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Title

Interaction studies to evaluate 2- carboxyphenolate analogues as inhibitor of anti-apoptotic protein Bcl-2

 

Authors

Mohammed A Al-Karaawi

 

Affiliation

Dean of Faculty of Health Sciences, Buraydah Colleges, Al-Qassim Buraydah, P.O.Box 51418

 

Email

karaawi@yahoo.co.uk; *Corresponding author

 

Article Type

Hypothesis

 

Date

Received December 08, 2012; Accepted December 20, 2013; Published May 25, 2013

 

Abstract

Apoptosis is a cellular process that leads to the death of damaged cells. Its malfunction can cause cancer and poor response to conventional chemotherapy. After being activated by cellular stress signals, pro-apoptotic proteins bind anti-apoptotic proteins, thus allowing apoptosis to go forward. An excess of anti-apoptotic proteins can prevent apoptosis. Designed molecules that imitate the roles of pro-apoptotic proteins can promote the death of cancer cells. In this work we have applied an insilico approach to study the binding of 2-carboxyphenolate analogues as potent inhibitors of anti-apoptotic protein Bcl-2. Molecular docking study was performed in order to find specific binding mode using AutoDock. From the docking results it was observed that zinc 2- carboxyphenolate showed strong inhibition with Bcl-2 with docking energy of -4.6 kcal/mol. The effects of the Zinc 2-hydroxybenzoate on apoptosis in HT-1080 cell lines were also analysed, which shows strong evidence for their apoptotic mode of action using flow cytometric analysis of Annexin-V. Our study gave valuable insights on inhibitor specificity of anti-apoptotic proteins and might be considered as potent chemopreventive agents.

 

Keywords

Apoptosis, Docking, Bcl-2, AutoDock, 2-carboxyphenolate analogues, 2-hydroxybenzoate analogues.

Citation

Al-Karaawi, Bioinformation 9(9): 477-480 (2013)

 

Edited by

P Kangueane

 

ISSN

0973-2063

 

Publisher

Biomedical Informatics

 

License

This is an Open Access article which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. This is distributed under the terms of the Creative Commons Attribution License.