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Identifier

000463331

Title

Development of innovative modulators for human 15-lipoxygenase-1

Alternative Title

Ανάπτυξη καινοτόμων ρυθμιστών για την ανθρώπινη 15-λιποξυγενάση-1

Author

Σπάχο, Ντανιέλα Κ.

Thesis advisor

Ελευθεριάδης, Νικόλαος

Reviewer

Παυλίδης, Ιωάννης
Στρατάκης, Μανόλης

Abstract

Human 15-lipoxygenase-1 (15-LOX-1), a non-heme containing enzyme, catalyzes the regio- and stereo-specific oxygenation of polyunsaturated fatty acids, yielding various bioactive lipid mediators. Its implication in inflammatory diseases, neurodegeneration and cancer renders 15-LOX-1 an attractive target for drug development. In this study, a multidisciplinary approach was employed for the development of innovative modulators designed to target 15-LOX-1, thereby serving as tools to better understand its biological role. Employing two-component (2-CR) reactions with amines and multicomponent reactions (MCRs), bioactive molecules such as activity-based probes (ABPs), photobiological switches, and photoactivated crosslinkers were synthesized. Furthermore, the pharmacological properties of phosphoeleganin, a marine natural product, were investigated through a fragment-based screening, providing information about the active site of the enzyme. This research contributes to a deeper understanding of 15-LOX-1 in order to facilitate the discovery of novel therapeutic agents against associated diseases.

Language

English

Subject

Activity-based probes

Enzyme kinetics

Inhibition

Modulation

Αναστολή

Ανιχνευτές

Ενζυμική κινητική

Ρύθμιση

Issue date