Solution and crystal structures of zipa and zipa complex and...

C - Chemistry – Metallurgy – 07 – K

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C07K 14/245 (2006.01) C07K 1/00 (2006.01) G01N 33/53 (2006.01)

Patent

CA 2403200

The present invention relates to the three dimensional solution and crystal structures of the C-terminal domain of ZipA ("ZipA185-328"), as well as the three dimensional crystal structure of ZipA185-328 complexed with a C-terminal region of FtsZ. These structures are critical for the design and selection of potent and selective inhibitors of ZipA/FtsZ complex activity, particularly for use as antibiotic agents against Gram negative bacteria. Also provided by the present invention are the inhibitors identified using the three dimensional structures disclosed herein.

La présente invention concerne une solution tridimensionnelle et des structures cristallines du domaine C-terminal de ZipA ("ZipA¿185-328?"), ainsi que la structure cristalline tridimensionnelle de ZipA¿185-328? complexé à une région C-terminale de FtsZ. Ces structures sont essentielles pour la conception et la sélection d'inhibiteurs puissants et sélectifs de l'activité du complexe ZipA/FtsZ, notamment en vue d'une utilisation comme agents antibiotiques dirigés contre les bactéries Gram-négatives. La présente invention concerne également des inhibiteurs identifiés au moyen des structures tridimensionnelles susmentionnées.

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