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Example sentences for: fhit
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Sodium salts of each compound were titrated into assays of purified Fhit [ 16 ] with 1.8 μM fluorescent substrate, Appp-S-(4-4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacine-3-yl)methylaminoacetyl (ApppBODIPY) [ 10 ] , and competitive K i values were obtained by calculating the inhibitor concentration-dependence in reduction of k cat / K m (apparent) for substrate hydrolysis [ 10 ] . As shown in Table 1, inhibitors 2b and 3b with two-carbon diol linkers were either only as inhibitory as the natural substrate 1 or substantially less so.
Derivatives of pentaerythritol, tetrapodal compounds 12,13 and 14, were also evaluated for Fhit inhibition.
Although human biochemists can depress activity more than 10 5-fold in Fhit [ 35, 36] and Hint [ 30] with a single active-site His mutation, hens apparently continued to peck at the sequence of Hint, altering all four of the absolutely conserved His residues.
The phosphorothioate analogs, 5b and 6b, bound approximately 10 and 75 times better to Fhit than 1 . Thus, conservation of bond-lengths between adenylate moieties of 1 , 5 and 6 is conducive to binding Fhit.
We presume that compounds 6b , 12b and 13b with 2, 3 or 4 identical CH 2 -phosphorothioadenosyl groups can present a manganese bound 6b -like complex to Fhit in a similar manner.
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