1456708-45-4Relevant articles and documents
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
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.
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.
