共查询到20条相似文献,搜索用时 14 毫秒
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Dr. Joy Debnath Prof. Swagata Dasgupta Prof. Tanmaya Pathak 《Chemistry (Weinheim an der Bergstrasse, Germany)》2012,18(6):1618-1627
Ribonuclease A (RNase A) serves as a convenient model enzyme in the identification and development of inhibitors of proteins that are members of the ribonuclease superfamily. This is principally because the biological activity of these proteins, such as angiogenin, is linked to their catalytic ribonucleolytic activity. In an attempt to inhibit the biological activity of angiogenin, which involves new blood vessel formation, we employed different dinucleosides with varied non‐natural backbones. These compounds were synthesized by coupling aminonucleosides with dicarboxylic acids and amino‐ and carboxynucleosides with an amino acid. These molecules show competitive inhibition with inhibition constant (Ki) values of (59±3) and (155±5) μM for RNase A. The compounds were also found to inhibit angiogenin in a competitive fashion with corresponding Ki values in the micromolar range. The presence of an additional polar group attached to the backbone of dinucleosides was found to be responsible for the tight binding with both proteins. The specificity of different ribonucleolytic subsites were found to be altered because of the incorporation of a non‐natural backbone in between the two nucleosidic moieties. In spite of the replacement of the phosphate group by non‐natural linkers, these molecules were found to selectively interact with the ribonucleolytic site residues of angiogenin, whereas the cell binding site and nuclear translocation site residues remain unperturbed. Docked conformations of the synthesized compounds with RNase A and angiogenin suggest a binding preference for the thymine–adenine pair over the thymine–thymine pair. 相似文献
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Cover Picture: Chemistry of Lipid A: At the Heart of Innate Immunity (Chem. Eur. J. 2/2015) 下载免费PDF全文
Prof. Antonio Molinaro Prof. Otto Holst Dr. Flaviana Di Lorenzo Dr. Maire Callaghan Dr. Alessandra Nurisso Dr. Gerardino D'Errico Dr. Alla Zamyatina Prof. Francesco Peri Dr. Rita Berisio Prof. Roman Jerala Prof. Jesús Jiménez‐Barbero Dr. Alba Silipo Prof. Sonsoles Martín‐Santamaría 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(2):473-473
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Cover Picture: A Modular Synthesis of Conformationally Preorganised Extended β‐Strand Peptidomimetics (Chem. Eur. J. 42/2015) 下载免费PDF全文
Dr. Tohru Yamashita Dr. Peter C. Knipe Dr. Nathalie Busschaert Dr. Sam Thompson Prof. Dr. Andrew D. Hamilton 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(42):14653-14653
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《Chemistry (Weinheim an der Bergstrasse, Germany)》2007,13(19):5317-5317
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Monica Melegari Dr. Michele Suman Dr. Laura Pirondini Dr. Davide Moiani Dr. Chiara Massera Dr. Franco Ugozzoli Prof. Elina Kalenius Dr. Pirjo Vainiotalo Prof. Jean‐Christophe Mulatier Jean‐Pierre Dutasta Dr. Enrico Dalcanale Prof. 《Chemistry (Weinheim an der Bergstrasse, Germany)》2008,14(19):5699-5699