Diarylquinolines target subunit c of mycobacterial ATP synthase.

A. Koul; N. Dendouga; B. Molenberghs; L. Vranckx; R. Willebrords; Z. Ristic; H. Lill; I. Dorange; J. Guillemont; D. Bald; K. Andries

doi:10.1038/nchembio884

Diarylquinolines target subunit c of mycobacterial ATP synthase.

A. Koul
, N. Dendouga
, B. Molenberghs
, L. Vranckx
, R. Willebrords
, Z. Ristic
, H. Lill
, I. Dorange
, J. Guillemont
, D. Bald
, K. Andries

Research output: Contribution to Journal › Article › Academic › peer-review

Abstract

The diarylquinoline R207910 (TMC207) is a promising candidate in clinical development for the treatment of tuberculosis. Though R207910-resistant mycobacteria bear mutations in ATP synthase, the compound's precise target is not known. Here we establish by genetic, biochemical and binding assays that the oligomeric subunit c (AtpE) of ATP synthase is the target of R207910. Thus targeting energy metabolism is a new, promising approach for antibacterial drug discovery. © 2007 Nature Publishing Group.

Original language	English
Pages (from-to)	323-324
Journal	Nature Chemical Biology
Volume	3
DOIs	https://doi.org/10.1038/nchembio884
Publication status	Published - 2007

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10.1038/nchembio884

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abstract = "The diarylquinoline R207910 (TMC207) is a promising candidate in clinical development for the treatment of tuberculosis. Though R207910-resistant mycobacteria bear mutations in ATP synthase, the compound's precise target is not known. Here we establish by genetic, biochemical and binding assays that the oligomeric subunit c (AtpE) of ATP synthase is the target of R207910. Thus targeting energy metabolism is a new, promising approach for antibacterial drug discovery. {\textcopyright} 2007 Nature Publishing Group.",

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doi = "10.1038/nchembio884",

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T1 - Diarylquinolines target subunit c of mycobacterial ATP synthase.

AU - Koul, A.

AU - Dendouga, N.

AU - Molenberghs, B.

AU - Vranckx, L.

AU - Willebrords, R.

AU - Ristic, Z.

AU - Lill, H.

AU - Dorange, I.

AU - Guillemont, J.

AU - Bald, D.

AU - Andries, K.

PY - 2007

Y1 - 2007

N2 - The diarylquinoline R207910 (TMC207) is a promising candidate in clinical development for the treatment of tuberculosis. Though R207910-resistant mycobacteria bear mutations in ATP synthase, the compound's precise target is not known. Here we establish by genetic, biochemical and binding assays that the oligomeric subunit c (AtpE) of ATP synthase is the target of R207910. Thus targeting energy metabolism is a new, promising approach for antibacterial drug discovery. © 2007 Nature Publishing Group.

AB - The diarylquinoline R207910 (TMC207) is a promising candidate in clinical development for the treatment of tuberculosis. Though R207910-resistant mycobacteria bear mutations in ATP synthase, the compound's precise target is not known. Here we establish by genetic, biochemical and binding assays that the oligomeric subunit c (AtpE) of ATP synthase is the target of R207910. Thus targeting energy metabolism is a new, promising approach for antibacterial drug discovery. © 2007 Nature Publishing Group.

U2 - 10.1038/nchembio884

DO - 10.1038/nchembio884

M3 - Article

SN - 1552-4450

VL - 3

SP - 323

EP - 324

JO - Nature Chemical Biology

JF - Nature Chemical Biology

ER -

Diarylquinolines target subunit c of mycobacterial ATP synthase.

Abstract

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