Raphael Taiwo Aruleba
University of Zululand, South Africa
Title: Development of new and effective anti-schistosomal drugs using antimicrobial peptides as lead compounds: A computer-aided drug design study
Biography
Biography: Raphael Taiwo Aruleba
Abstract
With the exponential increase in the prevalence of schistosomiasis, Praziquantel (PZQ) remains the only eff ective drug
in the anti-schistosomal arsenal. However, no signifi cant approaches have been made in recent years in the discovery
of new anti-schistosomal drugs, even with widely-reported resistance of the schistosome worm to PZQ over very large foci.
Th erefore, it is imperative to develop a new drug against this debilitating disease using the broad-spectrum therapeutic potentials
of antimicrobial peptides (AMPs). AMPs are natural antibiotics produced by all living species; they have multifunctional
properties and are currently explored as a vital source for the development of new drugs. In this study, six putative AMPs
(TAK1-TAK6) were identifi ed to possess anti-schistosomal capabilities. Added to this, glycosyltransferase and axonemal
dynein intermediate chain schistosomal proteins were identifi ed using in silico methods as vital proteins for the survival of the
parasite in the host. Th e 3D structures of the AMPs and the proteins were modelled using the I-TASSER, while Patch Dock
was employed to ascertain the interaction between these schistosome proteins and the AMPs. Results obtained show the
putative AMPs have good binding affi nity to the schistosomal proteins. So, TAK3 and TAK6 showed highest binding affi nities
to glycosyltransferase and axonemal dynein intermediate chain respectively. On the whole, all generated AMPs are potential
therapeutics target that could be further developed as drug candidates in the fi ght against schistosomiasis and could as well
prove eff ective against PZQ resistant schistosome strains.