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

Table 3. Inhibition constants (Ki) of MMP1CAT and MMP10CAT with N-TIMP2 selective variants.

Ki* (nM) Fold change of Ki** Specificity shift
Clone MMP1CAT MMP10CAT MMP1CAT MMP10CAT MMP1CAT MMP10CAT
N-TIMP2WT 0.7 ± 0.1 3.5 ± 0.8
N-TIMP214_17 0.92 ± 0.15 3.2 ± 0.4 0.8 1.1 212# 154#
N-TIMP29_13 18 ± 8 40 ± 14 0.04 0.08 10+ 5+

*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 clone N-TIMP214_17, specificity shifts were calculated as the ratio between the fold improvement to MMP14CAT, as compared to MMP1CAT and MMP10CAT (the specificity shift is defined as the fold change of Ki for MMP14/fold change of Ki for MMPX, where X designates either MMP1CAT or MMP10CAT).

+ For the MMP9-inhibiting clone N-TIMP29_13, specificity shifts were calculated as the ratio between the fold of improvement to MMP9CAT in comparison to MMP1CAT and MMP10CAT (the specificity shift is defined as the fold change of Ki for MMP9/fold change of Ki for MMPX, where X designates either MMP1CAT or MMP10CAT).

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