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• W1983676465 endingPage "12033" @default.
• W1983676465 startingPage "12028" @default.
• W1983676465 abstract "Inhibition of aminopeptidase N and neutral endopeptidase-24.11, two zinc metallopeptidases involved in the inactivation of the opioid peptides enkephalins, produces potent physiological analgesic responses, without major side-effects, in all animal models of pain in which morphine is active. Dual inhibitors of both enzymes could fill the gap between opioid analgesics and antalgics. Until now, attempts to find a compound with high affinity both for neutral endopeptidase and aminopeptidase N have failed. We report here the design of dual competitive inhibitors of both enzymes with K I values in the nanomolar range. These have been obtained by selecting R 1 , R 2, and R 3 determinants in aminophosphinic-containing inhibitors: NH 2 —CH(R 1 )P(O)—(OH)CH 2 —CH(R 2 )CONH—CH(R 3 )COOH, for optimal recognition of the two enkephalin inactivating enzymes, whose active site peculiarities, determined by site-directed mutagenesis, have been taken into account. The best inhibitors were 10× more potent than described dual inhibitors in alleviating acute and inflammatory nociceptive stimuli in mice, thus providing a basis for the development of a family of analgesics devoid of opioid side effects." @default.
• W1983676465 created "2016-06-24" @default.
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• W1983676465 date "1998-09-29" @default.
• W1983676465 modified "2023-10-18" @default.
• W1983676465 title "Aminophosphinic inhibitors as transition state analogues of enkephalin-degrading enzymes: A class of central analgesics" @default.
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• W1983676465 doi "https://doi.org/10.1073/pnas.95.20.12028" @default.
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