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参考文献:新型环肽作为促凋亡剂的开发
标题:新型环肽作为促凋亡剂的开发
摘要:我们最近发现紫杉醇可作为内源蛋白nur77的拟肽模拟物,激发了两种肽(pep1和pep2)的设计,从而再现了紫杉醇对bcl-2和微管蛋白的作用,证明了紫杉醇的拟肽性质.从这些肽命中开始,我们在本文中描述了与pep2结构相关的线性和环状肽的合成和生物学研究.虽然线性肽(图2A,2B,3A中,B,4,图6A-F)在基于细胞的测定中发现无活性的,生物分析表明大多数的环肽(的促凋亡作用5A-G).细胞渗透率为5A(以及2A,B通过共聚焦显微镜分析评估hl60细胞上的).对一组白血病细胞系(hl60,Jurkat,Mec,Ebvb)和实体瘤细胞系(乳腺癌mcf-7细胞,人黑素瘤a375和501Mel细胞以及鼠类黑素瘤b16F1细胞)的进一步细胞研究证实了促凋亡环肽的作用.细胞周期分析显示,用5A,5C,5D或5F处理导致sub-G 0 / G 1峰中的细胞数量增加.在体外评估了最有希望的化合物与
DOI:10.1016/j.Ejmech.2016.04.001

专利信息

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-2012095211-A1
优先权日:2010-09-22
标 题 :Substituted proline inhibitors of hepatitis c virus replication
发明人：BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D
权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC
摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.

专利号:US-7651997-B2
优先权日:2000-04-07
标 题 :Deoxo-proline-containing tamandarin and didemnin analogs, dehydro-proline-containing tamandarin and didemnin analogs, and methods of making and using them
发明人：JOULLIE MADELEINE M; LIANG BO; DING XIAOBIN
权利人:UNIV PENNSYLVANIA
摘要:The present invention relates to tamandarin and didemnin analogs which have a deoxo-proline residue or a dehydro-proline residue in their structure. These analogs are useful as anti-cancer agents and for other purposes. Methods of making these analogs and methods of using them as inhibitors of protein synthesis, cell growth, and tumorigenesis and as enhancers of apoptosis are also provided.