis and biological activity of nitronyl nitroxide containing peptides
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[1-(1′,3′-Dioxyl-4′,4′,5′, 5′-tetramethyldihydroimidazol-2-yl)-phenyl-4-yl]oxyacetic acid (4), a nitronyl nitroxide, and its peptide derivatives, N-[1-(1′,3′-dioxyl- 4′,4′,5′,5′-tetramethyldihydroimidazol-2-yl) -phenyl-4-yl]oxyacetyl-ARPAK (9a), -GRPAK (9b), and -QRPAK (9c), were synthesized and characterized. Judging from the results of electron spin resonance analysis, the newly synthesized nitronyl nitroxide containing peptides, 9a, 9b, and 9c, demonstrated the characteristics of free radicals. The free radical scavenging activities of 9a, 9b, and 9c were assessed using in vitro free radical scavenging tests. The thrombolysis effect of 9a, 9b, and 9c was evaluated using an euglobulin clot lysis test, a fibrinolytic lysis test, and in vivo thrombolysis tests. Results indicated that these nitronyl nitroxide containing peptides possessed both free radical scavenging activity and thrombolytic activity.
- Zhao, Ming,Liu, Junling,Wang, Chao,Wang, Lili,Liu, Hu,Peng, Shiqi
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p. 4285 - 4292
(2007/10/03)
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- Granulopoiesis Inhibiting Factor: Synthesis and Biological Activity
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Three schemes of synthesis for pentapeptide Glp-Glu-Asp-Cys-Lys-OH were compared.Acetamidomethyl protection was used for the mercapto group of cysteine.For the same purpose, cystine was used as the starting compound for synthesis.The optimal method was shown to be the solid phase method with S-acetamidomethyl cysteine protection that can be removed by mercuric acetate before the cleavage of a peptide from a polymer.The stabilized peptide inhibits proliferation of bone marrow cells of patients with chronic myeloleukemia 5- to 20-fold and has a less pronounced effect (up to 2-fold inhibition) on peripheral blood cells.Thus, its application for the therapy of hemoblastoses is promising. Key words: granulopoiesis inhibiting factor, solid phase peptide synthesis, cysteine-containing pentapeptide
- Kulikov, S. V.,Leonova, E. B.,Kalinina, N. M.,Samartsev, M. A.,Bubnova, L. N.,et al.
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p. 362 - 369
(2007/10/02)
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- Method for the preparation of GYK-DTPA
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Disclosed herein is a novel method for preparing a DPTA tripeptide-chelator. In particular, a method for preparing GYK-DTPA is described. The method disclosed herein is an improvement over the known methods of preparation based on the cost and labor savings of the present invention. The present invention utilizes t-butyloxycarbonyl (Boc) protecting groups to facilitate the polypeptide-chelator production.
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