6251-30-5Relevant articles and documents
A highly fluorescent nucleoside analog based on thieno[3,4-d]pyrimidine senses mismatched pairing
Srivatsan, Seergazhi G.,Weizman, Haim,Tor, Yitzhak
, p. 1334 - 1338 (2008)
A highly emissive nucleobase analog, based on a thieno[3,4-d]pyrimidine core, is enzymatically incorporated into RNA oilgonucleotides that function as base discriminating fluorescent probes. The Royal Society of Chemistry.
Real-Time Monitoring of Human Guanine Deaminase Activity by an Emissive Guanine Analog
Bucardo, Marcela S.,Wu, You,Ludford, Paul T.,Li, Yao,Fin, Andrea,Tor, Yitzhak
, p. 1208 - 1214 (2021/07/26)
Guanine deaminase (GDA) deaminates guanine to xanthine. Despite its significance, the study of human GDA remains limited compared to other metabolic deaminases. As a result, its substrate and inhibitor repertoire are limited, and effective real-time activity, inhibitory, and discovery assays are missing. Herein, we explore two emissive heterocyclic cores, based on thieno[3,4-d]pyrimidine (thN) and isothiazole[4,3-d]pyrimidine (tzN), as surrogate GDA substrates. We demonstrate that, unlike the thieno analog, thGN, the isothiazolo guanine surrogate, tzGN, does undergo effective enzymatic deamination by GDA and yields the spectroscopically distinct xanthine analog, tzXN. Further, we showcase the potential of this fluorescent nucleobase surrogate to provide a visible spectral window for a real-time study of GDA and its inhibition.
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1 H,3 H)-dione: Synthesis, molecular modeling, and pharmacological and biostructural characterization
Venskutonytè, Raminta,Butini, Stefania,Sanna Coccone, Salvatore,Gemma, Sandra,Brindisi, Margherita,Kumar, Vinod,Guarino, Egeria,Maramai, Samuele,Valenti, Salvatore,Amir, Ahmad,Valadés, Elena Antón,Frydenvang, Karla,Kastrup, Jette S.,Novellino, Ettore,Campiani, Giuseppe,Pickering, Darryl S.
, p. 4793 - 4805 (2011/10/01)
The physiological function of kainate receptors (GluK1-GluK5) in the central nervous system is not fully understood yet. With the aim of developing potent and selective GluK1 ligands, we have synthesized a series of new thiophene-based GluK1 agonists (6a-c) and antagonists (7a-d). Pharmacological evaluation revealed that they are selective for the GluK1 subunit, with 7b being the most subtype-selective ligand reported to date (GluK1 vs GluK3). The antagonist 7a was cocrystallized with the GluK1 ligand binding domain, and an X-ray crystallographic analysis revealed the largest flexibility in GluK1 ligand binding domain opening upon binding of a ligand seen to date. The results provide new insights into the molecular mechanism of GluK1 receptor ligand binding and pave the way to the development of new tool compounds for studying kainate receptor function.
AMINOPYRROLIDINE COMPOUND
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Page/Page column 65, (2009/01/24)
Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC4 receptor antagonistic effect.
COMPOUNDS ACTIVE ON GLUTAMATERGIC RECEPTORS
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, (2008/06/13)
The present invention relates to a compound of Formula (I) process for its preparation and uses thereof.
KINASE INHIBITORS
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Page/Page column 112, (2008/06/13)
Compounds are provided for use with kinases that comprise (I), (II): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful f
PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSYNE KINASES
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Page/Page column 108, (2008/06/13)
Compounds of formula (I): and their use in the inhibition of Trk activity are described.