Active core structure of terfestatin A, a new specific inhibitor of auxin signaling

The auxins, plant hormones, regulate many aspects of the growth and development of plants. Terfestatin A (TrfA), a novel auxin signaling inhibitor, was identified in a screen of Streptomyces sp. F40 extracts for inhibition of the expression of an auxin-inducible gene. However, the mode of action of TrfA has not been elucidated. To identify the active core structure, 25 derivatives of TrfA were synthesized and their inhibitory activities against auxin-inducible gene expression were evaluated. The structure activity relationships revealed the essential active core structure of TrfA, 3-butoxy-4-methylbiphenyl-2,6-diol, which will lead to the design of biotin-tagged active TrfA. (C) 2008 Elsevier Ltd. All rights reserved.

生长素是植物激素，调节植物生长和发育的许多方面。特非司他汀A（TrfA）是一种新型的生长素信号传导抑制剂，是在对链霉菌F40提取物进行筛选以抑制生长素诱导基因表达的过程中被发现的。然而，TrfA的作用方式尚未阐明。为了确定活性核心结构，合成了25种TrfA衍生物，并评估了它们对生长素诱导基因表达的抑制活性。构效关系揭示了TrfA的基本活性核心结构，即3 - 丁氧基 - 4 - 甲基联苯 - 2,6 - 二醇，这将有助于设计生物素标记的活性TrfA。（C）2008爱思唯尔有限公司。保留所有权利。