COMBINATORIAL DIFFUSION ASSAY USED TO IDENTIFY TOPICALLY ACTIVE MELANOCYTE-STIMULATING HORMONE-RECEPTOR ANTAGONISTS

被引：54

作者：

QUILLAN, JM ^{[1
]}

JAYAWICKREME, CK ^{[1
]}

LERNER, MR ^{[1
]}

机构：

[1] YALE UNIV,SCH MED,BOYER CTR MOLEC MED,DEPT INTERNAL MED,NEW HAVEN,CT 06536

来源：

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA | 1995年 / 92卷 / 07期

关键词：

SYNTHETIC COMBINATORIAL; CHEMISTRY; XENOPUS LAEVIS; SKIN TONE;

D O I：

10.1073/pnas.92.7.2894

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

alpha-Melanocyte-stimulating hormone (alpha-MSH) is implicated in pigmentation, central nervous system and immune system functions, growth, mitogenisis, and melanoma. Evaluation of these roles has been hindered by the lack of alpha-MSH antagonists. A combinatorial chemistry-based diffusion assay is used to find random tripeptides that antagonize normal frog and human melanoma MSH receptors and to identify pharmacological groups responsible for receptor interaction. The alpha-MSH antagonist D-Trp-Arg-Leu-NH2 is used to demonstrate directly the contribution of MSH to normal skin tone in frogs following injection or topical application.

引用

页码：2894 / 2898

页数：5

共 29 条

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