57436-38-1Relevant academic research and scientific papers
An electrochemically controlled supramolecular zip tie based on host-guest chemistry of CB[8]
Barriada, Jose L.,Domarco, Olaya,Franchi, Paola,García, Marcos D.,Lucarini, Marco,Neira, Iago,Peinador, Carlos
supporting information, p. 5228 - 5233 (2020/07/23)
Three molecular threads incorporating two viologen units attached by an oligo-ethylene glycol chain of variable length and an electron rich naphthalene moiety were prepared. The internal viologen unit is connected to the naphthalene by a rigid linker that
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.
BIS(2-HALOACETAMIDO)-COMPOUNDS FOR USE AS LINKING AGENTS AND RESULTANT PRODUCTS WHICH COMPRISE ANTIBODIES, HALF-ANTIBODIES AND ANTIBODY FRAGMENTS
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Page/Page column 27; 37-38, (2021/01/23)
Bis(2-haloacetamido)- compounds for use as linkers to chemically cross-linking multiple thiol groups, and particularly, although not exclusively, the thiol groups of cysteine amino acids in peptide chains are described, along with their use as linking age
NOVEL DIHYDROPYRIDINONE AND DIHYDROPYRIMIDINONE COMPOUNDS AND THEIR USE
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Page/Page column 66; 67, (2017/12/27)
The present invention is directed to novel compounds of Formula I; pharmaceutically acceptable salts or solvates thereof, and their use.
SMALL MOLECULE BASED ANTIBODY-RECRUITING COMPOUNDS FOR CANCER TREATMENT
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Page/Page column 56; 57, (2017/03/08)
The present invention relates to chimeric (including bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds bind to the urokinase-type plasminogen activator receptor (uPAR) on the surface of a cancer cell, including a metastatic cancer cell, and consequently recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and antibody-dependent cellular cytotoxicity (ADCC) and/or complement dependent cytotoxicity (CDC) against a large number and variety of cancers, thus providing cancer cell death and an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.
Re-engineering the Immune Response to Metastatic Cancer: Antibody-Recruiting Small Molecules Targeting the Urokinase Receptor
Rullo, Anthony F.,Fitzgerald, Kelly J.,Muthusamy, Viswanathan,Liu, Min,Yuan, Cai,Huang, Mingdong,Kim, Minsup,Cho, Art E.,Spiegel, David A.
supporting information, p. 3642 - 3646 (2016/03/23)
Developing selective strategies to treat metastatic cancers remains a significant challenge. Herein, we report the first antibody-recruiting small molecule (ARM) that is capable of recognizing the urokinase-type plasminogen activator receptor (uPAR), a uniquely overexpressed cancer cell-surface marker, and facilitating the immune-mediated destruction of cancer cells. A co-crystal structure of the ARM-U2/uPAR complex was obtained, representing the first crystal structure of uPAR complexed with a non-peptide ligand. Finally, we demonstrated that ARM-U2 substantially suppresses tumor growth in vivo with no evidence of weight loss, unlike the standard-of-care agent doxorubicin. This work underscores the promise of antibody-recruiting molecules as immunotherapeutics for treating cancer.
Efficient synthesis of Hsp90 inhibitor dimers as potential antitumor agents
Sekiguchi, Hironori,Muranaka, Kazuhiro,Osada, Akiko,Ichikawa, Satoshi,Matsuda, Akira
experimental part, p. 5732 - 5737 (2010/09/11)
The PU-H58-dimers 13a-15b were efficiently synthesized and their biological properties were evaluated. The copper-catalyzed alkyne azide coupling was effective in simultaneously linking three components via a triazole formation to afford the target dimers
Macrocyclic receptor molecules with a pendant carboxylic acid group for the complexation of urea
Aarts, Veronika M. L. J.,Grootenhuis, Peter D. J.,Reinhoudt, David N.,Czech, Anna,Czech, Bronislaw P.,Bartsch, Richard A.
, p. 94 - 104 (2007/10/02)
The synthesis of 5,5'-di-tert-butyl-3-(carboxymethyl)biphenyl crown ethers and several lariat ethers with pendant carboxylic acid groups, together with the determinations of the pKa values of these crown ether carboxylic acids, are described.In
