Rajh H M, Mariman E C, Tesser G I, Nivard R J
Int J Pept Protein Res. 1980 Mar;15(3):200-10. doi: 10.1111/j.1399-3011.1980.tb02569.x.
Six sulphated octapeptide amide analogues, representing the C-terminal sequence of pancreozymin have been prepared in addition to the natural sequence. The tryptophyl residue which is essential for biological activity was replaced in this series by structurally, closely related analogues each of which resemble the properties of the original moiety to varying extents. The syntheses were so conducted that the C-terminal tetrapeptide amides (modified tetragastrins) could be secured. The results of the measurement of one of the biological parameters are indicated. The activity was determined to elucidate which of the physicochemical properties of the tryptophyl residue is most essential for exertion of biological activity in the described test.
除了天然序列外,还制备了六种代表促胰酶素C端序列的硫酸化八肽酰胺类似物。在该系列中,对生物活性至关重要的色氨酸残基被结构上密切相关的类似物取代,每个类似物在不同程度上类似于原始部分的性质。合成过程中确保了C端四肽酰胺(修饰的四肽胃泌素)的获得。给出了其中一个生物学参数的测量结果。测定活性是为了阐明在所描述的试验中,色氨酸残基的哪些物理化学性质对生物活性的发挥最为关键。