Inhibition of human carboxylesterases hCE1 and hiCE by cholinesterase inhibitors
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چکیده
منابع مشابه
Reversible inhibition of human carboxylesterases by acyl glucuronides.
UNLABELLED Carboxylesterases hydrolyze esters, amides, and thioesters to produce carboxylic acids and resulting alcohols, amines, and thiols, respectively. Uridine 5'-diphosphate- glucuronosyltransferases are colocalized with carboxylesterases and have the potential to further metabolize carboxylic acids to acyl glucuronides, but it is currently unknown if acyl glucuronides, being esters, also ...
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The power of chosen carbamates and hydrazinium derivatives (carbazates) to inhibit the hydrolysis of acetylthiocholine by butyrylcholinesterase or acetylcholinesterase was tested. The determined pI50 values (= negative logarithm of the molar concentration inhibiting the enzyme activity by 50%) of the tested substances were compared with pI50 values of the commercially used drugs for the Alzheim...
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The dose-limiting toxicity of the highly effective anticancer agent 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxy-camptothecin (irinotecan; CPT-11) is delayed diarrhea. This is thought to be caused by either bacteria-mediated hydrolysis of the glucuronide conjugate of the active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38) or direct conversion of CPT-11 to SN-38 by carboxylesterase...
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The pI50 index and separation coefficients of chosen 3-N,N-diethylaminophenyl-N',N'-dialkylcarbamates were determined. Index pL50 (pI50 = negative logarithm of molar concentration of inhibitor inhibiting the enzyme activity by 50%) describes the effectiveness of the inhibitor. The rate of ability of the inhibitor to pass the blood-brain barrier is usually described by the separation coefficient...
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Esterases catalyze the hydrolysis of therapeutic drugs containing esters or amides in their structures. Human carboxylesterase (CES) and arylacetamide deacetylase (AADAC) are the major enzymes that catalyze the hydrolysis of drugs in the liver. Characterization of the enzyme(s) responsible for drug metabolism is required in drug development and to realize optimal drug therapy. Because multiple ...
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ژورنال
عنوان ژورنال: Chemico-Biological Interactions
سال: 2013
ISSN: 0009-2797
DOI: 10.1016/j.cbi.2012.10.018