Albany 2013: Book of Abstracts
June 11-15 2013
©Adenine Press (2012)
A cutting - edge to drug discovery in Cancer; Cyclins as novel targets - an in silico technique
Cyclins are requisite factors operating in eukaryotic cell cycle. Disorientation of their function leads to tumourgenesis (M. Stamatakos et. al., 2010). Various cyclins bind to cyclin dependent kinases (CDK/ cyclin complexes) as crucial regulators during transcription and mRNA processing operating between G0, G1, S, G2 and M phases of cell cycle (P. Loyera et. al., 2005).
The overview on the role and function of the cyclins in the cell cycle is presented in the current article. The cyclins – Cyclin C and Cyclin D2 were taken up to arrest the initial stages of cell cycle progression by designing new chemical entities for cancer therapy. The structure of the cyclin proteins have been modelled by homology modelling and validated. Active site for the cyclin structures were identified and subjected to virtual screening using various databanks. A set of new lead molecules were identified. (Sarita Rajender P et. al., 2011, Bhargavi et.al., and 2010). The leads were prioritised, synthesised and tested for activity. The new leads showed promising cancer activity.
Pascal Loyera,b, Janeen H. Trembleya, Robert Katonac, Vincent J. Kidda,and Jill M. Lahtia. (2005), Role of CDK/cyclin complexes in transcription and RNA splicing Cellular Signalling, 17: 1033 – 1051.
Sarita Rajender P, Vasavi M, and Uma Vuruputuri. (2011), Identification of novel selective antagonists for cyclin C by Homology modeling and virtual screening. International journal of biological macromolecules, 48: 292-300.
K. Bhargavi, Kalyan P. Chaitanya, D. Ramasree, M. Vasavi, D. K. Murthy, V. Uma*. (2010).Homology modeling and docking studies of human Bcl-2L10 protein. J Biomol Struct Dyn. 28:379-391.