Please use this identifier to cite or link to this item: https://www.um.edu.mt/library/oar/handle/123456789/49771
Title: Identification of lead molecules capable of the simultaneous agonism of the PPARƴ and PPARα subtypes for the dual management of diabetes mellitus and dyslipidaemia
Authors: Ellul, Claire
Shoemake, Claire
Keywords: Drugs -- Design -- Research
Peroxisome proliferator-activated receptors
PPAR alpha
PPAR gamma
Diabetes
Dyslipidemias
Issue Date: 2016-07
Publisher: University of Malta. Department of Pharmacy
Citation: Ellul, C., & Shoemake, C. (2016, July). Identification of lead molecules capable of the simultaneous agonism of the PPARƴ and PPARα subtypes for the dual management of diabetes mellitus and dyslipidaemia. Poster session presented at the MuTaLig COST Action CA15135 at Università della Svizzera Italiana in Lugano, Switzerland.
Abstract: A poster presentation regarding the identification of lead molecules capable of the simultaneous agonism of the PPARƴ and PPARα subtypes for the dual management of diabetes mellitus and dyslipidaemia. Introduction: This is a rational drug design study aiming to identify lead molecules capable of successfully interacting with more than one Peroxisome Proliferator Activated Receptor (PPAR) subtype in order to simultaneously manage more than one PPAR mediated condition. The PPARs are nuclear receptors involved in the regulation of cellular differentiation, development, and metabolism (carbohydrate, lipid, protein), and tumorigenesis of higher organisms. This study stems from the loss of the glitazone hypoglycaemics (full PPARƴ agonists) from the market due to their unacceptable side effect profile, and from the realisation that full PPARƴ agonism could not be separated from this adverse effect spectrum. It uses the PPARƴ partial agonist angiotensin receptor blocker telmisartan (pdb ID 3VN2) and an experimental fibrate PPARα agonist GW590735 (pdb ID 2P54) to probe these respective PPAR Ligand Binding Pockets (PPAR_LBPs).
URI: https://www.um.edu.mt/library/oar/handle/123456789/49771
Appears in Collections:Scholarly Works - FacM&SPha



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