Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr)

Christoph T. Behrendt; Andrea Kunfermann; Victoria Illarionova; An Matheeussen; Miriam K. Pein; Tobias Gräwert; Johannes Kaiser; Adelbert Bacher; Wolfgang Eisenreich; Boris Illarionov; Markus Fischer; Louis Maes; Michael Groll; Thomas Kurz

doi:10.1021/jm200694q

Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr)

Christoph T. Behrendt
, Andrea Kunfermann
, Victoria Illarionova
, An Matheeussen
, Miriam K. Pein
, Tobias Gräwert
, Johannes Kaiser
, Adelbert Bacher
, Wolfgang Eisenreich
, Boris Illarionov
, Markus Fischer
, Louis Maes
, Michael Groll
, Thomas Kurz

Chair of Biochemistry

Heinrich-Heine-University
Technical University of Munich
Universität Hamburg
University of Antwerp

Research output: Contribution to journal › Article › peer-review

59 Scopus citations

Abstract

Reverse hydroxamate-based inhibitors of IspC, a key enzyme of the non-mevalonate pathway of isoprenoid biosynthesis and a validated antimalarial target, were synthesized and biologically evaluated. The binding mode of one derivative in complex with EcIspC and a divalent metal ion was clarified by X-ray analysis. Pilot experiments have demonstrated in vivo potential.

Original language	English
Pages (from-to)	6796-6802
Number of pages	7
Journal	Journal of Medicinal Chemistry
Volume	54
Issue number	19
DOIs	https://doi.org/10.1021/jm200694q
State	Published - 13 Oct 2011

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This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

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10.1021/jm200694q

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abstract = "Reverse hydroxamate-based inhibitors of IspC, a key enzyme of the non-mevalonate pathway of isoprenoid biosynthesis and a validated antimalarial target, were synthesized and biologically evaluated. The binding mode of one derivative in complex with EcIspC and a divalent metal ion was clarified by X-ray analysis. Pilot experiments have demonstrated in vivo potential.",

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doi = "10.1021/jm200694q",

language = "English",

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T1 - Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr)

AU - Behrendt, Christoph T.

AU - Kunfermann, Andrea

AU - Illarionova, Victoria

AU - Matheeussen, An

AU - Pein, Miriam K.

AU - Gräwert, Tobias

AU - Kaiser, Johannes

AU - Bacher, Adelbert

AU - Eisenreich, Wolfgang

AU - Illarionov, Boris

AU - Fischer, Markus

AU - Maes, Louis

AU - Groll, Michael

AU - Kurz, Thomas

PY - 2011/10/13

Y1 - 2011/10/13

N2 - Reverse hydroxamate-based inhibitors of IspC, a key enzyme of the non-mevalonate pathway of isoprenoid biosynthesis and a validated antimalarial target, were synthesized and biologically evaluated. The binding mode of one derivative in complex with EcIspC and a divalent metal ion was clarified by X-ray analysis. Pilot experiments have demonstrated in vivo potential.

AB - Reverse hydroxamate-based inhibitors of IspC, a key enzyme of the non-mevalonate pathway of isoprenoid biosynthesis and a validated antimalarial target, were synthesized and biologically evaluated. The binding mode of one derivative in complex with EcIspC and a divalent metal ion was clarified by X-ray analysis. Pilot experiments have demonstrated in vivo potential.

UR - https://www.scopus.com/pages/publications/80053909858

U2 - 10.1021/jm200694q

DO - 10.1021/jm200694q

M3 - Article

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SN - 0022-2623

VL - 54

SP - 6796

EP - 6802

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 19

ER -

Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr)

Abstract

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