5693-80-1Relevant academic research and scientific papers
Glycosyl-Substituted Dicarboxylates as Detergents for the Extraction, Overstabilization, and Crystallization of Membrane Proteins
Nguyen, Kim-Anh,Peuchmaur, Marine,Magnard, Sandrine,Haudecoeur, Romain,Boyère, Cédric,Mounien, Saravanan,Benammar, Ikram,Zampieri, Veronica,Igonet, Sébastien,Chaptal, Vincent,Jawhari, Anass,Boumendjel, Ahcène,Falson, Pierre
supporting information, p. 2948 - 2952 (2018/02/19)
To tackle the problems associated with membrane protein (MP) instability in detergent solutions, we designed a series of glycosyl-substituted dicarboxylate detergents (DCODs) in which we optimized the polar head to clamp the membrane domain by including, on one side, two carboxyl groups that form salt bridges with basic residues abundant at the membrane–cytoplasm interface of MPs and, on the other side, a sugar to form hydrogen bonds. Upon extraction, the DCODs 8 b, 8 c, and 9 b preserved the ATPase function of BmrA, an ATP-binding cassette pump, much more efficiently than reference or recently designed detergents. The DCODs 8 a, 8 b, 8 f, 9 a, and 9 b induced thermal shifts of 20 to 29 °C for BmrA and of 13 to 21 °C for the native version of the G-protein-coupled adenosine receptor A2AR. Compounds 8 f and 8 g improved the diffraction resolution of BmrA crystals from 6 to 4 ?. DCODs are therefore considered to be promising and powerful tools for the structural biology of MPs.
Copper-Catalyzed Bromination of C(sp3)?H Bonds Distal to Functional Groups
Liu, Tao,Myers, Michael C.,Yu, Jin-Quan
supporting information, p. 306 - 309 (2016/12/30)
Selective bromination of γ-methylene C(sp3)?H bonds of aliphatic amides and δ-methylene C(sp3)?H bonds of nosyl-protected alkyl amines are developed using NBS as the brominating reagent and catalytic amount of CuII/phenanthroline complexes as the catalyst. Aryl and benzylic C?H bonds at other locations remain intact during this directed radical abstraction reaction.
3-heterocyclylpropanohydroxamic acid PCP inhibitors
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, (2008/06/13)
Compounds of formula (I): and their salts, solvates, hydrates and prodrugs are useful PCP inhibitors, processes for making the same, compositions comprising the same, and methods of treating a PCP-mediated condition or disease using the same.
3-heterocyclylpropanohydroxamic acid PCP inhibitors
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, (2008/06/13)
Compounds of formula (I) and their salts, solvates and prodrugs, wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.
3-ox(adi) azolylpropanohydroxamic acids useful as procollagen C- Proteinase inhibitors
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, (2008/06/13)
Compounds of formula (I): wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP.
PROCOLLAGEN C-PROTEINASE INHIBITORS
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, (2008/06/13)
and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.
