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In silico identification of noncompetitive inhibitors targeting an uncharacterized allosteric site of falcipain-2
(2021-01-01)
Falcipain-2 (FP-2) is a Plasmodium falciparum hemoglobinase widely targeted in the search for antimalarials. FP-2 can be allosterically modulated by various noncompetitive inhibitors that have been serendipitously identified. ...
Non-competitive reversible inhibition of laccase by H2O2 in osmium mediated layer-by-layer multilayer O2 biocathodes
(Electrochemical Society, 2015-07)
A systematic study of the inhibition of laccase by hydrogen peroxide in oxygen biocathodes composed of layer-by-layer selfassembled multilayers of Trametes-trogii laccase and osmium derivatized poly(allylamine) redox ...
CNS-selective noncompetitive cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline
(Elsevier B.V., 2008-02-12)
LASSBio-767 [(-)-3-O-acetyl-spectaline] and LASSBio-822 [(-)-3-O-tert-Boc-spectaline] were recently described as cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline, obtained from the ...
CNS-selective noncompetitive cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline
(Elsevier B.V., 2008-02-12)
LASSBio-767 [(-)-3-O-acetyl-spectaline] and LASSBio-822 [(-)-3-O-tert-Boc-spectaline] were recently described as cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline, obtained from the ...
Tricyclic antidepressants inhibit homomeric Cys-loop receptors by acting at different conformational states
(Elsevier Science, 2008-04)
Tricyclic antidepressants not only inhibit monoamine reuptake but also modulate Cys-loop receptors. However, it is not understood how this modulation is involved in their therapeutic effects. We analyzed the mechanisms of ...
Anacardic acid derivatives as inhibitors of glyceraldehyde-3-phosphate dehydrogenase from Trypanosoma cruzi
(PERGAMON-ELSEVIER SCIENCE LTD, 2008)
Chagas` disease, a parasitic infection caused by the flagellate protozoan Trypanosoma cruzi, is a major public health problem affecting millions of individuals in Latin America. On the basis of the essential role in the ...
The local anaesthetics proadifen and adiphenine inhibit nicotinic receptors by different molecular mechanisms
(Wiley Blackwell Publishing, Inc, 2009-07)
Background and purpose: Many local anaesthetics are non-competitive inhibitors of nicotinic receptors (acetylcholine receptor, AChR). Proadifen induces a high-affinity state of the receptor, but its mechanism of action and ...
Is the antidepressant activity of selective serotonin reuptake inhibitors mediated by nicotinic acetylcholine receptors?
(Molecular Diversity Preservation International, 2021-04)
It is generally assumed that selective serotonin reuptake inhibitors (SSRIs) induce antidepressant activity by inhibiting serotonin (5-HT) reuptake transporters, thus elevating synaptic 5-HT levels and, finally, ameliorates ...