The double mutation of both residues further compromises cation selectivity.
Additional hydrogen bonds to kinase hinge do not necessarily correlate with an increase in potency; conversely they appear to compromise kinase selectivity.
We find that mutation of the S4 segment's third arginine R211 (R3) compromises proton selectivity, enabling conduction of a metal cation and even of the large organic cation guanidinium, reminiscent of Shaker's omega pore.
While greater doses of SYKi could be administered to likely enhance efficacy, we did not want to compromise kinase selectivity.
A single oral dose of tofacitinib or PRT062607 in naive mice resulted in a rapid increase of plasma levels (tmax = 1 3 h), reaching maximal concentrations that did not compromise kinase selectivity, and were completely cleared daily.
But the efficacy of PDT was compromised by insufficient selectivity and low solubility.
However, the PDT efficacy is compromised by insufficient selectivity and low solubility.
Results indicate that, because of membrane thickness, selectivity was compromised by facilitation of CO2 transport.
However substrate selectivity is compromised due to metabolism by the human one- and two-electron oxidoreductases cytochrome P450 oxidoreductase (POR) and aldo-keto reductase 1C3 (AKR1C3).
Localization is compromised by the sequence selectivity of RNase digestion.
