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. Author manuscript; available in PMC: 2017 May 17.
Published in final edited form as: Anal Chem. 2016 Nov 11;88(23):11860–11867. doi: 10.1021/acs.analchem.6b03621

Table 4.

Inhibition of MTAP/MTAN with Transition State Analogue Inhibitorsa

MT-ImmA Ki
MT-DADMe-ImmA Ki
pCl-PhT-DADMe-ImmA Ki
enzyme measured literature measured literature measured literature
hsMTAP 330 ± 68 pM 1 ± 0.5 nM 63 ± 10 pM 90 ± 10 pM 47 ± 13 pM 10 ± 5 pM
hpMTAN 66 ± 11 pM 40 ± 20 pM 15 ± 1.4 pM 89 ± 19 pM 360 ± 32 pM 570 ± 90 pM
a

The Ki values of three transition state analogues were measured (Figures 3 and 4) and compared to literature values. Most values are similar to previously reported values, but show a smaller margin of error.21,22