2auz: Difference between revisions

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==Overview==
==Overview==
Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of, semicarbazone-based cathepsin K inhibitors with greater solubility and, better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an, ex vivo rat calvarial bone resorption model. However, based on enzyme, inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and, 13C NMR experiments, these semicarbazones probably function as prodrugs of, aldehydes.
Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.


==Disease==
==Disease==
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Adkison, K.K.]]
[[Category: Adkison, K K.]]
[[Category: Barrett, D.G.]]
[[Category: Barrett, D G.]]
[[Category: Deaton, D.N.]]
[[Category: Deaton, D N.]]
[[Category: Gampe, R.T.]]
[[Category: Gampe, R T.]]
[[Category: Hassell, A.M.]]
[[Category: Hassell, A M.]]
[[Category: Long, S.T.]]
[[Category: Long, S T.]]
[[Category: McFadyen, R.B.]]
[[Category: McFadyen, R B.]]
[[Category: Miller, A.B.]]
[[Category: Miller, A B.]]
[[Category: Miller, L.R.]]
[[Category: Miller, L R.]]
[[Category: Shewchuk, L.M.]]
[[Category: Shewchuk, L M.]]
[[Category: CT2]]
[[Category: CT2]]
[[Category: SO4]]
[[Category: SO4]]
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[[Category: cysteine protease]]
[[Category: cysteine protease]]


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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:31:17 2008''