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【求助】关于化学名称pnu类化合物的求助已有4人参与
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| 比如化学名称pnu109112代表一特定结构的化合物，其中pnu是什么意思？怎么据此查找其结构式？多谢 |
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2楼2010-10-14 13:37:07
gdqabc(金币+1):欢迎讨论 2010-10-24 08:51:15
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3楼2010-10-15 11:05:10
4楼2010-10-15 15:23:47
nkbeholder
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5楼2010-10-15 15:55:24
6楼2010-10-15 17:08:45
leonumn
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7楼2010-10-22 09:43:15
leonumn
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8楼2010-10-22 09:46:22
leonumn
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gdqabc(金币+1):欢迎讨论 2010-10-24 08:52:02
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Activated Sulfonamides are Cleaved by Glutathione-S-Transferases Kenneth A. Koeplinger1, Zhiyang Zhao1,2, Tillie Peterson1, Joseph W. Leone1, Francis S. Schwende2, Robert L. Heinrikson1 and Alfredo G. Tomasselli1 + Author Affiliations 1Protein Science (K.A.K., T.P., J.W.L., R.L.H., A.G.T.) and2Drug Metabolism (Z.Z., F.S.S.), Pharmacia & Upjohn, Incorporated, Kalamazoo, Michigan Next SectionAbstract In preclinical pharmacokinetic studies and in in vitro rat, dog, and human primary hepatocyte incubations, the sulfonamide (-NH-SO2-) bond of a potent inhibitor of the HIV-1 protease containing the p-cyanopyridinyl moiety (PNU-109112), undergoes metabolic cleavage to form the corresponding amine metabolite (PNU-143070). Strikingly, a compound, PNU-140690, obtained by substituting the cyanopyridinyl group of PNU-109112 with a trifluoropyridinyl moiety, was stable under the same in vivo and in vitro conditions used for PNU-109112. The apparent “sulfonamidase activity” present in liver was localized to the cytosolic fraction and shown to be an enzyme-mediated reaction requiring reduced glutathione (GSH). The enzyme responsible was purified in a single step on a GSH immobilized gel and was identified as glutathione-S-transferase (GST) by sequence analysis of peptides obtained by tryptic digestion of the purified protein. Moreover, a mixture of GST isoenzymes purified from rat liver, and three recombinant human GST isoforms, A1–1, M1–1, and P1–1, were active toward PNU-109112 sulfonamide cleavage; the three isoforms exhibited differential rates of PNU-109112 cleavage, demonstrating isoenzyme selectivity. |
9楼2010-10-22 09:46:54
leonumn
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gdqabc(金币+1):欢迎讨论 2010-10-24 08:52:08
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Targeting the HIV-protease in AIDS therapy: a current clinical perspective1 References and further reading may be available for this article. To view references and further reading you must purchase this article. Alfredo G. Tomasselli and Robert L. Heinrikson2 Department of Protein Science, Pharmacia and Upjohn, Kalamazoo, MI 49001, USA Received 1 November 1999; accepted 1 December 1999. Available online 8 March 2000. Abstract This review deals with clinical applications of compounds that inhibit the action of the protease encoded within the genome of human immunodeficiency virus (HIV). The HIV-protease is essential for viral maturation and represents an important therapeutic target in the fight against AIDS. Following a brief overview of the enzyme structure and function, the article focuses on a number of peptide and non-peptide based HIV-protease inhibitors that are in current clinical use. These drugs are discussed both with respect to their efficacy in treatment of AIDS, and to problems related to insurgence of viral resistance and side effects seen to date in patient populations. |
10楼2010-10-22 09:47:13