Draper M W, Rizack M A, Merrifield R B
Biochemistry. 1975 Jul;14(13):2933-8. doi: 10.1021/bi00684a022.
Twenty-three analogs of the ACTH-(4-10)-heptapeptide sequence, which forms the "active core" of adrenocorticotropin (ACTH) and related hormones, have been synthesized by the solid-phase method. These analogs all contain structural modifications at or near the 5-glutamic acid residue of ACTH. The peptides were purified to electrophoretic and chromatographic homogeneity. The peptides were assayed for lipolytic activity in an isolated cell system derived from rabbit adipose tissue. In this system, it was determined that residue 5 plays a very important "spacer" role in the peptide, but that this spacer function is not very dependent on the nature of the side chain of the position 5 amino acid. It was found, however, that a number of analogs containing basic residues (arginine or lysine) in position 3 and/or position 5 of ACTH-(3-10) and ACTH-(4-10) fragments have 5 to 10 times the activity of the respective parent peptides. The presence of a latent anionic locus in the rabbit fat-cell receptor for ACTH is suggested by this study.
已通过固相法合成了促肾上腺皮质激素（ACTH）-（4-10）七肽序列的23种类似物，该序列构成了促肾上腺皮质激素（ACTH）及相关激素的“活性核心”。这些类似物在ACTH的5-谷氨酸残基处或其附近均含有结构修饰。这些肽经纯化后达到电泳和色谱均一性。在源自兔脂肪组织的分离细胞系统中测定了这些肽的脂解活性。在该系统中，已确定5位残基在肽中起着非常重要的“间隔”作用，但这种间隔功能并不十分依赖于5位氨基酸侧链的性质。然而，已发现，在ACTH-（3-10）和ACTH-（4-10）片段的3位和/或5位含有碱性残基（精氨酸或赖氨酸）的许多类似物，其活性是各自亲本肽的5至10倍。这项研究表明，兔脂肪细胞ACTH受体中存在潜在的阴离子位点。
