UM
Antagonism of mTOR activity by a kinetically inert rhodium(III) complex
Zhong H.-J.; Leung K.-H.; Liu L.-J.; Lu L.; Chan D.S.-H.; Leung C.-H.; Ma D.-L.
2014
Source PublicationChemPlusChem
ISSN21926506
Volume79Issue:4Pages:508
AbstractKinetically inert Group 9 metal complexes have found emerging use as inhibitors of protein kinases or as modulators of protein-protein interactions. A series of cyclometalated rhodium(III) and iridium(III) complexes was investigated as inhibitors of mammalian target of rapamycin (mTOR) activity. Cell-free and cell-based experiments revealed rhodium(III) complex 1 to be a potent mTOR inhibitor (IC50=0.01 μM in the cell-free system), with potency comparable to that of rapamycin. The inhibition by complex 1 was found to be dependent on FK506-binding protein 12 (FKBP12), which suggests that complex 1 may behave as a modulator of the mTOR-FKBP12 interaction. Preliminary structure-activity relationships indicated that the donor ligand and the nature of the metal center are important determinants for mTOR inhibitory activity. Rhodium(III) complex 1 represents the first metal-based inhibitor of mTOR activity, and demonstrates the potential of kinetically inert Group 9 complexes as protein-protein interaction modulators. Limiting activity: The first metal-based inhibitor of mammalian target of rapamycin (mTOR) activity has been found. The cyclometalated rhodium(III) complex 1 (see scheme) inhibits mTOR activity in cell-free and cell-based systems. The size and hydrophobicity of the N N donor ligand and the nature of the metal center are determinants for mTOR inhibitory activity. The inhibitory effect of 1 is also dependent on FK506-binding protein 12. Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Keywordbioorganometallic chemistry Group 9 metal complexes inhibitors rhodium structure-activity relationships
DOI10.1002/cplu.201400014
URLView the original
Language英语
The Source to ArticleScopus
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被引频次[WOS]:25   [WOS记录]     [WOS相关记录]
Document TypeJournal article
专题University of Macau
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Zhong H.-J.,Leung K.-H.,Liu L.-J.,et al. Antagonism of mTOR activity by a kinetically inert rhodium(III) complex[J]. ChemPlusChem,2014,79(4):508.
APA Zhong H.-J..,Leung K.-H..,Liu L.-J..,Lu L..,Chan D.S.-H..,...&Ma D.-L..(2014).Antagonism of mTOR activity by a kinetically inert rhodium(III) complex.ChemPlusChem,79(4),508.
MLA Zhong H.-J.,et al."Antagonism of mTOR activity by a kinetically inert rhodium(III) complex".ChemPlusChem 79.4(2014):508.
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