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PEPTIDES HAVING CYCLIC STRUCTURES AND EXERTING P53 PROTEIN ACTIVTY-RESTORING EFFECT ON P53 PROTEIN MUTANTS

机译：具有环结构的肽并发挥P53蛋白活性恢复对P53蛋白突变的影响

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摘要

Peptides having cyclic structures represented by the following general formula(I): R¹(X¹)ⁿ¹(X²)ⁿ²(X³)ⁿ³(X⁴)ⁿ⁴(X⁵)ⁿ⁵(X⁶)ⁿ⁶(X⁷)ⁿ⁷ (X⁸)ⁿ⁸(X⁹)ⁿ⁹(X¹⁰)ⁿ¹⁰(x¹¹)n¹¹(X¹²)ⁿ¹²(X¹³)ⁿ¹³(X¹⁴)ⁿ¹⁴(X¹⁵)ⁿ¹⁵(X¹⁶)ⁿ¹⁶(X¹⁷)ⁿ¹⁷R2 and exerting the effect of restoring a P53 protein activity on P53 protein mutants or pharmacologically acceptable salts thereof. In said formula (I) Xⁱ means an arbitrary member selected from among X¹ to X¹⁷ while nⁱ means an arbitrary member selected from among n¹ to n¹⁷ (provided that i is an integer of from 1 to 17), then Xⁱ represents an amino acid residue or an organic acid residue; a functional group in a residue X^p selected among X¹ to X¹¹ (provided that p is an integer of from 1 to 11) and a functional group X^q selected from among X⁸ to X¹⁷ (provided that q is an integer of from 8 to 17 and larger than p) form a cyclic structure having a crosslinkage selected from among S-S, S-CH₂-S, S-CH₂-C₆H₄,-CH₂-S, S-CH₂-CO, CO-NH, NH-CO, O-CO or CO-O; R¹ represents optionally substituted alkanoyl, etc.; and R² represents optionally substitued alkoxy, etc.

机译：具有以下通式（I）表示的环状结构的肽：R ^{1 （X ^{1 ）^{n1 （X ^{2 ）^{n2 （X ^{3 ）^{n3 （X ^{4 ）^{n4 （ X ^{5 ）^{n5 （X ^{6 ）^{n6 （X ^{7 ）^{n7 （X ^{8 ）^{n8 （X ^{9 ）^{n9 （X ^{10 ）^{n10 （x ^{11 ）n ^{11 （X ^{12 ）^{n12 （X ^{13 ）^{n13 （X ^{14 ）^{n14 （X ^{15 ）^{n15 （X ^{16 ）^{n16 （X ^{17 ）^{n17 R2并发挥作用恢复P53蛋白活性对P53蛋白突变体或其药理学上可接受的盐的作用。在上述式（I）中，X ^{i 表示从X ^{1 至X ^{17 中选择的任意成员，而n ^{i 表示从n ^{1 到n ^{17 中选择的任意成员（假设i是1到17的整数），则X ^{i 代表氨基酸残基或有机酸残基;从X ^{1 至X ^{11 中选择的残基X ^{p 中的官能团（假设p为1至11的整数），并且从X ^{8 到X ^{17 中选择的官能团X ^{q （前提是q是8到17的整数并且大于p ）形成具有从SS，S-CH _{2 -S，S-CH _{2 -C _{6 H < Sub> 4 ，-CH _{2 -S，S-CH _{2 -CO，CO-NH，NH-CO，O-CO或CO-O ; R ^{1 表示任选取代的烷酰基等。 R ^{2 代表可选被取代的烷氧基等。}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}

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公开/公告号EP0989136A4

专利类型
公开/公告日2002-10-09

原文格式PDF
申请/专利权人 KYOWA HAKKO KOGYO CO. LTD.;
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申请/专利号EP19980919612
发明设计人 YOSHIDA TETSUO;ANAZAWA HIDEHARU;SHIBATA KENJI;SHINKAI AKEO;YAMASAKI MOTOO;MIZUKAMI TAMIO;
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申请日1998-05-15
分类号C07K14/82;
国家 EP
入库时间 2022-08-22 00:35:15

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