BIOLOGICALLY-ACTIVE CALCITONIN ANALOGS WHICH HAVE MINIMAL INTERACTIONS WITH PHOSPHOLIPIDS
BIOLOGICALLY-ACTIVE CALCITONIN ANALOGS WHICH HAVE MINIMAL INTERACTIONS WITH PHOSPHOLIPIDS
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DOI：
10.1016/s0006-291x(88)80700-9
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发表时间：
1988-04-15
影响因子：
3.1
通讯作者：
ORLOWSKI, RC
中科院分区：
文献类型：
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作者：
EPAND, RM;EPAND, RF;ORLOWSKI, RC
许多肽激素已被证明含有能够结合磷脂的两亲性螺旋片段。这种构象特征与这些激素的生物活性增加有关。然而，我们证明了两种降钙素类似物，[Gly 8，Ala 16]-des-Leu 19鲑鱼降钙素和des-1-氨基-[Ala 1，7，Gly 8]-des-Leu 19鲑鱼降钙素与磷脂的相互作用最小。这些肽在二肉豆蔻酰磷脂酰甘油的存在下都没有获得任何增加的螺旋含量，并且这些肽在改变这种脂质的相变性质方面仅具有微弱的作用。因此，尽管磷脂诱导的两亲性螺旋序列的存在可以增强生物活性，但它不是活性所必需的。
A number of peptide hormones have been shown to contain amphipathic helical segments capable of binding to phospholipids. This conformational feature has been associated with increased biological activity of these hormones. We demonstrate, however, that two calcitonin analogs, [Gly8, Ala16]-des-Leu19 salmon calcitonin and des-1-amino-[Ala1,7, Gly8]-des-Leu19 salmon calcitonin have minimal interactions with phospholipids. Neither of these peptides acquire any increased helical content in the presence of dimyristoylphosphatidylglycerol and these peptides have only weak effects in altering the phase transition properties of this lipid. Therefore, although the presence of a phospholipid-induced amphipathic helical sequence may enhance the biological activity, it is not required for activity.