Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation.
Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation.
复制标题
通过限制氨基酸和骨架掺入优化生长抑素模拟物。
DOI：
10.1016/s0960-894x(00)00552-7
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发表时间：
2000
影响因子：
2.7
通讯作者：
Ellman,JA
中科院分区：
文献类型：
--
作者：
Souers,AJ;Rosenquist,A;Jarvie,EM;Ladlow,M;Feniuk,W;Ellman,JA
通过将构象约束引入到九元杂环支架中，制备了有效的和亚型选择性的生长抑素模拟物1的限制性类似物5-7。与先导化合物1相比，每个受限制的模拟肽类药物的活性都发生了变化，其中化合物7分别与生长抑素受体亚型sst4和sst5的结合增强了25倍和2倍。
Constrained analogues 5–7 of the potent and subtype selective somatostatin mimetic 1 were prepared by incorporating conformational constraints into the nine-membered heterocyclic scaffold. Each constrained peptidomimetic showed an altered activity profile relative to lead compound 1, with compound 7 exhibiting a 25-fold and 2-fold binding enhancement against somatostatin receptor subtypes sst4 and sst5, respectively.