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Nuclear magnetic resonance spectroscopy has been used to investigate the solution conformation of tuftsin, threonyllysylprolylarginine, as well as a pentapeptide inhibitor of tuftsin, threonyllysylprolylprolylarginine. Both proton and carbon-13 studies were performed. In water, neither peptide gives evidence of a preferred conformation. In dimethyl-d6 sulfoxide, tuftsin appears to prefer a particular conformation, but the inhibitor does not. The conformation of tuftsin is one in which the amide NH proton of arginine is solvent shielded. The conformation does not, however, appear to be such that a normal 4 leads to 1 beta turn exists. 相似文献
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Lizette Auezova Fadia Najjar Olga Selivanova Elie Hajj Moussa Mona Diab Assaf 《Journal of applied phycology》2013,25(4):1189-1196
The present study aims to investigate the levels of polyphenols and antioxidant activity in one of the most important commercial species of seaweeds in Kamchatka, an edible brown seaweed Saccharina bongardiana. Six extracts of S. bongardiana, acetone, methanol, ethanol, and the respective 70 % aqueous solutions, were assessed for total phenol content in order to determine the most efficient extracting solvent. The total phenol content was measured by the Folin–Ciocalteu method and expressed as phloroglucinol equivalents (PGE). The antioxidant tests used were 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay, linoleic acid-β carotene oxidation inhibiting assay, and Fe2+ ion chelating method. Higher phenolic contents were obtained using aqueous organic solvents, as compared to the respective absolute solvents; 70 % acetone was found to be the most efficient solvent (1.039 mg PGE 100 mg?1 dry algal powder). High significant correlations were noted between total phenol content and the tested antioxidant activities; so the aqueous organic extracts exhibited the highest antioxidant activities versus DPPH radicals (EC50 values of 0.6–1.1 mg dry weight (DW) mL?1), linoleic acid-β carotene oxidation (74–78 % at 0.8 mg DW mL?1), as well as ferrous ions (EC50 values of 5.0–7.9 mg DW mL?1). Some methodological recommendations regarding the assays used and the expression of results are proposed. 相似文献
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Zeynep Eroglu Sheri L. Holmen Qing Chen Nikhil I. Khushalani Ravi Amaravadi Reena Thomas Kamran A. Ahmed Hussein Tawbi Sunandana Chandra Joseph Markowitz Inna Smalley James K. C. Liu Yian Ann Chen Yana G. Najjar Florian A. Karreth Daniel Abate‐Daga Isabella C. Glitza Jeffrey A. Sosman Vernon K. Sondak Marcus Bosenberg Meenhard Herlyn Michael B. Atkins Harriet Kluger Kim Margolin Peter A. Forsyth Michael A. Davies Keiran S. M. Smalley 《Pigment cell & melanoma research》2019,32(3):458-469
In February 2018, the Melanoma Research Foundation and the Moffitt Cancer Center hosted the Second Summit on Melanoma Central Nervous System (CNS) Metastases in Tampa, Florida. In this white paper, we outline the current status of basic science, translational, and clinical research into melanoma brain metastasis development and therapeutic management. We further outline the important challenges that remain for the field and the critical barriers that need to be overcome for continued progress to be made in this clinically difficult area. 相似文献
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Kelsey H. Fisher-Wellman James A. Draper Michael T. Davidson Ashley S. Williams Tara M. Narowski Dorothy H. Slentz Olga R. Ilkayeva Robert D. Stevens Gregory R. Wagner Rami Najjar Mathew D. Hirschey J. Will Thompson David P. Olson Daniel P. Kelly Timothy R. Koves Paul A. Grimsrud Deborah M. Muoio 《Cell reports》2019,26(6):1557-1572.e8
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Robin Bonomi Uday Mukhopadhyay Aleksandr Shavrin Hsien-Hsien Yeh Anjoy Majhi Sajeewa W. Dewage Amer Najjar Xin Lu G. Andrés Cisneros William P. Tong Mian M. Alauddin Ren-Shuan Liu Thomas J. Mangner Nashaat Turkman Juri G. Gelovani 《PloS one》2015,10(8)
Histone deacetylases (HDAC’s) became increasingly important targets for therapy of various diseases, resulting in a pressing need to develop HDAC class- and isoform-selective inhibitors. Class IIa deacetylases possess only minimal deacetylase activity against acetylated histones, but have several other client proteins as substrates through which they participate in epigenetic regulation. Herein, we report the radiosyntheses of the second generation of HDAC class IIa–specific radiotracers: 6-(di-fluoroacetamido)-1-hexanoicanilide (DFAHA) and 6-(tri-fluoroacetamido)-1-hexanoicanilide ([18F]-TFAHA). The selectivity of these radiotracer substrates to HDAC class IIa enzymes was assessed in vitro, in a panel of recombinant HDACs, and in vivo using PET/CT imaging in rats. [18F]TFAHA showed significantly higher selectivity for HDAC class IIa enzymes, as compared to [18F]DFAHA and previously reported [18F]FAHA. PET imaging with [18F]TFAHA can be used to visualize and quantify spatial distribution and magnitude of HDAC class IIa expression-activity in different organs and tissues in vivo. Furthermore, PET imaging with [18F]TFAHA may advance the understanding of HDACs class IIa mediated epigenetic regulation of normal and pathophysiological processes, and facilitate the development of novel HDAC class IIa-specific inhibitors for therapy of different diseases. 相似文献
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