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. 2018 Aug 10;9(62):32036–32053. doi: 10.18632/oncotarget.25885

Table 2. Inhibition constants (Ki) of MMP14 and MMP9 with N-TIMP2 selective variants.

Ki* (nM) Fold change of Ki**
Clone MMP14CAT MMP9CAT MMP14CAT MMP9CAT Specificity shift***
N-TIMP2WT 5 ± 1 0.5 ± 0.04
N-TIMP214_17 0.03 ± 0.003 3.58 ± 0.5 170 0.14 1175
N-TIMP214_18 0.024 ± 0.005 1.25 ± 0.2 211 0.41 512
N-TIMP29_1 240 ± 31 0.78 ± 0.02 0.021 0.66 31
N-TIMP29_13 832 ± 44 1.2 ± 0.007 0.006 0.41 68

*Ki values (nM) of the purified variants were obtained by fitting the experimental data to Morrison's tight binding equation (Eq. 1).

**Fold change of Ki reflects the ratio between the Ki of N-TIMP2WT and the Ki of an N-TIMP2 variant.

***For the MMP14-inhibiting clones N-TIMP214_17 and N-TIMP214_18, specificity shifts were calculated as the ratio between the fold improvement to MMP14CAT, as compared to MMP9CAT (the specificity shift is defined as the fold change of Ki for MMP14/fold change of Ki for MMP9). For the MMP9-inhibiting clones N-TIMP29_1 and N-TIMP29_13, specificity shifts were calculated as the ratio between the fold of improvement to MMP9 in comparison to MMP14 (the specificity shift is defined as the fold change of Ki for MMP9/fold change of Ki for MMP14).