首页> 外国专利> SHIGA TOXIN B-SUBUNIT AS A VECTOR FOR TUMOR DIAGNOSIS AND DRUG DELIVERY TO GB3 EXPRESSING TUMORS

SHIGA TOXIN B-SUBUNIT AS A VECTOR FOR TUMOR DIAGNOSIS AND DRUG DELIVERY TO GB3 EXPRESSING TUMORS

机译:SHIGA TOXIN B-SUBUNIT作为肿瘤诊断和药物递送至GB3表达肿瘤的媒介

摘要

The invention relates to new compounds for cancer therapy or diagnosis andmore specifically to the use of a non-toxic B subunit of Shiga toxin mutant asa vector for diagnostic products or drugs in over-expressing Gb3 receptorcells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)- Twherein - STxB is the Shiga Toxin B subunit or a functional equivalentthereof, - Z(n) wehrein n is 0 or 1 and when n is 1, Z is an amino-acidresidue devoidof sulfydryl group, or is a polypeptide, - Cys is the amino-acidresidue for Cysteine, - T is a molecule linked by a covalent bound to the Spart of Cys, selected in a group comprising: . agents for in vivo diagnosis, .cytotoxic agents, . prodrugs, or . enzymes for the conversion of a prodrug toa drug, - Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between Tand Cys, said linker being either cleavable or not cleavable for the releaseof T after the internalization of the hybrid compound into said cells.
机译:本发明涉及用于癌症治疗或诊断的新化合物和更具体地说,是将志贺毒素突变体的无毒B亚基用作过度表达Gb3受体的诊断产品或药物的载体细胞,具有下式的化合物:STxB-Z(n)-Cys-Y(m)-T其中-STxB是志贺毒素B亚基或功能等同物其中,-Z(n),其中n为0或1,并且当n为1时,Z为氨基酸不含巯基的残基,或为多肽,-Cys为氨基酸半胱氨酸残基,-T是通过共价键与S连接的分子半胱氨酸的一部分,选自:用于体内诊断的药物。细胞毒性剂,。前药,或。用于将前药转化为-Y(m),其中m为0或1,并且当m为1时,Y是T之间的连接基和Cys,所述接头对于释放而言是可裂解的或不可裂解的杂化化合物内化到所述细胞中后的T的变化。

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