50515-98-5Relevant academic research and scientific papers
Chemical probes for the rapid detection of fatty-acylated proteins in mammalian cells
Hang, Howard C.,Geutjes, Ernst-Jan,Grotenbreg, Gijsbert,Pollington, Annette M.,Bijlmakers, Marie Jose,Ploegh, Hidde L.
, p. 2744 - 2745 (2007)
The attachment of lipids onto proteins modulates the activity of proteins in many biological settings. The analysis of protein lipidation, however, is challenging due to the relatively few methods for the detection of lipid-modified proteins. Here we describe the synthesis of ω-azido-fatty acids as non-radioactive chemical probes for the rapid visualization of fatty-acylated proteins in mammalian cells. Following metabolic installation of the ω-azido-fatty acids onto target proteins by cellular enzymes, fatty-acylated proteins are selectively biotinylated with a phosphine-biotin reagent via the Staudinger ligation and visualized by streptavidin blotting. Depending on the chain length of the ω-azido-fatty acids, N-myristoylated and S-palmitoylated proteins can be visualized selectively in cell lysates and on specific proteins. These chemical probes provide new tools to analyze fatty acylation of proteins in living cells. Copyright
HETEROCYCLIC DERIVATIVES
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Page/Page column 52; 112-113, (2020/08/13)
Compounds of the formula (I): Q1-Q2-Q3, in which Q1, Q2 and Q3 have the meanings indicated in Claim 1, degrade target proteins, and can be employed, inter alia, for the treatment of diseases such as cancer, multiple sclerosis, cardiovascular diseases, central nervous system injury and different forms of inflammation.
SELECTIVE PYY COMPOUNDS AND USES THEREOF
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Paragraph 0258; 0259; 0260; 0261, (2016/12/12)
The invention relates to PYY compounds having the amino acid in the position corresponding to position 30 of hPYY(1-36) substituted with tryptophan and derivatives thereof with a modifying group attached to the position corresponding to position 7 of hPYY(1-36). The compounds of the invention are selective Y2 receptor agonists. The invention also relates to pharmaceutical compositions comprising such PYY compounds and pharmaceutically acceptable excipients, as well as the medical use of the PYY compounds.
Products of cytochrome P450Biol (CYP107H1)-catalyzed oxidation of fatty acids
Cryle, Max J.,Matovic, Nick J.,de Voss, James J.
, p. 3341 - 3344 (2007/10/03)
(Matrix presented) Oxidation of tetradecanoic and hexadecanoic acids by cytochrome P450Biol (CYP107H1) produces mainly the 11-, 12-, and 13-hydroxy C14 fatty acids and the 11- to 15-hydroxy C16 fatty acids, respectively. In contrast to previous reports, terminal hydroxylation is not observed. The enantiospecificity of fatty acid hydroxylation by P450Biol was also determined, and the enzyme was shown to be moderately selective for production of the (R)-alcohols.
Pyridinecarboxamide derivatives
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, (2008/06/13)
Pyridinecarboxamide derivatives of the formula STR1 (wherein n represents an integer of 14-18, and R represents a hydrogen atom or a straight or branched C1 -C4 alkyl group) or physiologically acceptable salts thereof. The compounds have excellent inhibiting activity of cerebral edema, especially ischemic cerebral edema, and inhibiting activity of delayed death of neuronal cells (an inhibiting activity of Ca-influx in neuronal cells). Cerebral edema is a pathologic condition accompanying cerebrovascular disorders, especially the acute stage of cerebrovascular disorders and then the compounds are useful as an agent for inhibiting cerebral edema or a therapeutic agent for cerebrovascular disorders. Moreover, the compounds have no hypotensive action which is considered to be side-effect in treating the acute stage cerebrovascular disorders and hardly show a behavior suppressing action so that they are an excellent therapeutic agent for, in particular, the acute stage cerebrovascular disorders. Moreover, the compounds show a cerebral protective activity (an anti-anoxic activity), an increasing activity of cerebral blood flow, and an inhibiting activity of lipid peroxidation and these activities may lead to the increased utility as a therapeutic agent for cerebrovascular disorders.
