| US 7,534,742 B2 | ||
| Isoprenoid biosynthesis | ||
| Wolfgang Eisenreich, Prälat-Michael-Höck-Str. 27, D-85354 Freising (Germany); Monika Fellermeier, Eichenweg 6, D-83556 Griesstaett (Germany); Markus Fischer, Rupperstr. 10, D-80337 München (Germany); Stefan Hecht, Ganghofer Str. 4a, D-83043 Bad Aibling (Germany); Stefan Herz, Albrechtsstr. 32, D-80636 München (Germany); Klaus Kis, Beustweg 3, CH-8032 Zürich (Switzerland); Holger Lüttgen, Fritz-von-Briesen-Str. 22, D-69151 Neckargemünd (Germany); Felix Rohdich, Moosburger Str. 16, D-85406 Zolling (Germany); Silvia Sagner, Hess Str. 41, D-80798 München (Germany); Christoph A. Schuhr, Carl-Benz-Str. 39 A, D-68167 Mannheim (Germany); Jurathip Wungsintaweekul, Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112 (Thailand); Adelbert Bacher, Köigsberger Str. 74, D-85748 Garching (Germany); and Meinhart H. Zenk, Carl-von-Ossietzky-Str. 14, D-Halle/Saale (Germany) | ||
| Filed on Sep. 25, 2006, as Appl. No. 11/526,318. | ||
| Application 11/526318 is a division of application No. 10/048874, granted, now 7,122,331, previously published as PCT/EP00/07548, filed on Aug. 03, 2000. | ||
| Claims priority of application No. 199 36 663 (DE), filed on Aug. 04, 1999; application No. 199 45 174 (DE), filed on Sep. 21, 1999; application No. 199 45 175 (DE), filed on Sep. 21, 1999; application No. 199 48 887 (DE), filed on Oct. 11, 1999; application No. 199 53 309 (DE), filed on Nov. 05, 1999; and application No. 100 20 996 (DE), filed on Apr. 28, 2000. | ||
| Prior Publication US 2007/0015216 A1, Jan. 18, 2007 | ||
| Int. Cl. C40B 30/04 (2006.01) | ||
| U.S. Cl. 506—9 [435/7.4; 506/12; 506/23] | 6 Claims |
| 1. A method for screening a chemical library for an inhibitor of the biosynthesis of isoprenoids by blocking the conversion
of 4-diphosphocytidyl-2C-methyl-D-erythritol, comprising:
(a) reacting an aqueous mixture comprising:
i) a protein that is enzymatically functional for the conversion of 4-diphosphocytidyl-2C-methyl-D-erythritol,
ii) 4-diphosphocytidyl-2C-methyl-D-erythritol or a source thereof selected from the group consisting of glyceraldehyde-3-phosphate,
pyruvate, 1-deoxy-D-xylulose 5-phosphate, and 2C-methyl-D-erythritol-4-phosphate, and
iii) a divalent metal salt;
for a predetermined period of time at a predetermined temperature;
(b) detecting the level of conversion of 4-diphosphocytidyl-2C-methyl-D-erythritol in step (a);
(c) repeating steps (a) and (b) in the presence of a test sample of the chemical library;
(d) detecting the level of conversion of 4-diphosphocytidyl-2C-methyl-D-erythritol in step (c); and
(e) comparing the level of conversion in step (b) with the level of conversion in step (d), whereby a decrease in the level
of conversion in step (d) identifies the test sample as an inhibitor of the biosynthesis of isoprenoids by blocking the conversion
of 4-diphosphocytidyl-2C-methyl-D-erythritol.
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