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Quality not Quantity: The Role of Marine Natural Products in Drug Discovery and Reverse Chemical Proteomics

View Article: PubMed Central

ABSTRACT

Reverse chemical proteomics combines affinity chromatography with phage display and promises to be a powerful new platform technology for the isolation of natural product receptors, facilitating the drug discovery process by rapidly linking biologically active small molecules to their cellular receptors and the receptors’ genes. In this paper we review chemical proteomics and reverse chemical proteomics and show how these techniques can add value to natural products research. We also report on techniques for the derivatisation of polystyrene microtitre plates with cleavable linkers and marine natural products that can be used in chemical proteomics or reverse chemical proteomics. Specifically, we have derivatised polystyrene with palau’amine and used reverse chemical proteomics to try and isolate the human receptors for this potent anticancer marine drug.

No MeSH data available.


Oxidation of the backbone of PS yields carboxyl groups on the polymer surface [46].
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f4-marinedrugs-03-00036: Oxidation of the backbone of PS yields carboxyl groups on the polymer surface [46].

Mentions: Rotmans and Delwel described a method of introducing amine groups onto the surface of PS plates for the covalent immobilisation of antigens [44]. The PS surface was first nitrated with fuming nitric acid and then reduced with sodium dithionite (Fig. 3). This yielded aromatic amines on the plate surface that could then be derivatised with an amine-reactive molecule of choice [45]. Zammatteo and colleagues oxidised the surface of PS microtitre plates with acidic potassium permanganate to generate free carboxyl groups on the polymer backbone, which were then activated with EDC and coupled with DNA probes for hybridisation assays [46] (Fig. 4).


Quality not Quantity: The Role of Marine Natural Products in Drug Discovery and Reverse Chemical Proteomics
Oxidation of the backbone of PS yields carboxyl groups on the polymer surface [46].
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3756327&req=5

f4-marinedrugs-03-00036: Oxidation of the backbone of PS yields carboxyl groups on the polymer surface [46].
Mentions: Rotmans and Delwel described a method of introducing amine groups onto the surface of PS plates for the covalent immobilisation of antigens [44]. The PS surface was first nitrated with fuming nitric acid and then reduced with sodium dithionite (Fig. 3). This yielded aromatic amines on the plate surface that could then be derivatised with an amine-reactive molecule of choice [45]. Zammatteo and colleagues oxidised the surface of PS microtitre plates with acidic potassium permanganate to generate free carboxyl groups on the polymer backbone, which were then activated with EDC and coupled with DNA probes for hybridisation assays [46] (Fig. 4).

View Article: PubMed Central

ABSTRACT

Reverse chemical proteomics combines affinity chromatography with phage display and promises to be a powerful new platform technology for the isolation of natural product receptors, facilitating the drug discovery process by rapidly linking biologically active small molecules to their cellular receptors and the receptors’ genes. In this paper we review chemical proteomics and reverse chemical proteomics and show how these techniques can add value to natural products research. We also report on techniques for the derivatisation of polystyrene microtitre plates with cleavable linkers and marine natural products that can be used in chemical proteomics or reverse chemical proteomics. Specifically, we have derivatised polystyrene with palau’amine and used reverse chemical proteomics to try and isolate the human receptors for this potent anticancer marine drug.

No MeSH data available.