Peptidomimetics and Pseudopeptides

Code:

53304

ECTS:

3.0

Lecturers in charge:

prof. dr. sc. Lidija Barišić

Lecturers:

prof. dr. sc. Lidija Barišić - Seminar

doc. dr. sc. Monika Kovačević - Laboratory exercises

Take exam:

Studomat

Load:

1. komponenta

Lecture type	Total
Lectures	15
Seminar	4
Laboratory exercises	20

* Load is given in academic hour (1 academic hour = 45 minutes)

Description:

The disadvantages of natural peptides (proteolytic instability, polarity, conformational freedom) can be overcome by using their mimetics. Potential peptidomimetics include small peptide or nonpeptide molecules that mimic the fragment of the peptide secondary structure (helix, beta sheet, turn) involved in molecular recognition. By conformational analysis of potential peptidomimetics in solution using standard spectroscopy techniques (IR, NMR and CD spectroscopy) and by comparing their secondary structure with the secondary structure of the original peptide, it is possible to predict the biological activity of peptidomimetics based on SAR (structure activity relationship) studies. The aim of this course is: (i) to familiarise students with the possibilities of overcoming the shortcomings of natural peptides by using their synthetic mimetics, (ii) to show that structural complementarity of ligands and receptors is a prerequisite for achieving biological activity, and (iii) to demonstrate the conformational analysis of peptides and their mimetics in solution by IR, NMR and CD spectroscopy.

Learning outcomes:

Literature:

Trabocchi, A. Guarna, Peptidomimetics in Organic and Medicinal Chemistry: The Art of Transforming Peptides in Drugs, 2014 John Wiley and Sons Ltd, The Atrium, Southern Gate, Chichester, West Sussex, PO19 8SQ, United Kingdom.

A. S Gokhale, S. Satyanarayanajois, Peptides and peptidomimetics as Immunomodulators, Immunotherapy 2014, 6, 755.

N. P. Croft, A.W. Purcell, Peptidomimetics: modifying peptides in the pursuit of better vaccines, Expert Review of Vaccines 2011, 10, 211.

E. Ko, Ji.Liu, K. Burgess, Minimalist and universal peptidomimetics, Chemical Society Reviews 2011, 40, 4411.

E. Ko, J. Liu, L. M. Peres, G. Lu, A. Schaefer, K. Burgess, Universal Peptidomimetics, Journal of American Chemical Society 2011, 133, 462.

M. A. Estiarte, D. P. Rich, Peptidomimetics for Drug Design, Burger's Medicinal Chemistry and Drug Discovery, Sixth Edition, Volume 1: Drug Discovery, Edited by Donald J. Abraham 2003 John Wiley and Sons, Inc., Hoboken, New Jersey.

L. Gentilucci, A. Tolomelli, F. Squassabia, Peptides and Peptidomimetics in Medicine, Surgery and Biotechnology, Current Medicinal Chemistry 2006, 13, 2449.
A. Grauer, B. König, Peptidomimetics A Versatile Route to Biologically Active Compounds, European Journal of Organic Chemistry 2009, 5099.

P. Ruzza, Peptides and Peptidomimetics in Medicinal Chemistry, INTECH Open Access Publisher, 2012.,

3. semester

Bioprocesno inženjerstvo - B1 - Regular studij - Bioprocess Engineering

Elective course - Regular studij - Bioprocess Engineering

Prehrambeno inženjerstvo - B1 - Regular studij - Food Engineering

Elective course - Regular studij - Food Engineering

Upravljanje sigurnošću hrane - B1 - Regular studij - Food Safety Management

Elective course - Regular studij - Food Safety Management

Molekularna biotehnologija - B1 - Regular studij - Molecular Biotechnology

Elective course - Regular studij - Molecular Biotechnology

Consultations schedule:

Peptidomimetics and Pseudopeptides