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Molecules 2018, 23(4), 765;

Small Molecule Catalysts with Therapeutic Potential

Division of Bioorganic Chemistry, School of Pharmacy, Saarland University, D-66123 Saarbruecken, Germany
Department of Pharmaceutics and Pharmaceutical Technology, School of Pharmacy, Damascus University, Damascus, Syria
Author to whom correspondence should be addressed.
Received: 8 March 2018 / Revised: 22 March 2018 / Accepted: 24 March 2018 / Published: 27 March 2018
(This article belongs to the Special Issue Small Molecule Catalysts with Therapeutic Potential)
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Catalysts are employed in many areas of research and development where they combine high efficiency with often astonishing selectivity for their respective substrates. In biology, biocatalysts are omnipresent. Enzymes facilitate highly controlled, sophisticated cellular processes, such as metabolic conversions, sensing and signalling, and are prominent targets in drug development. In contrast, the therapeutic use of catalysts per se is still rather limited. Recent research has shown that small molecule catalytic agents able to modulate the redox state of the target cell bear considerable promise, particularly in the context of inflammatory and infectious diseases, stroke, ageing and even cancer. Rather than being “active” on their own in a more traditional sense, such agents develop their activity by initiating, promoting, enhancing or redirecting reactions between biomolecules already present in the cell, and their activity therefore depends critically on the predisposition of the target cell itself. Redox catalysts, for instance, preferably target cells with a distinct sensitivity towards changes in an already disturbed redox balance and/or increased levels of reactive oxygen species. Indeed, certain transition metal, chalcogen and quinone agents may activate an antioxidant response in normal cells whilst at the same time triggering apoptosis in cancer cells with a different pre-existing “biochemical redox signature” and closer to the internal redox threshold. In pharmacy, catalysts therefore stand out as promising lead structures, as sensor/effector agents which are highly effective, fairly selective, active in catalytic, i.e., often nanomolar concentrations and also very flexible in their structural design. View Full-Text
Keywords: catalysis; cellular thiolstat; drug design; enzymes; mimics; redox modulation; selenium; sensor/effector agents; transition metal complexes catalysis; cellular thiolstat; drug design; enzymes; mimics; redox modulation; selenium; sensor/effector agents; transition metal complexes

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Ney, Y.; Jawad Nasim, M.; Kharma, A.; Youssef, L.A.; Jacob, C. Small Molecule Catalysts with Therapeutic Potential. Molecules 2018, 23, 765.

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