Brancaccio, Diego (2011) Interaction of peptides and small molecules with biological targets. [Tesi di dottorato] (Unpublished)

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Item Type: Tesi di dottorato
Language: English
Title: Interaction of peptides and small molecules with biological targets
Creators:
CreatorsEmail
Brancaccio, Diegodiego.brancaccio@unina.it
Date: 30 November 2011
Number of Pages: 249
Institution: Università degli Studi di Napoli Federico II
Department: Chimica farmaceutica e tossicologica
Doctoral School: Scienze farmaceutiche
PHD name: Scienza del farmaco
PHD cycle: 24
PHD Coordinator:
nameemail
D'Auria, Maria Valeriamadauria@unina.it
Tutor:
nameemail
Carotenuto, Alfonsoalfonso.carotenuto@unina.it
Date: 30 November 2011
Number of Pages: 249
Uncontrolled Keywords: NMR, peptide, conformational analysis
MIUR S.S.D.: Area 03 - Scienze chimiche > CHIM/08 - Chimica farmaceutica
Date Deposited: 06 Dec 2011 11:27
Last Modified: 30 Apr 2014 19:48
URI: http://www.fedoa.unina.it/id/eprint/8816

Abstract

During my PhD course, I focused my attention on the conformational analysis of peptides that interact with GPCR and ligand-receptor interactions from NMR spectroscopy with possible application to cytotoxic agents binding to DNA. In particular, I investigated the conformational behaviour of peptide analogues of Urotensin, Melanocortin and Somatostatin in water solution and membrane mimetic environment (SDS and DPC micelles). Another research field was the NMR-based screening as potent technique for the identification of small molecules that interact with macromolecule targets. Several methods based on the ligand observation have been proposed in the literature, among these WaterLOGSY (water-ligand observed via gradient spectroscopy), and STD-NMR (saturation transfer difference) experiments. I applied these NMR techniques for the evaluation of the DNA interactions of a new series of thiophen-naphthoquinones with interesting cytotoxic activity.

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