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Title

Targeting cysteine rich C1 domain of Scaffold protein Kinase Suppressor of Ras (KSR) with anthocyanidins and flavonoids a binding affinity characterization study

 

Authors

Dhananjayan Karthik1*, Pulak Majumder2, Sivanandy Palanisamy3, Kalathil Khairunnisa4 & Varsha Venugopal5

 

Affiliation

1Department of Pharmacology, Amrita School of Pharmacy, AIMS Health Science Campus, Amrita Vishwa Vidyapeetham University, Kochi, Kerala, India; 2Department of Pharmacognosy, Acharya & B.M.Reddy College of Pharmacy, Bangalore, Karnataka, India; 3Department of Pharmacy Practice, International Medical University, Kualalampur, Malaysia; 4Department of Pharmacology, Grace College of Pharmacy, Palakkad, Kerala, India; 5Department of Pharmacognosy, Government Medical College, Thiruvananthapuram, Kerala, India

 

Email

karthikdcology@gmail.com; *Corresponding author

 

Article Type

Hypothesis

 

Date

Received September 05, 2014; Accepted September 06, 2014; Published September 30, 2014

 

Abstract

Kinase Suppressor of Ras (KSR) is a molecular scaffold that interacts with the core kinase components of the ERK cascade, Raf, MEK, ERK to provide spatial and temporal regulation of Ras-dependent ERK cascade signaling. Interruption of this mechanism can have a high influence in inhibiting the downstream signaling of the mutated tyrosine kinase receptor kinase upon ligand binding. Still none of the studies targeted to prevent the binding of Raf, MEK binding on kinase suppressor of RAS. In that perspective the cysteine rich C1 domain of scaffold proteins kinase suppressor of Ras-1 was targeted rather than its ATP binding site with small ligand molecules like flavones and anthocyanidins and analyzed through insilico docking studies. The binding energy evaluation shows the importance of hydroxyl groups at various positions on the flavone and anthocyanidin nucleus. Over all binding interaction shows these ligands occupied the potential sites of cysteine rich C1 domain of scaffold protein KSR.  

 

Keywords

Kinase suppressor of Ras, MAPK signaling, flavones, anthocyanidins, insilico docking, AutoDock 4.2.6, Neoplasia

 

Citation

Karthik et al.   Bioinformation 10(9): 580-585 (2014)
 

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.