Rojas-Pierce Marcela, Titapiwatanakun Boosaree, Sohn Eun Ju, Fang Fang, Larive Cynthia K, Blakeslee Joshua, Cheng Yan, Cutler Sean R, Peer Wendy A, Murphy Angus S, Raikhel Natasha V
Department of Botany and Plant Sciences, University of California, Riverside, Riverside, CA 92521, USA.
Chem Biol. 2007 Dec;14(12):1366-76. doi: 10.1016/j.chembiol.2007.10.014.
ATP-binding cassette (ABC) transporters have been implicated in a multitude of biological pathways. In plants, some ABC transporters are involved in the polar transport of the plant hormone auxin and the gravitropic response. We previously identified Gravacin as a potent inhibitor of gravitropism in Arabidopsis thaliana. We demonstrate that P-glycoprotein19 (PGP19) is a target for Gravacin and participates in its inhibition of gravitropism. Gravacin inhibited the auxin transport activity of PGP19 and PGP19-PIN complexes. Furthermore, we identified E1174 as an important residue for PGP19 activity and its ability to form active transport complexes with PIN1. Gravacin is an auxin transport inhibitor that inhibits PGPs, particularly PGP19, which can be used to further dissect the role of PGP19 without the inhibition of other auxin transporters, namely PIN proteins.
ATP结合盒（ABC）转运蛋白参与了多种生物途径。在植物中，一些ABC转运蛋白参与植物激素生长素的极性运输和向重力性反应。我们之前鉴定出重力蛋白是拟南芥向重力性的有效抑制剂。我们证明P-糖蛋白19（PGP19）是重力蛋白的作用靶点，并参与其对向重力性的抑制作用。重力蛋白抑制了PGP19和PGP19-PIN复合物的生长素运输活性。此外，我们确定E1174是PGP19活性及其与PIN1形成主动运输复合物能力的重要残基。重力蛋白是一种生长素运输抑制剂，可抑制PGP，尤其是PGP19，它可用于在不抑制其他生长素转运蛋白（即PIN蛋白）的情况下进一步剖析PGP19的作用。
