Saccone, Irene (2016) Design and Synthesis of Peptide and Peptidomimetics Involved in Antiretroviral and Anticancer Therapies. [Tesi di dottorato]

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Item Type: Tesi di dottorato
Lingua: English
Title: Design and Synthesis of Peptide and Peptidomimetics Involved in Antiretroviral and Anticancer Therapies
Creators:
CreatorsEmail
Saccone, Ireneirene.saccone@unina.it
Date: 23 March 2016
Number of Pages: 133
Institution: Università degli Studi di Napoli Federico II
Department: Farmacia
Scuola di dottorato: Scienze farmaceutiche
Dottorato: Scienza del farmaco
Ciclo di dottorato: 28
Coordinatore del Corso di dottorato:
nomeemail
D'Auria, ValeriaEMAIL mariavaleria.dauria@unina.i
Tutor:
nomeemail
Santagada, VincenzoUNSPECIFIED
Date: 23 March 2016
Number of Pages: 133
Uncontrolled Keywords: NC inhibitors, 2,6-dipeptidilantraquinones, IGFBP6 fragment, auxiliary
Settori scientifico-disciplinari del MIUR: Area 03 - Scienze chimiche > CHIM/08 - Chimica farmaceutica
Date Deposited: 11 Apr 2016 07:43
Last Modified: 11 May 2017 01:00
URI: http://www.fedoa.unina.it/id/eprint/10706

Abstract

Abstract Unit 1 The development of new anti-HIV-1 drugs is a global need, due to the resistance and the side effects arising from the therapies currently in use, for this reason we focused on an innovative target, the nucleocapsidic chaperonic protein(NC) of HIV-1 virus, which is involved in many steps of the virus replication, expecially the trascription. Moreover it plays a role of mediator in the annealing reaction of TAR with cTAR. 2,6-Dipeptidyl-anthraquinones are a promising class of nucleic acid-binding compounds that act as NC inhibitors in vitro. We designed, synthesized and tested new series of 2,6-disubstituted-anthraquinones, which are able to bind viral nucleic acid substrates of NC. We demonstrated that these novel derivatives interact preferentially with non-canonical structures of TAR and cTAR, stabilize their dynamics structures, such as bulge and loop, and interfere with NC chaperone activity.

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