The synthesis, in vitro activity, and in vivo profile of this class of inhibitors is outlined.
The 5-substituent is also a critical determinant of the characteristic corepressor recruitment profile of this class of FXR antagonists, though distinct mechanisms appear to be involved: 15h stabilizes the corepressor-nuclear receptor interaction, while 15g inhibits coactivator recruitment.
This fact, together with the low side-effect profile of this class of drug, makes selective COX-2 inhibitors a safe therapeutic option in this type of headache [26, 27].
Therefore, we further investigated the expression profiling of this class.
A topical JAK inhibitor may decrease the risk/benefit profile of this class of drugs.
The distinct efficacy and safety profile of this class of drugs provides a novel approach for add-on therapy in the event of failure of other antidiabetic agents.
Reviews that address the 'steroid-sparing' or rescue medication reduction features of various approaches to the pharmacological treatment of asthma are an important sub-group of studies, given the known side-effect profile of this class of drugs [ 62, 64- 66, 68, 70- 75, 77, 77, 82- 84, 87, 88, 92, 93, 96, 98, 103- 105].
The potent cell-based activity prompted us to investigate kinome selectivity profiles for this class of compound by screening 7a and 7d in a 102-kinase panel at a concentration of 1 μM.
Additional safety assessments did not reveal any unexpected results beyond the known AE profile for this class of medication.
