82909-47-5Relevant articles and documents
INSULIN CONJUGATES
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, (2020/07/05)
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.
METHODS FOR THE DETECTION OF FATTY-ACYLATED PROTEIN
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, (2010/08/07)
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.
Robust fluorescent detection of protein fatty-acylation with chemical reporters
Charron, Guillaume,Zhang, Mingzi M.,Yount, Jacob S.,Wilson, John,Raghavan, Anuradha S.,et al.
supporting information; scheme or table, p. 4967 - 4975 (2009/09/29)
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
N-Myristoyl transferase-mediated protein labelling in vivo
Heal, William P.,Wickramasinghe, Sasala R.,Leatherbarrow, Robin J.,Tate, Edward W.
experimental part, p. 2308 - 2315 (2009/02/02)
N-Myristoyl transferase-mediated labelling using a substrate modified with an azide or alkyne tag is described as an efficient and site-selective method for the introduction of a bioorthogonal tag at the N-terminus of a recombinant protein. The procedure may be performed in vitro, or in a single over-expression/tagging step in vivo in bacteria; tagged proteins may then be captured using Staudinger-Bertozzi or 'click' chemistry protocols to introduce a secondary label for downstream analysis. The straightforward synthesis of the chemical and molecular biological tools described should enable their use in a wide range of N-terminal labelling applications.
Synthesis of carboxyl-tethered symmetric conjugated polyenes as fluorescent transmembrane probes of lipid bilayers
Quesada, Ernesto,Acuna, A. Ulises,Amat-Guerri, Francisco
, p. 1308 - 1318 (2007/10/03)
The synthesis of a new series of fluorescent transmembrane probes in which two hydrophilic methyl ester or carboxyl groups are connected by a polymethylene chain, with four, five or six conjugated double bonds in a central position, is reported. The length of the linear structures was designed to match the width of typical lipid bilayers. These bolaamphiphilic compounds result, with overall yields higher than 80%, from an easy PdII-catalyzed double cross-coupling between terminal acetylene esters and conjugated 1,ω-dihalopolyenes, followed by selective triple bond partial reduction with activated zinc, and iodine isomerization to the all-(E) isomer. An alternative approach, based on a Stille double cross-coupling between the appropriate all-(E)-ω-halopolyenes and (E)-bis(tributylstannyl)ethene, yielded mixtures that could not be resolved by standard chromatographic methods due to the presence of other simultaneous coupling reactions, which are also discussed in detail. Nevertheless, the Stille method can be of utility for the obtention of carbonyl-polyene conjugated analogs. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.
Synthesis and thermotropic properties of macrocyclic lipids related to archaebacterial membranes
Menger,Chen,Brocchini,Hopkins,Hamilton
, p. 6600 - 6608 (2007/10/02)
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.
A GENERAL METHOD FOR THE SYNTHESIS OF DIACETYLENIC ACIDS
Singh, Alok,Schnur, Joel M.
, p. 847 - 852 (2007/10/02)
A simple and convenient method for the synthesis of twelve novel alkadiynoic acids, HOOC(CH2)mCC-C-CC(CH2)n-CH3, is reported.
Isomerization of acetylenic acids with sodium salt of 1,2-diaminoethane: a one step synthesis of megatomic acid
Abrams, S. R.
, p. 1238 - 1243 (2007/10/02)
A number of isomeric tetradecynoic acids were isomerized with the sodium salt of 1,2-diaminoethane.Isomers having the triple bond near the carboxyl group rearranged to E,Z-3,5- and E,E-3,5-tetradecadienoic acids (1 and 2), the former compound being the sex pheromone of the black carpet beetle.Isomers having the triple bond closer to the terminus of the chain afforded some 13-tetradecynoic acid along with 1 and 2.Delocalized anions 12 and 13 are thought to contribute to the formation of 1 and 2.
