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首页> 外文期刊>Journal of Medicinal Chemistry >Synthesis and Pharmacological Evaluation of an Analogue of the Peptide Hormone Oxytocin That Contains a Mimetic of an Inverse gamma-Turn.
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Synthesis and Pharmacological Evaluation of an Analogue of the Peptide Hormone Oxytocin That Contains a Mimetic of an Inverse gamma-Turn.

机译：合成和药理学评估的肽激素催产素的类似物，其中包含类似的反向伽玛转。

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摘要

Oxytocin is a neurohypophyseal peptide hormone that induces labor and lactation in mammals. An inverse gamma-turn mimetic corresponding to the tripeptide Ile-Val-Asn has been synthesized and incorporated instead of residues 3-5 of oxytocin to probe the hypothesis that a gamma-turn involving these residues is found in the receptor bound conformation of oxytocin. In the turn mimetic, residues i and i + 1 are connected by a psi[CH(2)O] isostere while a covalent methylene bridge replaces the hydrogen bond that is often found between residues i and i + 2 in gamma-turns. The turn mimetic was assembled from three types of building blocks: an azido epoxide, an alpha-bromo acid, and a protected beta-amino alcohol. The oxytocin analogue did not induce contractions of the uterus nor did it inhibit oxytocin-induced contractions. It is suggested that the loss of bioactivity is mainly due to the presence of a psi[CH(2)O] isostere instead of an amide bond between residues i and i + 1 in the turn mimetic.
机译：催产素是一种神经下垂体肽激素，可在哺乳动物中引起分娩和泌乳。已经合成了对应于三肽Ile-Val-Asn的逆γ-转模拟物，并代替了催产素的残基3-5，以探究在催产素的受体结合构象中发现了涉及这些残基的γ-转的假说。在转弯模拟中，残基i和i +1通过psi [CH（2）O]等排物连接，而共价亚甲基桥取代了在伽马转角中通常在残基i和i + 2之间发现的氢键。模拟转弯由三种类型的构件组装而成：叠氮基环氧化物，α-溴酸和受保护的β-氨基醇。催产素类似物既不引起子宫收缩也不抑制催产素引起的收缩。建议生物活性的损失主要是由于在模拟转弯过程中，残基i和i +1之间存在psi [CH（2）O]异构体而不是酰胺键。

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