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21.
Charles Romain Charlotte K. Williams 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2014,126(6):1633-1636
A novel chemoselective polymerization control yields predictable (co)polymer compositions from a mixture of monomers. Using a dizinc catalyst and a mixture of caprolactone, cyclohexene oxide, and carbon dioxide enables the selective preparation of either polyesters or polycarbonates or copoly(ester‐carbonates). The selectivity depends on the nature of the zinc–oxygen functionality at the growing polymer chain end, and can be controlled by the addition of exogeneous switch reagents. 相似文献
22.
Dr. Karin Mannerstedt Dr. Narendra Kumar Mishra Dr. Ebbe Engholm Dr. Morten Lundh Dr. Charlotte S. Madsen Dr. Philip J. Pedersen Dr. Priska Le-Huu Dr. Søren L. Pedersen Dr. Nina Buch-Månson Dr. Björn Borgström Dr. Thomas Brimert Dr. Lisbeth N. Fink Dr. Keld Fosgerau Prof. Niels Vrang Prof. Knud J. Jensen 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(9):3166-3176
A glucose responsive insulin (GRI) that responds to changes in blood glucose concentrations has remained an elusive goal. Here we describe the development of glucose cleavable linkers based on hydrazone and thiazolidine structures. We developed linkers with low levels of spontaneous hydrolysis but increased level of hydrolysis with rising concentrations of glucose, which demonstrated their glucose responsiveness in vitro. Lipidated hydrazones and thiazolidines were conjugated to the LysB29 side-chain of HI by pH-controlled acylations providing GRIs with glucose responsiveness confirmed in vitro for thiazolidines. Clamp studies showed increased glucose infusion at hyperglycemic conditions for one GRI indicative of a true glucose response. The glucose responsive cleavable linker in these GRIs allow changes in glucose levels to drive the release of active insulin from a circulating depot. We have demonstrated an unprecedented, chemically responsive linker concept for biopharmaceuticals. 相似文献
23.
Kätchen K. Lachmayr Charlotte M. Wentz Prof. Lawrence R. Sita 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2020,132(4):1537-1542
“One-component” soft material Frank–Kasper (FK) phases are an intriguing structural form of matter that possess periodically ordered structures arising from the self-reconfiguration and close packing of an initial assembly of identical “deformable” spheres into two or more size- or shape-distinct sets of particles. Significant challenges that must still be addressed to advance the field of soft matter FK phases further, however, include their rare and unpredictable occurrence, uncertain mechanisms of solid-state assembly, and low thermodynamic stability. Here we show that a readily-accessible sugar–polyolefin conjugate quantitatively produces an exceptionally stable solid-state FK A15 phase through a rapid and irreversible thermotropic order–order transition, which contrary to other prevailing proposed mechanisms, does not require mass transfer between particles or large structural reorganization in the bulk to establish unit cell non-equivalency. Our results provide the basis for a realistic strategy for obtaining practical and scalable quantities of a diverse range of sugar–polyolefin FK A15 phases with unique intrinsic physical properties and chemical reactivities not previously seen in such systems. 相似文献
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25.
Dr. Jagadeesh Yerri Dr. José Dias Dr. Mallikajurna Reddy Nimmakayala Franck Razafindrainibe Charlotte Courageux Anne-Julie Gastellier Johanne Jegoux Dr. Caroline Coisne Dr. Christophe Landry Dr. Fabien Gosselet Johan Hachani Dr. Jean-François Goossens Prof. Marie-Pierre Dehouck Dr. Florian Nachon Dr. Rachid Baati 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(65):15035-15044
Novel 6-alkyl- and 6-alkenyl-3-fluoro-2-pyridinaldoximes have been synthesised by using a mild and efficient chemoselective hydrogenation of 6-alkynyl-3-fluoro-2-pyridinaldoxime scaffolds, without altering the reducible, unprotected, sensitive oxime functionality and the C−F bond. These novel 6-alkyl-3-fluoro-2-pyridinaldoximes may find medicinal application as antidotes to organophosphate poisoning. Indeed, one low-molecular-weight compound exhibited increased affinity for sarin-inhibited acetylcholinesterase (hAChE) and greater reactivation efficiency or resurrection for sarin-inhibited hAChE, compared with those of 2-pyridinaldoxime (2-PAM) and 1-({[4-(aminocarbonyl)pyridinio]methoxy}methyl)-2-[(hydroxyimino)methyl]pyridinium chloride (HI-6), two pyridinium salts currently used as antidote by several countries. In addition, the uncharged 3-fluorinated bifunctional hybrid showed increased in vitro blood–brain barrier permeability compared with those of 2-PAM, HI-6 and obidoxime. These promising features of novel low-molecular-weight alkylfluoropyridinaldoxime open up a new era for the design, synthesis and discovery of central non-quaternary broad spectrum reactivators for organophosphate-inhibited cholinesterases. 相似文献
26.
Niklas Jänsch Wisely Oki Sugiarto Marius Muth Aleksandra Kopranovic Charlotte Desczyk Matthias Ballweg Frank Kirschhöfer Dr. Gerald Brenner-Weiss Prof. Dr. Franz-Josef Meyer-Almes 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(58):13249-13255
Human histone deacetylase 8 is a well-recognized target for T-cell lymphoma and particularly childhood neuroblastoma. PD-404,182 was shown to be a selective covalent inhibitor of HDAC8 that forms mixed disulfides with several cysteine residues and is also able to transform thiol groups to thiocyanates. Moreover, HDAC8 was shown to be regulated by a redox switch based on the reversible formation of a disulfide bond between cysteines Cys102 and Cys153. This study on the distinct effects of PD-404,182 on HDAC8 reveals that this compound induces the dose-dependent formation of intramolecular disulfide bridges. Therefore, the inhibition mechanism of HDAC8 by PD-404,182 involves both, covalent modification of thiols as well as ligand mediated disulfide formation. Moreover, this study provides a deep molecular insight into the regulation mechanism of HDAC8 involving several cysteines with graduated capability to form reversible disulfide bridges. 相似文献
27.
28.
Analysis of non‐derivatised bacteriohopanepolyols by ultrahigh‐performance liquid chromatography/tandem mass spectrometry 下载免费PDF全文
29.
Tuning of Supramolecular Architectures of l‐Valine‐Containing Dicyanoplatinum(II) 2,2′‐Bipyridine Complexes by Metal–Metal, π–π Stacking,and Hydrogen‐Bonding Interactions 下载免费PDF全文
Heidi Li‐Ki Fu Dr. Charlotte Po Dr. Hexiang He Dr. Sammual Yu‐Lut Leung Prof. Kam Sing Wong Prof. Dr. Vivian Wing‐Wah Yam 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(33):11826-11836
A series of newly synthesized dicyanoplatinum(II) 2,2′‐bipyridine complexes exhibits self‐assembly properties in solution after the incorporation of the l ‐valine amino units appended with various hydrophobic motifs. These l ‐valine‐derived substituents were found to have critical control over the aggregation behaviors of the complexes in the solution state. On one hand, one of the complexes was found to exhibit interesting circularly polarized luminescence (CPL) signals at low temperature due to the formation of chiral spherical aggregates in the temperature‐dependent studies. On the other hand, systematic transformation from less uniform aggregates to well‐defined fibrous and rod‐like structures via Pt???Pt and π–π stacking interactions has also been observed in the mixed‐solvent studies. These changes were monitored by UV/Vis absorption, emission, circular dichroism (CD), and CPL spectroscopies, and morphologies were studied by electron microscopy. 相似文献
30.
Corrigendum: An NMR‐Driven Crystallography Strategy to Overcome the Computability Limit of Powder Structure Determination: A Layered Aluminophosphate Case 下载免费PDF全文