Jacobson K A, Verlander M S, Rosenkranz R P, Melmon K L, Goodman M
Int J Pept Protein Res. 1983 Sep;22(3):284-304. doi: 10.1111/j.1399-3011.1983.tb02095.x.
A series of monodisperse oligopeptide conjugates related to the catecholamine, isoproterenol, has been synthesized. The peptide carrier molecules used were synthesized by stepwise and fragment condensation techniques and ranged in size from a single, blocked amino acid derivative to isomeric pentapeptides. The amino acid compositions and sequences of the carriers were chosen so as to provide specific information concerning the effects of molecular weight, hydrophilic/hydrophobic balance, charge, etc., on the biological activity of the final conjugates. The common point of attachment for the drug in all carriers was a p-aminophenylalanine residue. The peptide-catecholamine conjugates were prepared via the attachment of carboxyl-containing catecholamine congeners, to the peptide carriers by techniques described previously. The conjugates were purified rigorously by chromatographic techniques and characterized by high-field n.m.r. spectroscopy.
已合成了一系列与儿茶酚胺异丙肾上腺素相关的单分散寡肽缀合物。所使用的肽载体分子是通过逐步和片段缩合技术合成的，大小范围从单个封闭氨基酸衍生物到异构五肽。选择载体的氨基酸组成和序列，以便提供有关分子量、亲水/疏水平衡、电荷等对最终缀合物生物活性影响的具体信息。所有载体中药物的共同连接点是对氨基苯丙氨酸残基。肽-儿茶酚胺缀合物是通过将含羧基的儿茶酚胺同系物按照先前描述的技术连接到肽载体上制备的。通过色谱技术对缀合物进行了严格纯化，并通过高场核磁共振光谱进行了表征。
