STUDY OF ACAT RECEPTOR WITH HETEROCYCLIC COMPOUNDS FOR DRUG DESIGNINGAbstract
ACAT enzyme is found in human body and it maintains cholesterol homeostasis in the cell. This leads to deposition of cholesterol in our body as cholesteryl esters. Freely deposited cholesterol in the membranes of the cells is cytotoxic. This deposition causes atherosclerosis, Alzheimer’s disease, Xanthelasma, etc. The first substrate for ACAT is both medium & long fatty acyl CoA. Therefore, we studied the ACAT enzyme, its active site, location and activity to develop the inhibitors of ACAT as antihyperlipidemic agents with the heterocyclic compounds for drug designing. ACAT is having two active sites: histidine and aspargines. ACAT 1 is present in two chromosomes 1 and 7. Active site His-460 Of ACAT-I is responsible for catalysis. For docking studies these factors should be known so that the hetercyclic compound could be developed having inhibitory activity against ACAT. Further many literature review have been done to find a hetercyclic moiety having the antihyperlipidemic activity in which we found that benzene ring with thiazole and oxazole rings having side chain could get results as ACAT inhibitors.
Shainda Laeeq * and Vishal Dubey
Faculty of Pharmacy, Naraina Vidya Peeth Group of Institutions, Kanpur, Uttar Pradesh, India.
06 April 2022
11 May 2022
31 May 2022
01 July 2022