Combinatorial Biocatalysis for Drug Discovery, Biomolecules, Precursors, Molecular, Random Mutation

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Combinatorial Biocatalysis for Drug Discovery

Nature synthesizes biomolecules of unparalleled structural complexity by encoding enzymes that catalyze a variety of reactions. These reactions are carried out on low molecular weight synthons (precursors), the biological equivalent of drug discovery lead compounds that are used for producing a variety of derivatives. Over an evolutionary time, random mutations in DNA result in the production of molecules, thus producing a vast diversity of natural products. This diversity in nature has though been utilized for the production of drugs and agrochemicals, approach of combinatorial biocatalysis has been used for creating additional diversity in a relatively short period of time (when compared to evolutionary time in nature).

This approach of combinatorial biocatalysis makes use of huge diversity of natural catalysts and the recombinant and engineered enzymes that are known. This approach of combinatorial biocatalysis, however, differs from combinatorial biosynthesis discussed above, which refers to the generation of novel molecules derived from natural products by genetic engineering of biosynthetic pathways in living organisms, but without making use of known biocatalytic activities.

Steps involved in the combinatorial synthesis of new biomolecules from synthons (precursors) in nature and from lead compounds in vitro
From Synthons in Nature	From Lead compounds in vitro

For drug discovery, several molecules have been used for generation of libraries employing combinatorial biocatalysis. These molecules include the following (Fig. 43.8): (i) nucleosides (e.g. adenosine); (ii) flavonoids (e.g. bergenin); (iii) alkaloids (e. g. 3,6-dihydroxytropane); (iv) polyketides (e.g. erythromycin) and (v) terpenoids and texanes. The use of combinatorial biocatalysis will be illustrated using bergenin as a lead compound, which has been sucessfully demonstrated in a study conducted in late 1990s.

Some example of lead molecules that have been used for the generation of libraries by combinatorial biocatalysis

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Diversity-Oriented Organic Synthesis and Evolving Synthetic Analysis Solid Phase Synthesis for Drug Discovery Combinatorial Biocatalysis for Drug Disovery Synthesis of Bergenin Derivatives Drug Discovery in Cancer Research Microbial Genomics for New Antibiotics Genomics Drugs (Pharmacogenomics) Immunotoxins as Drugs Drug Designing Drug Designing by Blocking Enzyme Activity Drug Designing through Blocking Hormone Receptors Drug Designing through Inhibition of Nucleic Acid Synthesis Drug Designing Against Heterogeneous Targets