Unit:
Κατεύθυνση Σχεδιασμός και Ανάπτυξη νέων Φαρμακευτικών Ενώσεων - Φαρμακευτική ΧημείαLibrary of the School of Science
Supervisors info:
Ιωάννης Κωστάκης, Επίκουρος Καθηγητής, Τμήμα Φαρμακευτικής, Εθνικό και Καποδιστριακό Πανεπηστήμιο Αθηνών
Original Title:
ΣΧΕΔΙΑΣΜΟΣ ΚΑΙ ΣΥΝΘΕΣΗ ΑΝΑΛΟΓΩΝ ΤΟΥ FLINDERSINE ΩΣ ΠΙΘΑΝΩΝ ΑΝΑΣΤΟΛΕΩΝ ΤΗΣ DYRK1A
Translated title:
DESIGN AND SYNTHESIS OF FLINDERSINE ANALOGUES AS DYRK1A INHIBITORS
Summary:
Protein Kinases are key regulators of cell function that catalyze the transfer of phosphate group between their substrates. Dysregulation of protein kinase activity is involved in pathological conditions, such as cancer and several neurological disorders. Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A). ) is a serine/threonine kinase that shows an important role in brain development in both embryonic neuronal development and physiology of the adult brain. Higher than normal levels are associated with neurogenesis in Down syndrome, the early onset of Alzheimer's disease-like symptoms and mental retardation that occurs in Down Syndrome. Thus it represents an attractive target for drug development: inhibition of DYRK1A is an interesting strategy to modify the disease. However, only a few inhibitors are reported, and their potential clinical uses require further evaluation. Our group has previously reported that Flindersine, a pyranoquinoline alkaloid, shows notable activity against DYRK1A. As a continuation of this study, in this project is been described the design and synthesis of novel spiro-flindersine analogs so as to better understand the structure-activity relationships regarding the interaction with DYRK1A.
Main subject category:
Science
Other subject categories:
Health Sciences
Keywords:
DYRK1A, Alzheimer's disease, Down synfrome, DYRK1A inhibitors, Flindersine, kinase inhibitors
