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As a system of encoding data, PKI was sound and reliable.
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Table S4 presents the raw data transformed into pKi values.
The potency values obtained for JNJ10397049 are consistent with previously published pKi data [5.7 and 8.2, respectively, 14].
Our data demonstrated that PKI-587 cells display improved antitumour activity when combined with cetuximab in resistant Kyse30 xenografts, with a prolonged advantage in terms of survival, compared with single-agent therapies.
All data are given as pKi values at human recombinant receptors, except when stated otherwise: rodent (r) receptors; N.D., not determined; *These pK i values are referred for the respective family receptor.
Our data demonstrated that when PKI-587 is used in combination with cetuximab, despite the inhibition of proliferation and induction of cell death that are observed in either cetuximab-sensitive or -resistant cells, a caspase-dependent activation of apoptosis is detected primarily in sensitive cell lines.
The PKI concentrates on data integrity and authentication schemes.
The pcDNA-NES vector (from Soner Gundemir, unpublished data) contains the NES of PKI alpha in a pcDNA3.1 (Invitrogen) backbone.
14 The biological data was further converted to pKi (exp) (negative decimal logarithm of experimental inhibition constant) parameters using the pIC50 value calculator 31 according to the Michaelis Menten enzyme substrate interaction equation for noncompetitive species: 32 where S is the substrate concentration and Km is the Michaelis Menten constant.
Our data demonstrate that the treatment with PKI-587 is able to enhance sensitivity to cetuximab in HNSCC cells in vitro and to revert constitutive or acquired resistance.
For the screening evaluation, the learned model is used to rank the respective screening data set according to the learned property (i.e. pKi or pIC50).
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