dc.contributor.author | Georgiades, Savvas N. | en |
dc.contributor.author | Mak, L. H. | en |
dc.contributor.author | Angurell, I. | en |
dc.contributor.author | Rosivatz, E. | en |
dc.contributor.author | Firouz Mohd Mustapa, M. | en |
dc.contributor.author | Polychroni, Christoulla | en |
dc.contributor.author | Woscholski, R. | en |
dc.contributor.author | Vilar, R. | en |
dc.creator | Georgiades, Savvas N. | en |
dc.creator | Mak, L. H. | en |
dc.creator | Angurell, I. | en |
dc.creator | Rosivatz, E. | en |
dc.creator | Firouz Mohd Mustapa, M. | en |
dc.creator | Polychroni, Christoulla | en |
dc.creator | Woscholski, R. | en |
dc.creator | Vilar, R. | en |
dc.date.accessioned | 2019-11-21T06:19:06Z | |
dc.date.available | 2019-11-21T06:19:06Z | |
dc.date.issued | 2011 | |
dc.identifier.uri | http://gnosis.library.ucy.ac.cy/handle/7/55495 | |
dc.description.abstract | The discovery of small-molecule modulators of signaling pathways is currently a particularly active area of research. We aimed at developing unprecedented metal-based activators of Akt signaling which can potentially find applications as tools for regulating glucose metabolism downstream of Akt or serve as lead structures for developing antidiabetic drugs. In this context, a highly diverse library of 11 new zinc(II) complexes with phenolic, picolinic, pyridino, and hydroxamic ligands, all containing features beneficial for medicinal purposes, was prepared and screened in an assay that detected levels of phospho-Akt in lysates from NIH3T3 cells after treatment with the compounds. The complexes featuring hydroxamic ligands were found to be the most prominent activators of Akt among the molecules prepared, with the most efficient compound acting at submicromolar concentrations. Further characterization revealed that this compound induces phosphorylation of the Akt downstream effector glycogen synthase kinase 3β, but does not act as an inhibitor of tyrosine phosphatases or PTEN. © 2010 SBIC. | en |
dc.source | Journal of Biological Inorganic Chemistry | en |
dc.source.uri | https://www.scopus.com/inward/record.uri?eid=2-s2.0-79951553267&doi=10.1007%2fs00775-010-0716-0&partnerID=40&md5=f1c096e1aa810620ca1a4b1bc35b4a23 | |
dc.subject | article | en |
dc.subject | controlled study | en |
dc.subject | priority journal | en |
dc.subject | protein expression | en |
dc.subject | unclassified drug | en |
dc.subject | nonhuman | en |
dc.subject | signal transduction | en |
dc.subject | drug screening | en |
dc.subject | Animals | en |
dc.subject | Mice | en |
dc.subject | animal cell | en |
dc.subject | mouse | en |
dc.subject | protein kinase B | en |
dc.subject | Proto-Oncogene Proteins c-akt | en |
dc.subject | enzyme phosphorylation | en |
dc.subject | phosphatidylinositol 3 kinase | en |
dc.subject | Phosphatidylinositol 3-Kinases | en |
dc.subject | enzyme inhibition | en |
dc.subject | Models, Biological | en |
dc.subject | Zinc | en |
dc.subject | Organometallic Compounds | en |
dc.subject | phenol | en |
dc.subject | enzyme activation | en |
dc.subject | NIH 3T3 Cells | en |
dc.subject | Phosphorylation | en |
dc.subject | cytotoxicity | en |
dc.subject | Hydroxamic Acids | en |
dc.subject | cell strain 3T3 | en |
dc.subject | enzyme structure | en |
dc.subject | enzyme purification | en |
dc.subject | antidiabetic agent | en |
dc.subject | glucose metabolism | en |
dc.subject | 3 formyl 4 hydroxybenzenesulfonic acid | en |
dc.subject | 4 amino n hydroxybenzamide | en |
dc.subject | 5 nitropyridine 2 carboxaldehyde | en |
dc.subject | Akt | en |
dc.subject | cell lysate | en |
dc.subject | ethyl isocyanate | en |
dc.subject | ethylenediamine | en |
dc.subject | Hydroxamic acid | en |
dc.subject | hydroxylamine sulfate | en |
dc.subject | methyl 4 (aminomethyl)benzoate | en |
dc.subject | n hydroxy 4 [(trifluoromethylsulfonamido)methyl]benzamide | en |
dc.subject | phosphatidylinositol 3,4,5 trisphosphate 3 phosphatase | en |
dc.subject | Phosphoinositide 3-kinase | en |
dc.subject | picolinic acid | en |
dc.subject | pyridine 2 carboxaldehyde | en |
dc.subject | pyridinol | en |
dc.subject | zinc complex | en |
dc.title | Identification of a potent activator of Akt phosphorylation from a novel series of phenolic, picolinic, pyridino, and hydroxamic zinc(II) complexes | en |
dc.type | info:eu-repo/semantics/article | |
dc.identifier.doi | 10.1007/s00775-010-0716-0 | |
dc.description.volume | 16 | |
dc.description.issue | 2 | |
dc.description.startingpage | 195 | |
dc.description.endingpage | 208 | |
dc.author.faculty | 002 Σχολή Θετικών και Εφαρμοσμένων Επιστημών / Faculty of Pure and Applied Sciences | |
dc.author.department | Τμήμα Χημείας / Department of Chemistry | |
dc.type.uhtype | Article | en |
dc.description.notes | <p>Cited By :6</p> | en |
dc.source.abbreviation | J.Biol.Inorg.Chem. | en |
dc.contributor.orcid | Georgiades, Savvas N. [0000-0002-6106-9904] | |
dc.gnosis.orcid | 0000-0002-6106-9904 | |