- GADD45BETA TARGETING AGENTS
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Compounds based around tetrapeptide, tripeptide and dipeptide moeties and corresponding peptiod moeties. Related methods and pharmaceutical compositions for use in treatment of cancer, inflammatory diseases, and other disorders.
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- Inhibitors selective for HDAC6 in enzymes and cells
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Histone deacetylase inhibitors with anticancer or anti-inflammatory activity bind to Class I or Class I and II HDAC enzymes. Here we compare selectivity of inhibitors of a Class II HDAC enzyme (HDAC6) and find one that retains high selectivity in macrophages.
- Gupta, Praveer K.,Reid, Robert C.,Liu, Ligong,Lucke, Andrew J.,Broomfield, Steve A.,Andrews, Melanie R.,Sweet, Matthew J.,Fairlie, David P.
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supporting information; experimental part
p. 7067 - 7070
(2011/01/03)
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- PREPARATION OF 6-AMINOCAPROIC ACID FROM α-KETOPIMELIC ACID
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The invention relates to a method for preparing 6-aminocaproic acid (hereinafter also referred to as '6-ACA')usinga biocatalyst. The invention further relates to a method for preparing e-caprolactam (hereafter referred to as 'caprolactam') by cyclising such 6-ACA. The invention further relates to a host cell, a micro-organism, or a polynucleotidewhich may be used inthe preparation of 6-ACA or caprolactam.
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Page/Page column 45-46
(2009/10/22)
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- INHIBITORS OF KYNURENINE AMINOTRANSFERASE AND USES THEREFOR
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Provided herein are methods of decreasing a level of kynurenic acid in a cell and of treating a pathophysiological condition in a subject associated with an increase in kynurenic acid in a subject. In these methods the inhibitory action of dicarboxylic acids or derivatives or analogs thereof are effective to inhibit activity of kynurenine aminotransferase II. Also provided is a method of screening for potential inhibitory compounds for kynurenine aminotransferase II. The dicarboxylic acids or derivatives or analogs thereof may have the structural formula, where R1 is H, NH2 or NHCH3, R2 is H or CH3, n is 0 to 14, and X is -COOH, CH2OH, -PO3H2, -SO2H, or -SO3H; or a pharmacologically acceptable salt.
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Page/Page column 21
(2008/06/13)
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- Peptides with an insulin-like action
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Peptides with an insulin-like action, of formula I: STR1 in which G is a hydrogen atom, an amino add residue, or a monosubstituted or polysubstituted amino acid; D is an amino acid residue, a phosphoamino acid residue, a monosaccharide residue, or a covalent bond; E is --NH--(CH2)n --NR52, a glycerol residue, or --NH--(CH2)p --R6 --R7 ; R1 is (C1 -C4)-alkyl or =O; R2 is a sulfhydryl protecting group, (C1 -C3)-alkyl, or a hydrogen atom; R3 and R4, independently of one another, are a hydrogen atom or methyl; R5, each being identical or different, is a hydrogen atom, 1 to 6 monosaccharide residues, or 1 to 6 monosubstituted or polysubstituted monosaccharide residues; R6 is O PO4 H, PO2 H, NHCOO, S or OCOO; R7 is a hydrogen atom, 1 to 6 monosaccharide residues, or 1 to 6 monosubstituted or polysubstituted monosaccharide residues; w is an integer 1 or 2; their preparation and use for treatment of diabetes mellitus or insulin-independent diabetes.
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