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Phenylalkyl ketones as potent reversible inhibitors of interleukin-1β converting enzyme |
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| Authors: | Adnan M. M. Mjalli Kevin T. Chapman Malcolm MacCoss Nancy A. Thornberry |
| Affiliation: | Department of Medicinal Chemical Research, Merck Research Laboratories Rahway, New Jersey 07065 U.S.A. a Department of Medicinal Chemical Research, Merck Research Laboratories Rahway, New Jersey 07065 U.S.A. |
| Abstract: | Phenylalkyl ketones are potent reversible inhibitors of interleukin-1β converting enzyme (ICE). The extended alkyl chain ketones AcTyrValAlaAspCO(CH2)nPh display increased potency over the simple aryl ketone. In particular, the tetrapeptide AcTyrValAlaAspCOPh has a Ki of 10μM while AcTyrValAlaAspCO(CH2)5Ph has a Ki of 18.5nM. |
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