- Preparation method of long-chain diacid
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The invention provides a preparation method of long-chain diacid, which comprises the following steps of: (S1) carrying out an addition reaction on olefine acid or an ester derivative thereof serving as a raw material and liquid bromine to obtain dibromo carboxylic acid or an ester derivative thereof; (S2) carrying out an elimination reaction on the dibromo carboxylic acid or ester derivative thereof under the action of sodium amide to obtain alkynyl-terminated carboxylic acid or an ester derivative thereof; (S3) carrying out an addition reaction on the alkynyl-terminated carboxylic acid or the ester derivative thereof and diborane to obtain borane or boric acid containing carboxyl or ester group; and (S4) oxidizing the borane or boric acid to obtain long-chain diacid. According to the invention, olefine acid is used as a raw material, is easily available in source and low in price, so that the production cost of the product is very low; and meanwhile, the raw materials used in the synthesis process do not contain precious metals or other expensive reagents, so that the synthesis process is suitable for industrial amplification production, and the defect that the method in the prior art is not environment-friendly, not suitable for industrial production and high in preparation cost is overcome.
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- INSULIN CONJUGATES
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The present invention relates to a conjugate comprising a sulfonamide of formula (I) and an active pharmaceutical ingredient such as an insulin analog comprising at least one mutation relative to the parent insulin, wherein the insulin analog comprises a mutation at position B16 which is substituted with a hydrophobic amino acid and/or a mutation at position B25 which is substituted with a hydrophobic amino acid. The present invention further relates to a sulfonamide of formula (A). Moreover, the present invention relates to an insulin analog comprising at least one mutation relative to the parent insulin.
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Paragraph 0580; 0592-0595; 0596
(2020/07/05)
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- Effect of carbon chain length in acyl coenzyme A on the efficiency of enzymatic transformation of okadaic acid to 7-O-acyl okadaic acid
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Okadaic acid (OA), a product of dinoflagellate Prorocentrum spp., is transformed into 7-O-acyl OA in various bivalve species. The structural transformation proceeds enzymatically in vitro in the presence of the microsomal fraction from the digestive gland of bivalves. We have been using LC-MS/MS to identify OA-transforming enzymes by detecting 7-O-acyl OA, also known as dinophysistoxin 3 (DTX3). However, an alternative assay for DTX3 is required because the OA-transforming enzyme is a membrane protein, and surfactants for solubilizing membrane proteins decrease the sensitivity of LC-MS/MS. The present study examined saturated fatty acyl CoAs with a carbon chain length of 10 (decanoyl), 12 (dodecanoyl), 14 (tetradecanoyl), 16 (hexadecanoyl) and 18 (octadecanoyl) as the substrate for the in vitro acylation reaction. Saturated fatty acyl CoAs with a carbon chain length of 14, 16 and 18 exhibited higher yields than those with a carbon chain length of 10 or 12. Acyl CoAs with carbon chain lengths from 14 to 18 and containing either a diene unit, an alkyne unit, or an azide unit in the carbon chain were synthesized and shown to provide the corresponding DTX3 with a yield comparable to that of hexadecanoyl CoA. The three functional units can be conjugated with fluorescent reagents and are applicable to the development of a novel assay for DTX3.
- Furumochi, Sachie,Onoda, Tatsuya,Cho, Yuko,Fuwa, Haruhiko,Sasaki, Makoto,Yotsu-Yamashita, Mari,Konoki, Keiichi
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p. 2992 - 2996
(2016/06/13)
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- METHODS FOR THE DETECTION OF FATTY-ACYLATED PROTEIN
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Sensitive, non-radioactive fatty-acyls of Formula I are useful in in vivo methods for detection and cellular imaging of a fatty-acylated substrate (e.g., protein or polypeptide). In Formula I the symbols X and A, and the subscript n are as described herein. These fatty-acyl compounds are can be used, inter alia, for analyzing the lipid composition of proteins in different biological states under various cellular conditions, and serve as a gateway into global lipidomic analysis of cellular proteins.
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- Robust fluorescent detection of protein fatty-acylation with chemical reporters
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Fatty-acylation of proteins in eukaryotes is associated with many fundamental cellular processes but has been challenging to study due to limited tools for rapid and robust detection of protein fatty-acylation in cells. The development of azido-fatty acid
- Charron, Guillaume,Zhang, Mingzi M.,Yount, Jacob S.,Wilson, John,Raghavan, Anuradha S.,et al.
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supporting information; scheme or table
p. 4967 - 4975
(2009/09/29)
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- Synthesis of Ceramide Mimics with a Pseudo Cyclic Framework
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We have designed and synthesized ceramide mimics with a pseudo cyclic framework that can be converted to 'dimeric' sphingomyelins and glycosphingolipids for potential components of artificial rafts. These molecules are characterized by the presence of (i) two hydrophilic head groups, (ii) a covalently bonded hydrocarbon chain, and (iii) two untethered alkyl chains. Self-assembling of a ceramide mimic into nanorods is briefly discussed.
- Suzuki, Hikokazu,Mori, Michiko,Shibakami, Motonari
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p. 2163 - 2166
(2007/10/03)
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- Synthesis and thermotropic properties of macrocyclic lipids related to archaebacterial membranes
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Macrocyclic phospholipids containing 32-44 ring atoms were synthesized by a route involving a high-temperature Glaser oxidation as the key step. These lipids are analogous to mammalian phospholipids except a single extra carboncarbon bond joins the chain termini. The new lipids offered, therefore, an opportunity to examine thermotropic properties of their membranes when the chains within a given molecule are unable to move independently of one another. It was concluded that chain "tethering" (a) raises the transition temperatures substantially for all but the shortest lipids, (b) lowers enthalpies of transition by, in part, reducing the number of gauche C-C linkages created during the melting process, and (c) lowers entropies of transition by impeding motional freedom within the liquid-crystalline phase. Molecular mechanics calculations on the macrocyclic lipids are described briefly.
- Menger,Chen,Brocchini,Hopkins,Hamilton
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p. 6600 - 6608
(2007/10/02)
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