阅读说明：本技术 Wt1衍生肽的缀合物和包含其的组合物 (Conjugates of WT 1-derived peptides and compositions comprising the same ) 是由 坂仁志 高梨洋辅 于 2018-12-26 设计创作，主要内容包括：本公开包括式(1)的化合物或其药学上可接受的盐,<Image he="115" wi="246" file="DEST_PATH_IMAGE002.GIF" imgContent="drawing" imgFormat="GIF" orientation="portrait" inline="no"></Image>其中癌抗原肽A是由7至30个氨基酸残基组成并含有至少一个半胱氨酸残基的MHC I类限制性肽,其中所述癌抗原肽A的半胱氨酸残基经由二硫键与R<Sup>1</Sup>结合；且R<Sup>1</Sup>是氢、式(2)的基团、式(3)的基团或癌抗原肽D,其中式(2)的基团是<Image he="97" wi="350" file="DEST_PATH_IMAGE004.GIF" imgContent="drawing" imgFormat="GIF" orientation="portrait" inline="no"></Image>其中X<Sup>a</Sup>和Y<Sup>a</Sup>独立地代表单键或由1至4个氨基酸残基组成的二价肽基团,条件是X<Sup>a</Sup>和Y<Sup>a</Sup>中氨基酸残基数量之和为0至4的整数,且癌抗原肽B是由9至30个氨基酸残基组成的MHC II类限制性肽,其中癌抗原肽B的N端氨基酸的氨基与式(2)中的Y<Sup>a</Sup>结合,并且癌抗原肽B的C端氨基酸的羰基与式(2)中的羟基结合,并且式(1)与式(2)经由二硫键结合,式(3)的基团是<Image he="91" wi="366" file="DEST_PATH_IMAGE006.GIF" imgContent="drawing" imgFormat="GIF" orientation="portrait" inline="no"></Image>其中X<Sup>b</Sup>和Y<Sup>b</Sup>独立地代表单键或由1至4个氨基酸残基组成的二价肽基团,条件是X<Sup>b</Sup>和Y<Sup>b</Sup>中氨基酸残基数量之和为0至4的整数,且癌抗原肽C是由9至30个氨基酸残基组成的MHC II类限制性肽,其中癌抗原肽C的C端氨基酸的羰基与式(3)中的X<Sup>b</Sup>结合,并且癌抗原肽C的N端氨基酸的氨基与式(3)中的氢原子结合,并且式(1)与式(3)经由二硫键结合,且癌抗原肽D是由9至30个氨基酸残基组成并含有至少一个半胱氨酸的MHC II类限制性肽,其中癌抗原肽D的半胱氨酸残基经由二硫键与R<Sup>1</Sup>结合。(The present disclosure includes compounds of formula (1) or a pharmaceutically acceptable salt thereof, wherein the cancer antigen peptide A is an MHC class I restricted peptide consisting of 7 to 30 amino acid residues and containing at least one cysteine residue, wherein the cysteine residue of the cancer antigen peptide A is linked to R via a disulfide bond 1 Combining; and R is 1 Is hydrogen, a group of formula (2), a group of formula (3) or a cancer antigen peptide D, wherein the group of formula (2) is Wherein X a And Y a Independently represents a single bond or a divalent peptide group consisting of 1 to 4 amino acid residues, with the proviso that X a And Y a The sum of the number of amino acid residues is an integer of 0 to 4, and the cancer antigen peptide B is an MHC class II restricted peptide consisting of 9 to 30 amino acid residues, wherein the amino group of the N-terminal amino acid of the cancer antigen peptide B is the same as that of Y in the formula (2) a And the carbonyl group of the C-terminal amino acid of the cancer antigen peptide B is bonded to the hydroxyl group in the formula (2), and the formula (1) and the formula (2) are bonded via a disulfide bond, the group of the formula (3) is Wherein X b And Y b Independently represents a single bond or a divalent peptide group consisting of 1 to 4 amino acid residues, with the proviso that X b And Y b The sum of the number of amino acid residues is an integer of 0 to 4, and the cancer antigen peptide C is an MHC class II restricted peptide consisting of 9 to 30 amino acid residues, wherein the carbonyl group of the C-terminal amino acid of the cancer antigen peptide C is bonded to X in the formula (3) b And an amino group of the N-terminal amino acid of the cancer antigen peptide C is bonded to a hydrogen atom in the formula (3), and the formula (1) and the formula (3) are bonded via a disulfide bond, and the cancer antigen peptide D is an MHC class II restricted peptide consisting of 9 to 30 amino acid residues and containing at least one cysteine, wherein the cysteine residue of the cancer antigen peptide D is bonded to R via a disulfide bond 1 And (4) combining.)