Schultz R M, Silberman S, Persky B, Bajkowski A S, Carmichael D F
Department of Biochemistry, Loyola University of Chicago, Stritch School of Medicine, Maywood, Illinois 60153.
Cancer Res. 1988 Oct 1;48(19):5539-45.
The human tissue inhibitor of metalloproteinases (TIMP) is a glycoprotein with a molecular weight of 28,000. It appears to be ubiquitous in human mesoderm tissues and has previously been shown to be identical to the collagenase inhibitor isolated from human skin fibroblasts. TIMP inhibits type I- and IV-specific collagenases and other neutral metalloendoproteinases that may be responsible for the degradation of extracellular matrix in tumor cell metastasis. In this work we have utilized recombinant human TIMP (rTIMP) obtained by expression of its cDNA gene (Carmichael et al., Proc. Natl. Acad. Sci. USA, 83:2407, 1986). The rTIMP is shown to have similar inhibition properties as natural TIMP against human skin fibroblast collagenase. In an in vitro amnion invasion assay system, rTIMP inhibited the invasion of B16-F10 murine melanoma cells through the human amniotic membrane at an identical concentration to that reported previously for natural TIMP. The mechanism by which rTIMP inhibits amniotic membrane invasion was compared to the mechanism by which the fibronectin receptor binding peptide RGDS and the aminin receptor binding peptide YIGSR inhibit amnion invasion. RGDS and YIGSR inhibited strong binding of the tumor cells to the amniotic membrane. In contrast rTIMP did not inhibit the cell adhesion step in amnion invasion, but actually increased the number of tumor cells that were tightly bound to the amnion. Thus rTIMP appears to inhibit a later step in the amnion invasion process, following B16-F10 cell adhesion. C57BL/6 mice treated with i.p. injections of rTIMP every 12 h for 6.5 days showed a significant inhibition of metastatic lung colonization by B16-F10 murine melanoma cells. While the rTIMP inhibited the number of metastatic lung tumors formed, it had no significant effect on the size of the lung tumors. Furthermore, tumors grown s.c. in mice receiving 12-h i.p. injections of rTIMP for 6.5 days, as in the in vivo colonization assay, showed no difference in size from controls. Thus the anticolonization effect of rTIMP appears not be due to an effect on tumor growth, but on the invasion step itself. The inhibition of lung colonization in C57BL/6 mice by rTIMP is one of the first examples showing an antimetastatic effect of a selective metalloproteinase inhibitor in a mammalian animal model, and supports an essential role for metalloproteinase(s) in the extravasation and invasion of tumor cells during lung colonization by blood-borne tumor cells.
人金属蛋白酶组织抑制剂(TIMP)是一种分子量为28,000的糖蛋白。它似乎在人胚层组织中普遍存在,并且先前已证明与从人皮肤成纤维细胞中分离出的胶原酶抑制剂相同。TIMP抑制I型和IV型特异性胶原酶以及其他可能负责肿瘤细胞转移过程中细胞外基质降解的中性金属内蛋白酶。在这项工作中,我们利用了通过其cDNA基因表达获得的重组人TIMP(rTIMP)(Carmichael等人,《美国国家科学院院刊》,83:2407,1986)。rTIMP对人皮肤成纤维细胞胶原酶显示出与天然TIMP相似的抑制特性。在体外羊膜侵袭试验系统中,rTIMP以与先前报道的天然TIMP相同的浓度抑制B16-F10小鼠黑色素瘤细胞对人羊膜的侵袭。将rTIMP抑制羊膜侵袭的机制与纤连蛋白受体结合肽RGDS和层粘连蛋白受体结合肽YIGSR抑制羊膜侵袭的机制进行了比较。RGDS和YIGSR抑制肿瘤细胞与羊膜的强结合。相反,rTIMP不抑制羊膜侵袭中的细胞粘附步骤,反而实际上增加了紧密结合在羊膜上的肿瘤细胞数量。因此,rTIMP似乎在B16-F10细胞粘附之后抑制羊膜侵袭过程中的后续步骤。每12小时腹腔注射rTIMP,持续6.5天的C57BL / 6小鼠显示出B16-F10小鼠黑色素瘤细胞对肺转移定植的显著抑制。虽然rTIMP抑制了形成的肺转移瘤数量,但对肺肿瘤的大小没有显著影响。此外,如在体内定植试验中一样,在接受每12小时腹腔注射rTIMP,持续6.5天的小鼠中皮下生长的肿瘤与对照相比大小没有差异。因此,rTIMP的抗定植作用似乎不是由于对肿瘤生长的影响,而是对侵袭步骤本身的影响。rTIMP对C57BL / 6小鼠肺定植的抑制是在哺乳动物动物模型中显示选择性金属蛋白酶抑制剂具有抗转移作用的首批例子之一,并支持金属蛋白酶在血源性肿瘤细胞肺定植过程中肿瘤细胞的外渗和侵袭中起重要作用。