1456708-45-4Relevant academic research and scientific papers
SsDNA templated assembly of oligonucleotides and bivalent naphthalene guests
Janssen, Pim G. A.,Brankaert, Niels J. M.,Vila, Xavier,Schenning, Albertus P. H. J.
, p. 1494 - 1502 (2010)
The hybridization of oligothymine templates with oligomeric adenine and naphthalene diaminotriazine guests has been studied by UV-vis and circular dichroism (CD) spectroscopy. First, the length of the oligothymine template and the oligoadenine guest has b
Synthetic Ion Channel Formed by Multiblock Amphiphile with Anisotropic Dual-Stimuli-Responsiveness
Sasaki, Ryo,Sato, Kohei,Tabata, Kazuhito V.,Noji, Hiroyuki,Kinbara, Kazushi
supporting information, p. 1348 - 1355 (2021/02/01)
Transmembrane proteins within biological membranes exhibit varieties of important functions that are vital for many cellular activities, and the development of their synthetic mimetics allows for deep understanding in related biological events. Inspired by the structures and functions of natural ion channels that can respond to multiple stimuli in an anisotropic manner, we developed multiblock amphiphile VF in this study. When VF was incorporated into the lipid bilayer membranes, VF formed a supramolecular ion channel whose ion transport property was controllable by the polarity and amplitude of the applied voltage. Microscopic emission spectroscopy revealed that VF changed its molecular conformation in response to the applied voltage. Furthermore, the ion transport property of VF could be reversibly switched by the addition of (R)-propranolol, an aromatic amine known as an antiarrhythmic agent, followed by the addition of β-cyclodextrin for its removal. The highly regulated orientation of VF allowed for an anisotropic dual-stimuli-responsiveness for the first time as a synthetic ion channel.
Design, Synthesis, and Pharmacological Characterization of Heterobivalent Ligands for the Putative 5-HT2A/mGlu2Receptor Complex
Poulie, Christian B. M.,Liu, Na,Jensen, Anders A.,Bunch, Lennart
, p. 9928 - 9949 (2020/09/12)
We report the synthesis of the first series of heterobivalent ligands targeting the putative heteromeric 5-HT2A/mGlu2 receptor complex, based on the 5-HT2A antagonist MDL-100,907 and the mGlu2 ago-PAM JNJ-42491293. The functional properties of monovalent and heterobivalent ligands were characterized in 5-HT2A-, mGlu2/Gqo5-, 5-HT2A/mGlu2-, and 5-HT2A/mGlu2/Gqo5-expressing HEK293 cells using a Ca2+ imaging assay and a [3H]ketanserin binding assay. Pronounced functional crosstalk was observed between the two receptors in 5-HT2A/mGlu2 and 5-HT2A/mGlu2/Gqo5 cells. While the synthesized monovalent ligands retained the 5-HT2A antagonist and mGlu2 ago-PAM functionalities, the seven bivalent ligands inhibited 5-HT-induced responses in 5-HT2A/mGlu2 cells and both 5-HT- and Glu-induced responses in 5-HT2A/mGlu2/Gqo5 cells. However, no definitive correlation between the functional potency and spacer length of the ligands was observed, an observation substantiated by the binding affinities exhibited by the compounds in 5-HT2A, 5-HT2A/mGlu2, and 5-HT2A/mGlu2/Gqo5 cells. In conclusion, while functional crosstalk between 5-HT2A and mGlu2 was demonstrated, it remains unclear how these heterobivalent ligands interact with the putative receptor complex.
NOVEL DIHYDROPYRIDINONE AND DIHYDROPYRIMIDINONE COMPOUNDS AND THEIR USE
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Page/Page column 69, (2017/12/27)
The present invention is directed to novel compounds of Formula I; pharmaceutically acceptable salts or solvates thereof, and their use.
CONJUGATES AND CONJUGATING REAGENTS COMPRISING A LINKER THAT INCLUDES AT LEAST TWO (-CH2-CH2-0-) UNITS IN A RING
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Page/Page column 49; 50, (2017/11/16)
A conjugate comprising a protein or peptide conjugated to a therapeutic, diagnostic or labelling agent via a linker, characterised in that the linker includes at least two ~(CH2-CH2- 0-)~ units within a ring, said ring being attached via a single tethering atom within the ring to the rest of the linker, or said ring being attached via two or more tethering atoms within the ring to the rest of the linker at a single point.
A cost-effective, column-free route to ethylene glycol oligomers EG 6, EG10, and EG12
Gothard, Chris M.,Grzybowski, Bartosz A.
, p. 717 - 722 (2012/04/04)
Although monodisperse ethylene glycol (EG) oligomers are important in a wide range of applications (ranging from drug therapeutics to materials science and engineering), their cost - especially for longer EG oligomers is often prohibitive. For example, decaethylene, EG10, and dodecaethylene, EG12, glycols cost hundreds of dollars per gram, and are only available from most vendors, including Sigma-Aldrich, in the polydispersed form. This high-cost is, in large part, due to laborious nature of synthesis and, above all, purification steps involved. Therefore, the motivation of our work was to design a cost-effective route to the EG oligomers that would altogether avoid the column-chromatography purification. This was achieved by a simple synthetic strategy, which combines bidirectional growth of the EG chains with the protection scheme using easy-to-remove trityl groups. Georg Thieme Verlag Stuttgart · New York.
