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US 7,989,416 B2Granted
Lantibiotic biosynthetic gene clusters from A. garbadinensis and A. Liguriae
AssigneeNovacta Biosystems Limited
InventorsSteven Boakes, Jesus Cortes Bargallo, Michael John Dawson
Life of this patent
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Abstract
Characterization of the biosynthetic gene cluster for the lantibiotic actagardine, identification of a novel variant of actagardine and its biosynthetic cluster, and methods of production and use of actagardine are described.
Claims15
A compound of the formula:
- wherein:
- -X1-X2- represent -Leu-Val-, -Val-Val- or -Leu-Ile-;
- Y is —S— or —S(O)—;
- Z is either —NH2 or an amino acid;
- and
- R represents the group —OH or —NR1R2, wherein R1 and R2 independently represent:
- (i) hydrogen;
- (ii) a group of formula —(CH2)n—NR3R4, in which n represents an integer from 2 to 8 and R3 and R4 independently represent hydrogen or (C1-C4) alkyl, or R3 and R4 taken together represent —(CH2)3—, —(CH2)4—, (CH2)2—O—(CH2)2—, —(CH2)2—S—(CH2)2— or —(CH2)5—;
- or R1 and R2 taken together with the adjacent nitrogen atom represent a piperazine which may be substituted in position 4 with a substituent selected from:
- (a) (C1-C4)alkyl;
- (b) (C5-C7)-cycloalkyl,
- (c) pyridyl,
- (d) —(CH2)p—NR5R6 in which p represents an integer from 1 to 8 and R5 and R6 independently represent hydrogen or (C1-C4) alkyl,
- (e) piperidinyl,
- (f) substituted piperidinyl, wherein the substituted piperidinyl bears a N-substituent which is (C1-4)alkyl,
- (g) benzyl, and
- (h) substituted benzyl, wherein a phenyl therein bears 1 or 2 substituents selected from chloro, bromo, nitro, (C1-C4)alkyl and (C1-C4)alkoxy;
- or a biologically active variant thereof wherein 1, 2, 3 or 4 amino acids at positions 2, 3, 4, 5, 8, 10, 11, 13 or 18 are substituted by another amino acid, and the another amino acid is a naturally occurring amino acid or its D-isoform, or a pharmaceutically acceptable salt of said compound or variant.
15 more elements
Dependencies are inferred from the claim text.