Novel tetronic acid derivative

C - Chemistry – Metallurgy – 12 – P

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C12P 19/62 (2006.01) A61K 31/7048 (2006.01) A61K 35/74 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01) C07H 17/08 (2006.01)

Patent

CA 2468046

Using the expression of a molecular chaperone GRP78 as an indication, attempts have been made to search for a substance capable of controlling the expression of GRP78. As a result, versipelostatin (also called JL68) represented by the formula (I), which is a novel tetronic acid derivative having an activity of inhibiting the GRP78 expression, is isolated from a metabolite of Streptomyces versipellis 4083-SVS6 strain. This versipelostatin can be obtained by culturing the Streptomyces versipellis 4083-SVS6 strain and collecting from the culture supernatant.

L'utilisation de l'expression d'un chaperon moléculaire GRP78 en tant qu'indication a permis d'essayer de rechercher une substance permettant de commander l'expression de GRP78. Ainsi, la versipelostatine (également appelée JL68) de formule (I) qui est un nouveau dérivé d'acide tétronique présentant une activité d'inhibition de l'expression de GRP78, est isolée à partir d'un métabolite de souche de <i>Streptomyces versipellis</i> 4083-SVS36. Cette versipelostatine peut être obtenue par le biais de la culture de la souche de <i>Streptomyces versipellis</i> 4083-SVS36 et par le recueillement du surnageant de la culture.

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