Reddy C C, Wells A, Lauffenburger D A
Department of Chemical Engineering, University of Illinois at Urbana-Champaign 61801, USA.
Med Biol Eng Comput. 1998 Jul;36(4):499-507. doi: 10.1007/BF02523222.
Transforming growth factor alpha (TGF alpha) has been reported to be a more potent agonist when compared to epidermal growth factor (EGF) in several systems while acting via their common receptor, the epidermal growth factor receptor (EGFR). It has been postulated that this increased potency is mediated by the increased recycling of EGFR upon activation by TGF alpha as against receptor activation by EGF. The authors test this hypothesis by simultaneously measuring mitogenesis and the dynamics of surface receptor number in response to these ligands in NR6 mouse fibroblasts expressing the EGFR. The data demonstrates that increased receptor recycling due to endosomal dissociation of TGF alpha can indeed realise an increased mitogenic potency relative to EGF under appropriate cellular and experimental conditions (i.e. situations in which the increase in the number of occupied receptors due to receptor sparing by TGF alpha represents additional mitogenic signalling capacity). However, this difference in receptor trafficking does not uniquely determine the relative potencies of these ligands since TGF alpha is a less potent mitogen compared to EGF when experimental conditions are dominated by the effects of ligand trafficking on growth factor availability. Thus, the relative potencies of these growth factors are determined in a given context by the relative importance of ligand and receptor trafficking effects which determine the availability of these signalling components. These results are consistent with a suggested model of hormone responsiveness which favours dissociative ligands (such as TGF alpha) in receptor-limited situations and non-dissociative ligands (such as EGF) in the case of ligand limitation.
据报道,在多个系统中,与表皮生长因子(EGF)相比,转化生长因子α(TGFα)通过其共同受体表皮生长因子受体(EGFR)发挥作用时,是一种更有效的激动剂。据推测,这种增强的效力是由TGFα激活后EGFR循环增加介导的,而EGF激活受体时则不然。作者通过在表达EGFR的NR6小鼠成纤维细胞中同时测量有丝分裂和响应这些配体时表面受体数量的动态变化来验证这一假设。数据表明,在适当的细胞和实验条件下(即由于TGFα的受体保留导致被占据受体数量增加代表额外有丝分裂信号能力的情况),由于TGFα的内体解离导致的受体循环增加确实可以实现相对于EGF增强的有丝分裂效力。然而,受体运输的这种差异并不能唯一地决定这些配体的相对效力,因为当实验条件受配体运输对生长因子可用性的影响主导时,TGFα作为有丝分裂原的效力低于EGF。因此,在给定的背景下,这些生长因子的相对效力由决定这些信号成分可用性的配体和受体运输效应的相对重要性决定。这些结果与一种建议的激素反应模型一致,该模型在受体受限的情况下有利于解离性配体(如TGFα),在配体受限的情况下有利于非解离性配体(如EGF)。