Objective
INVESTIGATION 0F ENZYME-INHIBITOR/ACTIVATOR INTERACTIONS BY MEANS 0F HIGH RESOLUTION NMR, ELECTRONIC AND EPR SPECTROSCOPY
The understanding at molecular level of the intricate processes which are involved in the enzymatic catalysis/inhibition is critical for designing novel types of drugs, as well as non-polluting biotechnologies among others One of the enzymes ubiquitously spread in the animal, vegetal and bacterian kingdoms is carbonic anhydrase (CA), a 3okd zinc enzyme which catalyzes a simple physiological reaction, the reversible hydration of carbon dioxide to bicarbonate.
The seven isozymes presently known in vertebrates are involved in important physiological processes such as respiration, transport of C02 between metabolizing tissues and lungs, anion excretion in urine, etc. Two main classes of inhibitors are known for this enzyme: the inorganic anions and the unsubstituted solfonamides.
The design of novel types of CA inhibitors is a permanent goal for many groups, due to the fact that isozyme-specific or organ-selective inhibitors were rarely reported. In this field, my group recently reported positively charged sulfonamides which main show specificity of inhibition for the membrane-associated isozymes.Together with this type of compounds, other inhibitors were prepared in order to obtain very unsoluble bulky inhibitors which presents a depot effect in vivo, highly liposoluble inhibitors containg large aliphatic moieties in their molecule, which may cross easier biological membranes and have access to the enzyme within the brain, as well as inhibitors with modified sulfonamido groups. Another vista of research was offered by the discovery of complex inhibitors of CA. These new compounds were characterized by standard procedures and assayed for CA inhibition. Unfortunately such inhibitors were never investigated by means of high resolution NMR spectroscopy, CD or X-ray studies. Thus one of the main goal of this research proposal concerns these aspects. The same type of investigation might be carried out on CA activators from different classes of compounds.
Performing such experiments might help to clarify some aspects connected with enzymatic inhibition/catalysis/activation, and might lead to the design of more rational drugs.
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Programme(s)
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Coordinator
50121 Firenze
Italy
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