Computer Aided Design of potential inhibitors for Gaucher disease

Acid β-glucosidase (GlcCerase) is a lysosomal enzyme, which is important in biodegradation of blood cells in human body. Mutation of GlcCerase will lead to Gaucher disease; the most common lysosomal storage disease. The current available treatments for Gaucher disease are enzyme replacement therapy...

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Main Authors: Noorbatcha, Ibrahim Ali, Mohd. Salleh, Hamzah
Format: Proceeding Paper
Language:English
Published: 2010
Subjects:
Online Access:http://irep.iium.edu.my/4074/
http://irep.iium.edu.my/4074/4/IRIIE-CAD_Gaucher.pdf
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author Noorbatcha, Ibrahim Ali
Mohd. Salleh, Hamzah
author_facet Noorbatcha, Ibrahim Ali
Mohd. Salleh, Hamzah
author_sort Noorbatcha, Ibrahim Ali
building IIUM Repository
collection Online Access
description Acid β-glucosidase (GlcCerase) is a lysosomal enzyme, which is important in biodegradation of blood cells in human body. Mutation of GlcCerase will lead to Gaucher disease; the most common lysosomal storage disease. The current available treatments for Gaucher disease are enzyme replacement therapy and substrate reduction therapy; and both are costly. With the help of computer molecular modeling, new drug candidate for Gaucher disease treatment can be designed. In this research, we have successfully designed a lead-candidate to act as a potential inhibitor, as a part of substrate reduction therapy by adapting novel in silico method. Lamarckian genetic algorithm is used to locate the potential inhibitor sites in the acid β- glucosidase and strength of the binding is evaluated using potential mean force (PMF) scores. Good correlation between experimental inhibition constant (Ki) and computational binding score is established with the correlation coefficient of 0.782. This correlation used as to predict the unknown Ki value of the new ligand. N-decyl deoxynojirimycin gave a promising result to be considered as a candidate inhibitor.
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spelling iium-40742021-06-23T03:50:06Z http://irep.iium.edu.my/4074/ Computer Aided Design of potential inhibitors for Gaucher disease Noorbatcha, Ibrahim Ali Mohd. Salleh, Hamzah TP248.13 Biotechnology Acid β-glucosidase (GlcCerase) is a lysosomal enzyme, which is important in biodegradation of blood cells in human body. Mutation of GlcCerase will lead to Gaucher disease; the most common lysosomal storage disease. The current available treatments for Gaucher disease are enzyme replacement therapy and substrate reduction therapy; and both are costly. With the help of computer molecular modeling, new drug candidate for Gaucher disease treatment can be designed. In this research, we have successfully designed a lead-candidate to act as a potential inhibitor, as a part of substrate reduction therapy by adapting novel in silico method. Lamarckian genetic algorithm is used to locate the potential inhibitor sites in the acid β- glucosidase and strength of the binding is evaluated using potential mean force (PMF) scores. Good correlation between experimental inhibition constant (Ki) and computational binding score is established with the correlation coefficient of 0.782. This correlation used as to predict the unknown Ki value of the new ligand. N-decyl deoxynojirimycin gave a promising result to be considered as a candidate inhibitor. 2010-01-26 Proceeding Paper NonPeerReviewed application/pdf en http://irep.iium.edu.my/4074/4/IRIIE-CAD_Gaucher.pdf Noorbatcha, Ibrahim Ali and Mohd. Salleh, Hamzah (2010) Computer Aided Design of potential inhibitors for Gaucher disease. In: IIUM Research, Innovation & Invention Exhibition (IRIIE 2010), 26 - 27 January 2010, Kuala Lumpur. (Unpublished)
spellingShingle TP248.13 Biotechnology
Noorbatcha, Ibrahim Ali
Mohd. Salleh, Hamzah
Computer Aided Design of potential inhibitors for Gaucher disease
title Computer Aided Design of potential inhibitors for Gaucher disease
title_full Computer Aided Design of potential inhibitors for Gaucher disease
title_fullStr Computer Aided Design of potential inhibitors for Gaucher disease
title_full_unstemmed Computer Aided Design of potential inhibitors for Gaucher disease
title_short Computer Aided Design of potential inhibitors for Gaucher disease
title_sort computer aided design of potential inhibitors for gaucher disease
topic TP248.13 Biotechnology
url http://irep.iium.edu.my/4074/
http://irep.iium.edu.my/4074/4/IRIIE-CAD_Gaucher.pdf