公开(公告)号：US5068223A

公开(公告)日：1991-11-26

申请号：US324151

申请日：1989-03-15

申请人： Peter E. Lipsky ,  Dwain L. Thiele

发明人： Peter E. Lipsky ,  Dwain L. Thiele

IPC分类号： A61K38/05

CPC分类号： A61K38/05

摘要： Esters or amides of a peptide, preferebly a dipeptide, consisting essentially of natural or synthetic L-amino acids with hydrophobic side chains were found to have specific cellular toxicities. Preferable amino acids of the peptide are leucine, phenylalanine valine, isoleucine, alanine, proline, glycine or aspartic acid beta methyl ester. Preferable dipeptides are L leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-Leucyl L-isoleucine, L-henylalanyl L-phenylalanine, L-valyl L-leucine, L-leucyl L-alanine, L-valyl L-valine, L-phenylalanyl L leucine, L prolyl L-leucine, L-leucyl L-valine, L-phenylalanyl L-valine, L glycyl L-leucine, L-leucyl L-glycine, glycyl L-phenylalanine and L-aspartyl beta methyl ester L-phenylalanine. Most preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-phenylalanyl L-leucine, L-leucyl L-isoleucine L-phenylalanyl L-phenylalanine and L-valyl L-leucine.The ester or amide of the dipeptide is most preferably alkyl, aralkyl or aryl a preferred alkylester is a methyl ester and may also be an ethyl ester or alkyl of up to about four carbon atoms such as propyl, isopropyl, butyl or isobutyl. Yet larger alkyl substituents may also be functional judging from the beta naphthyl substituent which is functional in certain embodiments.These alkyl, aryl or arylkyl esters and amides of dipeptides consist essentially of amino acids with hydrophobic side chains may be used to deplete cytotoxic T-lymphocytes or natural killer cells from organisms, cell populations or tissues.

摘要翻译： 被发现具有疏水侧链的天然或合成的L-氨基酸的肽，优先二肽的酯或酰胺具有特异性的细胞毒性。 肽的优选氨基酸是亮氨酸，苯丙氨酸缬氨酸，异亮氨酸，丙氨酸，脯氨酸，甘氨酸或天冬氨酸β-甲酯。 优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-亮氨酰L-异亮氨酸，L-苯丙氨酰丙氨酰L-苯丙氨酸，L-缬氨酰L-亮氨酸，L-亮氨酰L-丙氨酸 ，L-缬氨酰L-缬氨酸，L-苯丙氨酰L-亮氨酸，L脯氨酰L-亮氨酸，L-亮氨酰L-缬氨酸，L-苯丙氨酰L-缬氨酸，L-甘氨酰L-亮氨酸，L-亮氨酰L-甘氨酸， 苯丙氨酸和L-天冬氨酰基β-甲酯L-苯丙氨酸。 最优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-苯丙氨酰L-亮氨酸，L-亮氨酰L-异亮氨酸L-苯丙氨酰L-苯丙氨酸和L-缬氨酰L- 亮氨酸。 二肽的酯或酰胺最优选是烷基，芳烷基或芳基，优选的烷基酯是甲酯，也可以是最多约四个碳原子的乙酯或烷基，如丙基，异丙基，丁基或异丁基。 根据在某些实施方案中是功能的β萘基取代基，更大的烷基取代基也可以是官能的。 这些二肽的烷基，芳基或芳基烷基酯和酰胺基本上由具有疏水侧链的氨基酸组成可用于从生物体，细胞群或组织中消耗细胞毒性T淋巴细胞或天然杀伤细胞。

公开(公告)号：US5304474A

公开(公告)日：1994-04-19

申请号：US684010

申请日：1991-04-11

申请人： Peter E. Lipsky ,  Dwain L. Thiele

发明人： Peter E. Lipsky ,  Dwain L. Thiele

IPC分类号： A61K38/05 ,  C12P21/00

CPC分类号： A61K38/05

摘要： Esters or amides of a peptide, preferably a dipeptide, consisting essentially of natural or synthetic L-amino acids with hydrophobic side chains were found to have specific cellular toxicities. Preferable amino acids of the peptide are leucine, phenylalanine valine, isoleucine, alanine, proline, glycine or aspartic acid beta methyl ester. Preferable dipeptides are L leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-leucyl L-isoleucine, L-phenylalanyl L-phenylalanine, L-valyl L-leucine, L-leucyl L-alanine, L-valyl L-valine, L-phenylalanyl L leucine, L prolyl L-leucine, L-leucyl L-valine, L-phenylalanyl L-valine, L glycyl L-leucine, L-leucyl L-glycine, glycyl L-phenylalanine and L-aspartyl beta methyl ester L-phenylalanine. Most preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-phenylalanyl L-leucine, L-leucyl L-isoleucine L-phenylalanyl L-phenylalanine and L-valyl L-leucine.

摘要翻译： 被发现具有疏水侧链的天然或合成的L-氨基酸的肽，优选二肽的酯或酰胺具有特异性的细胞毒性。 肽的优选氨基酸是亮氨酸，苯丙氨酸缬氨酸，异亮氨酸，丙氨酸，脯氨酸，甘氨酸或天冬氨酸β-甲酯。 优选的二肽是L亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-亮氨酰L-异亮氨酸，L-苯丙氨酰L-苯丙氨酸，L-缬氨酰L-亮氨酸，L-亮氨酰L-丙氨酸 ，L-缬氨酰L-缬氨酸，L-苯丙氨酰L-亮氨酸，L脯氨酰L-亮氨酸，L-亮氨酰L-缬氨酸，L-苯丙氨酰L-缬氨酸，L-甘氨酰L-亮氨酸，L-亮氨酰L-甘氨酸， 苯丙氨酸和L-天冬氨酰基β-甲酯L-苯丙氨酸。 最优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-苯丙氨酰L-亮氨酸，L-亮氨酰L-异亮氨酸L-苯丙氨酰L-苯丙氨酸和L-缬氨酰L- 亮氨酸。

公开(公告)号：US5668112A

公开(公告)日：1997-09-16

申请号：US310677

申请日：1994-09-22

申请人： Peter E. Lipsky ,  Dwain L. Thiele

发明人： Peter E. Lipsky ,  Dwain L. Thiele

IPC分类号： A61K38/05

CPC分类号： A61K38/05

摘要： Esters or amides of a peptide, preferably a dipeptide, consisting essentially of natural or synthetic L-amino acids with hydrophobic side chains were found to have specific cellular toxicities. Preferable amino acids of the peptide are leucine, phenylalanine valine, isoleucine, alanine, proline, glycine or aspartic acid beta methyl ester. Preferable dipeptides are L leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-leucyl L-isoleucine, L-phenylalanyl L-phenylalanine, L-valyl L-leucine, L-leucyl L-alanine, L-valyl L-valine, L-phenylalanyl L leucine, L prolyl L-leucine, L-leucyl L-valine, L-phenylalanyl L-valine, L glycyl L-leucine, L-leucyl L-glycine, glycyl L-phenylalanine and L-aspartyl beta methyl ester L-phenylalanine. Most preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-phenylalanyl L-leucine, L-leucyl L-isoleucine L-phenylalanyl L-phenylalanine and L-valyl L-leucine.The ester or amide of the dipeptide is most preferably alkyl, aralkyl or aryl a preferred alkylester is a methyl ester and may also be an ethyl ester or alkyl of up to about four carbon atoms such as propyl, isopropyl, butyl or isobutyl. Yet larger alkyl substituents may also be functional judging from the beta naphthyl substituent which is functional in certain embodiments.These alkyl, aryl or arylkyl esters and amides of dipeptides consist essentially of amino acids with hydrophobic side chains may be used to deplete cytotoxic T-lymphocytes or natural killer cells from organisms, cell populations or tissues.

摘要翻译： 被发现具有疏水侧链的天然或合成的L-氨基酸的肽，优选二肽的酯或酰胺具有特异性的细胞毒性。 肽的优选氨基酸是亮氨酸，苯丙氨酸缬氨酸，异亮氨酸，丙氨酸，脯氨酸，甘氨酸或天冬氨酸β-甲酯。 优选的二肽是L亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-亮氨酰L-异亮氨酸，L-苯丙氨酰L-苯丙氨酸，L-缬氨酰L-亮氨酸，L-亮氨酰L-丙氨酸 ，L-缬氨酰L-缬氨酸，L-苯丙氨酰L-亮氨酸，L脯氨酰L-亮氨酸，L-亮氨酰L-缬氨酸，L-苯丙氨酰L-缬氨酸，L-甘氨酰L-亮氨酸，L-亮氨酰L-甘氨酸， 苯丙氨酸和L-天冬氨酰基β-甲酯L-苯丙氨酸。 最优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-苯丙氨酰L-亮氨酸，L-亮氨酰L-异亮氨酸L-苯丙氨酰L-苯丙氨酸和L-缬氨酰L- 亮氨酸。 二肽的酯或酰胺最优选是烷基，芳烷基或芳基，优选的烷基酯是甲酯，也可以是最多约四个碳原子的乙酯或烷基，如丙基，异丙基，丁基或异丁基。 根据在某些实施方案中是功能的β萘基取代基，更大的烷基取代基也可以是官能的。 这些二肽的烷基，芳基或芳基烷基酯和酰胺基本上由具有疏水侧链的氨基酸组成可用于从生物体，细胞群或组织中消耗细胞毒性T淋巴细胞或天然杀伤细胞。

公开(公告)号：US4752602A

公开(公告)日：1988-06-21

申请号：US774051

申请日：1985-09-09

申请人： Peter E. Lipsky ,  Dwain L. Thiele

发明人： Peter E. Lipsky ,  Dwain L. Thiele

IPC分类号： A61K38/05 ,  A61K37/02

CPC分类号： A61K38/05

摘要： An alkyl ester of dipeptide consisting essentially of natural or synthetic L-amino acids with hydrophobic side chains. Preferable amino acids are leucine, phenylalanine valine, isoleucine, alanine, proline, glycine or aspartic acid beta methyl ester. Preferable dipeptides are L leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-leucyl L-isoleucine, L-phenylalanyl L-phenylalanine, L-valyl L-leucine, L-leucyl L-alanine, L-valyl L-valine, L-phenylalanyl L leucine, L prolyl L-leucine, L-leucyl L-valine, L-phenylalanyl L-valine, L glycyl L-leucine, L-leucyl L-glycine or L-aspartyl beta methyl ester L-phenylalanine. Most preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-phenylalanyl L-leucine, L-leucyl L-isoleucine L-phenylalanyl L-phenylalanine and L-valyl L-leucine.The alkyl ester of the dipeptide is most preferably a methyl ester and may also be an ethyl ester or alkyl of up to about four carbon atoms such as propyl, isopropyl, butyl or isobutyl.These alkyl esters of dipeptides consisting essentially of amino acids with hydrophobic side chains may be used to deplete cytotoxic T-lymphocytes or natural killer cells from organisms, cell populations or tissues.

摘要翻译： 二肽的烷基酯主要由具有疏水侧链的天然或合成的L-氨基酸组成。 优选的氨基酸是亮氨酸，苯丙氨酸缬氨酸，异亮氨酸，丙氨酸，脯氨酸，甘氨酸或天冬氨酸β-甲酯。 优选的二肽是L亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-亮氨酰L-异亮氨酸，L-苯丙氨酰L-苯丙氨酸，L-缬氨酰L-亮氨酸，L-亮氨酰L-丙氨酸 ，L-缬氨酰L-缬氨酸，L-苯丙氨酰L亮氨酸，L脯氨酰L-亮氨酸，L-亮氨酰L-缬氨酸，L-苯丙氨酰L-缬氨酸，L-甘氨酰L-亮氨酸，L-亮氨酰L-甘氨酸或L-天冬氨酰 β-甲基酯L-苯丙氨酸。 最优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-苯丙氨酰L-亮氨酸，L-亮氨酰L-异亮氨酸L-苯丙氨酰L-苯丙氨酸和L-缬氨酰L- 亮氨酸。 二肽的烷基酯最优选是甲酯，也可以是最多约四个碳原子的乙酯或烷基，如丙基，异丙基，丁基或异丁基。 这些基本上由具有疏水侧链的氨基酸组成的二肽的烷基酯可用于从生物体，细胞群或组织中消耗细胞毒性T淋巴细胞或天然杀伤细胞。

公开(公告)号：US5346888A

公开(公告)日：1994-09-13

申请号：US994600

申请日：1992-12-21

申请人： Peter E. Lipsky ,  Dwain L. Thiele

发明人： Peter E. Lipsky ,  Dwain L. Thiele

IPC分类号： A61K38/05 ,  E21B10/20 ,  E21B10/22 ,  F16C17/04 ,  A61K37/02 ,  C07K5/06

CPC分类号： A61K38/05

摘要： An alkyl ester of dipeptide comprising natural or synthetic L-amino acids with hydrophobic side chains is provided herein. Preferable amino acids are leucine, phenylalanine valine, isoleucine, alanine, proline, glycine or aspartic acid beta methyl ester. Preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-leucyl L-isoleucine, L-phenylalanyl L-phenylalanine, L-valyl L-leucine, L-leucyl L-alanine, L-valyl L-valine, L-phenylalanyl L leucine, L prolyl L-leucine, L-leucyl L-valine, L-phenylalanyl L-valine, L glycyl L-leucine, L-leucyl L-glycine or L-aspartyl beta methyl ester L-phenylalanine. Most preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-phenylalanyl L-leucine, L-leucyl L-isoleucine L-phenylalanyl L-phenylalanine and L-valyl L-leucine. The alkyl ester of the dipeptide is most preferably a methyl ester and may also be an ethyl ester or alkyl of up to about four carbon atoms such as propyl, isopropyl, butyl or isobutyl. These alkyl esters of dipeptides comprising amino acids with hydrophobic side chains may be used to deplete cytotoxic T-lymphocytes or natural killer cells from organisms, cell populations or tissues. The O-alkyl esters of the described alkyl dipeptide esters inhibit lethal graft-vs-host disease and allograft rejection, particularly skin allograft rejection by a transplant recipient. The dipeptide most preferably employed is the O-alkyl dipeptide ester, or Leu-Leu-OMe.

摘要翻译： 本文提供了包含具有疏水侧链的天然或合成L-氨基酸的二肽的烷基酯。 优选的氨基酸是亮氨酸，苯丙氨酸缬氨酸，异亮氨酸，丙氨酸，脯氨酸，甘氨酸或天冬氨酸β-甲酯。 优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-亮氨酰L-异亮氨酸，L-苯丙氨酰L-苯丙氨酸，L-缬氨酰L-亮氨酸，L-亮氨酰L-亮氨酸， 丙氨酸，L-缬氨酰L-缬氨酸，L-苯丙氨酰L亮氨酸，L脯氨酰L-亮氨酸，L-亮氨酰L-缬氨酸，L-苯丙氨酰L-缬氨酸，L-甘氨酰L-亮氨酸，L-亮氨酰L-甘氨酸或L- 天冬氨酰基β甲酯L-苯丙氨酸。 最优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-苯丙氨酰L-亮氨酸，L-亮氨酰L-异亮氨酸L-苯丙氨酰L-苯丙氨酸和L-缬氨酰L- 亮氨酸。 二肽的烷基酯最优选是甲酯，也可以是最多约四个碳原子的乙酯或烷基，如丙基，异丙基，丁基或异丁基。 这些包含具有疏水侧链的氨基酸的二肽烷基酯可用于从生物体，细胞群或组织中消耗细胞毒性T淋巴细胞或天然杀伤细胞。 所述烷基二肽酯的O-烷基酯抑制致死性移植物抗宿主病和同种异体移植排斥，特别是移植受体的皮肤同种异体移植排斥。 最优选使用的二肽是O-烷基二肽酯或Leu-Leu-OMe。

公开(公告)号：US5047401A

公开(公告)日：1991-09-10

申请号：US168177

申请日：1988-03-15

申请人： Peter E. Lipsky ,  Dwain L. Thiele

发明人： Peter E. Lipsky ,  Dwain L. Thiele

IPC分类号： A61K38/05 ,  E21B10/20 ,  E21B10/22 ,  F16C17/04

CPC分类号： A61K38/05

摘要： An alkyl ester of dipeptide consisting essentially of natural or synthetic L-amino acids with hydrophobic side chains. Preferable amino acids are leucine, phenylalanine valine, isoleucine, alanine, proline, glycine or aspartic acid beta methyl ester. Preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-leucyl L-isoleucine, L-phenylalanyl L-phenylalanine, L-valyl L-leucine, L-leucyl L-alanine, L-valyl L-valine, L-phenylalanyl L-leucine, L-leucine, L-prolyl L-leucine, L-leucyl, L-valine, L-phenylalanyl L-valine, L-glycyl L-leucine, L-leucyl L-glycine or L-aspartyl beta methyl ester L-phenylalanine. Most preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-phenylalanyl L-leucine, L-leucyl L-isoleucine L-phenylalanyl L-phenylalanine and L-valyl L-leucine.The alkyl ester of the dipeptide is most preferably a methyl ester and may also be an ethyl ester or alkyl of up to about four carbon atoms such as propyl, isopropyl, butyl or isobutyl.These alkyl esters of dipeptides consisting essentially of amino acids with hydrophobic side chains may be used to deplete cytotoxic T-lymphocytes or natural killer cells from organisms, cell populations or tissues.

摘要翻译： 二肽的烷基酯主要由具有疏水侧链的天然或合成的L-氨基酸组成。 优选的氨基酸是亮氨酸，苯丙氨酸缬氨酸，异亮氨酸，丙氨酸，脯氨酸，甘氨酸或天冬氨酸β-甲酯。 优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-亮氨酰L-异亮氨酸，L-苯丙氨酰L-苯丙氨酸，L-缬氨酰L-亮氨酸，L-亮氨酰L-亮氨酸， 丙氨酸，L-缬氨酰L-缬氨酸，L-苯丙氨酰L-亮氨酸，L-亮氨酸，L-脯氨酰L-亮氨酸，L-亮氨酰，L-缬氨酸，L-苯丙氨酰L-缬氨酸，L-甘氨酰L-亮氨酸，L L-亮氨酸L-甘氨酸或L-天冬氨酰基β-甲酯L-苯丙氨酸。 最优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-苯丙氨酰L-亮氨酸，L-亮氨酰L-异亮氨酸L-苯丙氨酰L-苯丙氨酸和L-缬氨酰L- 亮氨酸。 二肽的烷基酯最优选是甲酯，也可以是最多约四个碳原子的乙酯或烷基，如丙基，异丙基，丁基或异丁基。 这些基本上由具有疏水侧链的氨基酸组成的二肽的烷基酯可用于从生物体，细胞群或组织中消耗细胞毒性T淋巴细胞或天然杀伤细胞。

公开(公告)号：US5602102A

公开(公告)日：1997-02-11

申请号：US890422

申请日：1992-05-29

申请人： Dwain L. Thiele ,  Peter E. Lipsky ,  Michael J. McGuire

发明人： Dwain L. Thiele ,  Peter E. Lipsky ,  Michael J. McGuire

IPC分类号： C07C237/06 ,  C07C245/14 ,  C07C381/12 ,  C12N9/48 ,  C12N15/113 ,  C12N15/57 ,  A61K38/05

CPC分类号： C12N15/1137 ,  C07C237/06 ,  C07C245/14 ,  C07C381/12 ,  C12N9/48 ,  C12Y304/14001 ,  C12N2310/315 ,  C12N2310/33

摘要： Therapeutic agents and methods for the treatment of immunologically mediated diseases and malignancies of myeloid cell or lymphoid cell origin. These particular methods utilize the characterization of particular activation mechanisms important to the progression of these pathologies in humans. Selective inhibition of cell types responsible for precipitating these disorders in humans are provided with therapeutic agents which include peptides capable of inhibiting dipeptidyl peptidase-I activation of proenzymes present primarily in cytotoxic T-cells and myeloid cells, such as Gly--Phe--CHN.sub.2. Antisense oligonucleotides are also characterized which are specific for human dipeptidyl peptidase-I gene which may be used in the treatment of the described disorders.

摘要翻译： 用于治疗免疫介导的疾病和骨髓细胞或淋巴细胞起源的恶性肿瘤的治疗剂和方法。 这些特定的方法利用对人类这些病理进展重要的特定活化机制的表征。 提供了负责沉淀人类这些疾病的细胞类型的选择性抑制，其包括能够抑制主要存在于细胞毒性T细胞和骨髓细胞如Gly-Phe-CHN2中的酶的二肽基肽酶-I活化的肽的治疗剂。 还表征了反义寡核苷酸，其可用于治疗所述疾病的人二肽基肽酶-I基因。

公开(公告)号：US5206221A

公开(公告)日：1993-04-27

申请号：US643538

申请日：1991-01-18

申请人： Peter E. Lipsky ,  Dwain L. Thiele

发明人： Peter E. Lipsky ,  Dwain L. Thiele

IPC分类号： A61K38/05 ,  E21B10/20 ,  E21B10/22 ,  F16C17/04

CPC分类号： A61K38/05

摘要： An alkyl ester of dipeptide consisting essentially of natural or synthetic L-amino acids with hydrophobic side chains. Preferable amino acids are leucine, phenylalanine valine, isoleucine, alanine, proline, glycine or aspartic acid beta methyl ester. Preferable dipeptides are L leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-leucyl L-isoleucine, L-phenylalanyl L-phenylalanine, L-valyl L-leucine, L-leucyl L-alanine, L-leucine, L-leucyl L-valine, L-phenylalanyl L-valine, L glycyl L-leucine, L-leucyl L-glycine or L-aspartyl beta methyl ester L-phenylalaine. Most preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-phenylalanyl L-leucine, L-leucyl L-isoleucine, L-phenylalanyl L-phenylalanine and L-valyl L-leucine.The alkyl ester of the dipeptide is most preferably a methyl ester and may also be an ethyl ester or alkyl of up to about four carbon atoms such as propyl, isopropyl, butyl or isobutyl.These alkyl esters of dipeptides consisting essentially of amino acids with hydrophobic side chains may be used to deplete cytotoxic T-lymphocytes or natural killer cells from organisms, cell populations or tissues.

摘要翻译： 二肽的烷基酯主要由具有疏水侧链的天然或合成的L-氨基酸组成。 优选的氨基酸是亮氨酸，苯丙氨酸缬氨酸，异亮氨酸，丙氨酸，脯氨酸，甘氨酸或天冬氨酸β-甲酯。 优选的二肽是L亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-亮氨酰L-异亮氨酸，L-苯丙氨酰L-苯丙氨酸，L-缬氨酰L-亮氨酸，L-亮氨酰L-丙氨酸 L-亮氨酸，L-亮氨酸L-缬氨酸，L-苯丙氨酰L-缬氨酸，L-甘氨酰L-亮氨酸，L-亮氨酰L-甘氨酸或L-天冬氨酰基β-甲酯L-苯基胺。 最优选的二肽是L-亮氨酸L-亮氨酸，L-亮氨酰L-苯丙氨酸，L-缬氨酰L-苯丙氨酸，L-苯丙氨酰L-亮氨酸，L-亮氨酰L-异亮氨酸，L-苯丙氨酰L-苯丙氨酸和L-缬氨酰L 亮氨酸 二肽的烷基酯最优选是甲酯，也可以是最多约四个碳原子的乙酯或烷基，如丙基，异丙基，丁基或异丁基。 这些基本上由具有疏水侧链的氨基酸组成的二肽的烷基酯可用于从生物，细胞群或组织中消耗细胞毒性T淋巴细胞或天然杀伤细胞。