Kishor S Jain
S P Pune University, India
Title: Some molecular targets for antihyperlipidemic drug research
Biography
Biography: Kishor S Jain
Abstract
High levels of cholesterol and other lipid constituents are major risk factors in the development of atherosclerosis as well as diseases and disorders associated with it. Though, drugs of various categories acting through different mechanisms are available for antihyperlipidemic therapy, there are limitations associated with each of them, keeping the interest in discovery of newer and better antihyperlipidemic drugs alive. Identification and exploitation of novel molecular targets for discovery of new antihyperlipidemic drugs is an important area of research. Twenty such drug targets shall be discussed for their biochemical roles, structures, estimations, as well as, exploitation for new drug discovery research. Few recently discovered drugs based on such molecular targets shall also be cited. Also discussed will be an investigation into the mechanism of antihyperlipidemic action of a few potential NCE’s from our lab. carried out through docking experiments with few of the above molecular targets; e.g., Niemann Pick C1 Like1 protein (NPC1L1), ATP citrate lyase (ACL), C-reactive protein (CRP), lanosterol 14α-demethylase(LDM), squalene synthase (SqS) and farnesiod X-receptor (FXR) etc. The interactions of these NCE’s with these molecular targets (receptors) were compared with the interactions of the respective co-crystallized native ligands at the active sites of these receptors. These comparisons are based on the docking parameters, as well as, types of interactions and vicinity with various amino acids in the active site pockets. On the basis of favorable interactions with molecular targets assessment of pharmacodynamics has been made in this study.