Nikiforovich G V, Rozenblit S A, Shenderovich M D, Chipens G I
FEBS Lett. 1984 May 21;170(2):315-20. doi: 10.1016/0014-5793(84)81335-6.
By comparing the results of energy calculation for alpha-MSH and its semirigid analogues Ac-[ Cys4 , Cys10 ]-alpha- MSH4 -10-NH2, Ac-[ Cys4 , Cys10 ]-alpha- MSH4 -13-NH2, and [ Cys4 - Cys10 ]-alpha-MSH, a detailed description of two possible bioactive conformations for the 'specific' central site of alpha- MSH6 -9 is proposed representing variants of chain-reversal structure. A possible explanation of the rise in melanotropic activity of the latter two semirigid analogues is presented.
通过比较α-MSH及其半刚性类似物Ac-[Cys4,Cys10]-α-MSH4-10-NH2、Ac-[Cys4,Cys10]-α-MSH4-13-NH2和[Cys4-Cys10]-α-MSH的能量计算结果,对α-MSH6-9“特定”中心位点的两种可能生物活性构象进行了详细描述,这些构象代表了链反转结构的变体。还对后两种半刚性类似物促黑素活性的增加给出了一种可能的解释。