Synthetic laminin-like peptides and pseudopeptides as potential antimetastatic agents.
Synthetic laminin-like peptides and pseudopeptides as potential antimetastatic agents.
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合成的层粘连蛋白样肽和伪肽作为潜在的抗转移剂。
DOI：
10.1021/jm00046a023
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发表时间：
1994
影响因子：
7.3
通讯作者：
Mokotoff,M
中科院分区：
文献类型：
--
作者：
Zhao,M;Kleinman,HK;Mokotoff,M
本文介绍了我们的努力，以研究结构-活性关系，提高抗转移的效力，并限制在体内酶降解的YIGSR-NH 2，从层粘连蛋白的B1链的合成肽，据报道，有潜力作为抗转移剂。为此，我们合成了YIGSRNH 2的一系列t/>（CH 2NH）肽类似物（5-9）和其中Tyr残基被D-Tyr（1）、Phe（2）、Phe（pF）（3）和Phe（p-NH 2）（4）置换的许多肽。所有新的肽在体外测定其促进B16 F10小鼠黑色素瘤细胞和HT-1080人纤维肉瘤细胞中细胞附着的能力。基于体外测定结果，在尾静脉中共注射B16 F10黑素瘤细胞和1 mg肽的小鼠中，体内测试肽3-5、8和9抑制肿瘤转移至肺的能力。总之，在九种新肽中，仅Phe（p-NH 2）肽4显示一致的体外细胞附着活性，但仅显示低的体内抗转移活性。
This paper describes our efforts to study structure-activity relationships, improve the antimetastatic potency, and limit the in vivo enzymatic degradation of YIGSR-NH2, a synthetic peptide from the B1 chain of laminin, which reportedly has potential as an antimetastatic agent. To this end we have synthesized a series of t/>(CH2NH) peptide analogs (5-9) of YIGSRNH2 and a number of peptides in which the Tyr residue was replaced with D-Tyr (1), Phe (2), Phe (pF)(3), and Phe (p-NH2)(4). All new peptides were assayed in vitro fortheir ability to promote cell attachment in both B16F10 mouse melanoma cells and HT-1080 human fibrosarcoma cells. On the basis of the in vitro assay results, peptides 3-5, 8, and 9 were tested in vivo fortheir ability to inhibit tumor metastasis to the lungs in mice that were coinjected in the tail vein with B16F10 melanoma cells and 1 mg of peptide. In summary, of the nine new peptides only the Phe (p-NH2) peptide 4 showed consistent in vitro cell attachment activity, but only low in vivo antimetastatic activity.
鉴定层粘连蛋白中用于促进细胞粘附和迁移并抑制体内黑色素瘤肺部定植的第二个活性位点。
影响因子：
3.9
作者：
H. Kleinman;J. Graf;Y. Iwamoto;M. Sasaki;C. Schasteen;Yoshihiko Yamada;G. Martin;F. Robey
通讯作者：
F. Robey