Article ID Journal Published Year Pages File Type
5521105 Drug Discovery Today 2017 9 Pages PDF
Abstract

•Morpheein model describes the new mode of allosteric regulation of proteins.•l-asparaginase is present as morpheein in some microorganisms.•l-Asparaginase is involved in the virulence mechanism of several fatal diseases.•Virulent l-asparaginase present in morpheein form can be compelling drug target.•Shifting equilibrium towards inactive morpheein form can silence the virulence.

Allosterism has emerged as an innovative and significant mode of drug discovery. It facilitates the targeting of an allosteric site that is unique and more specific. A relatively new approach to allosteric regulation is the morpheein model, a concerted dissociative model that describes the equilibrium of alternate quaternary structure assemblies, whose architectures are dictated by alternate conformations in the dissociated state. It is involved in various biological phenomena, including enzyme regulation. One such enzyme is l-asparaginase, which is exploited by pathogenic microbes to cause infectious disease in humans. Thus, the morpheein model can be applied as a novel approach to the discovery of allosteric modulators that regulate l-asparaginase function to control virulence and serves as the basis for novel drug discovery research.

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Life Sciences Biochemistry, Genetics and Molecular Biology Biotechnology
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