Linear and cyclic alpha-melanotropin [4-10]-fragment analogues that exhibit superpotency and residual activity.
Linear and cyclic alpha-melanotropin [4-10]-fragment analogues that exhibit superpotency and residual activity.
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线性和环状 α-促黑素激素 [4-10]-片段类似物，具有超效和残留活性。
DOI：
10.1111/j.1600-0749.1989.tb00242.x
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发表时间：
1989
期刊：
影响因子：
--
通讯作者：
Castrucci,AM
中科院分区：
文献类型：
--
作者：
Hadley,ME;Marwan,MM;al-Obeidi,F;Hruby,VJ;Castrucci,AM
合成了(Ac‐Ser‐Tyr‐Ser‐Met‐Glu‐His‐Phe‐Arg‐Trp‐Gly‐Lys‐Pro‐Val‐NH2)，Ac-[Nle4，Asp5，D-Phe7，Lys10]α-MsH4-10NH2和Ac-[Nle4，Asp5，D-Phe7，Lys10]α-MsH4-10-NH2的两个类似物α-MsH4-10-NH2，并在多种生物测定中比较了它们的促黑活性。在体外青蛙和蜥蜴皮肤生物测定以及S91黑色素瘤细胞酪氨酸酶测定中确定了效价。在所有的生物测定中，两个类似物都与α-msh相同或更有效，并且与α-msh相比，其活性延长。这两个类似物对纯化的蛋白水解酶(α-胰凝乳杆菌酶、胰蛋白酶和胃酶)具有很强的耐受性。这两种多肽可以在小鼠体内局部应用并经皮渗透，导致毛囊黑素细胞内从黑色素生成到真黑素生成的转变。与线状肽相比，环状类似物显示出更强的效力、更长的活性和抗酶失活的稳定性。讨论了这些发现对进一步设计促黑激素类似物的意义，以及这些促黑激素类似物在生物医学研究中使用的可能相关性。
Two analogues of α‐MSH (Ac‐Ser‐Tyr‐Ser‐Met‐Glu‐His‐Phe‐Arg‐Trp‐Gly‐Lys‐Pro‐Val‐NH2), Ac‐[Nle4, Asp5,D‐Phe7, Lys10]α‐MSH4–10NH2and Ac‐[Nle4, Asp5,D‐Phe7, Lys10] α‐MSH4–10‐NH2, were synthesized, and the melanotropic activities of the peptides were compared in several bioassays. Potencies were determined in the in vitro frog and lizard skin bioassays and in the S91 melanoma cell tyrosinase assay. Both analogues were equipotent or more potent than α‐MSH in all bioassays, and the activities of the analogues were prolonged compared to α‐MSH. The two analogues were very resistant to inactivation by purified proteolytic enzymes (α‐chymotrypsin, trypsin, and pepsin). The two peptides could be topically applied and transdermally delivered across the skin of mice in vivo, resulting in a shift from pheomelanogenesis to eumelanogenesis within follicular melanocytes. The cyclic analogue exhibited greater potency, prolonged activity, and stability against enzyme inactivation than did the linear peptide. The significance of the findings for the further design of melanotropin analogues is discussed, as in the possible relevance of these melanotropin analogues for use in biomedical studies.
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哺乳动物酪氨酸酶的酪氨酸羟化酶活性。
影响因子：
4.8
作者：
S. Pomerantz
通讯作者：
S. Pomerantz
超强 α-促黑素细胞刺激 S91 黑色素瘤酪氨酸酶活性
影响因子：
4.1
作者：
M. Marwan;Z. A. Malek;K. Kreutzfeld;M. Hadley;B. Wilkes;V. Hruby;A. Castrucci
通讯作者：
A. Castrucci
α-促黑素激素高效活性位点类似物的生物活性比较。
影响因子：
7.3
作者：
Sawyer,TK;Hruby,VJ;Wilkes,BC;Draelos,MT;Hadley,ME;Bergsneider,M
通讯作者：
Bergsneider,M
[Nle4，D-Phe7]-α-MSH：一种超强促黑素，“不可逆”激活黑色素瘤酪氨酸酶。
影响因子：
2.1
作者：
Hadley,ME;AbdelMalek,ZA;Marwan,MM;Kreutzfeld,KL;Hruby,VJ
通讯作者：
Hruby,VJ
通过局部和注射促黑素激素刺激小鼠滤泡黑素生成。
DOI：
10.1111/1523-1747.ep12471337
发表时间：
1987
期刊：
The Journal of investigative dermatology
影响因子：
--
作者：
Levine,N;Lemus-Wilson,A;Wood,SH;AbdelMalek,ZA;Al-Obeidi,F;Hruby,VJ;Hadley,ME
通讯作者：
Hadley,ME