Naslov
Photo-activable oligopeptides for targeting proteins and DNA

Autori
Husak, Antonija

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
European School of Medicinal Chemistry / Proceedings of PhD Student Poster Sesion / - , 2016, 46-46

Skup
European School of Medicinal Chemistry

Mjesto i datum
Urbino, Italija, 26.06.2016. - 01.07.2016

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
photodeamination ; quinone methide ; tripetides

Sažetak
Peptide therapeutics are starting to show a maturity that reflects their potential for addressing a growing range of medical challenges and about half of the peptides in clinical trials target indications in oncology, metabolic, cardiovascular and infectious disease. Peptides are more frequently considered as drugs candidates since they form non-covalent complexes with proteins and DNA, which in principle enables selective targeting of a desired enzyme or a gene sequence. Herein synthesis of different dipeptides and tripetides will be presented that contain modified tyrosine, as shown in one example by structure 1. Photochemical reaction of deamination in these peptides deliver quinone methide (QM) derivatives. It has been demonstrated that QMs react with DNA and proteins, so they have been intensively investigated reactive because of their anticipated biological activity. Photochemical reaction of deamination provides a mild and easy access to QMs, especially applicable in biological systems since photoexcitation allows for temporal and spatial control of the process. Research with newly synthesized peptides containing modified tyrosine includes investigation of photochemical reactivity with preparative irradiations, and study of noncovalent interactions of peptides with DNA and proteins. Photochemical formation of QMs in the supramolecular complexes with biologically important molecules is anticipated to lead to their covalent modifications. Such a photo-activable alkylation methodology could have significant implications in medicinal chemistry in the development of different enzyme inhibitors or antirpoliferative agents.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA