Sanja Koštrun

TL;DR: Western blot analyses showed different mechanisms of cytostatic activity between compounds 10c and 11f that could be associated with the nature of aromatic substituent at 1-(1,2,3-triazolyl) and amidino moiety at C-5 position of benzimidazole ring.

TL;DR: The development of the first models for macrolide cellular pharmacokinetics was described, using relatively easily determined and conceptually simple descriptors: experimentally determined physicochemical parameters ChromlogD and CHI IAM, as well as a calculated number of positively charged atoms (POS).

TL;DR: It is concluded that LPS-stimulated J774A.1 cells in presented experimental setup are not a representative cellular model for the evaluation of macrolide anti-inflammatory potential in clinical trials, and shows that, at least in in vitro models, binding to biological membranes may be the crucial factor of Macrolide mechanism of action.

TL;DR: The three-dimensional structure of Fyn tyrosine kinase, a Src-family enzyme involved in T-cell receptor signal transduction, is presented and it is revealed that Fyn is inhibited by a linear-mixed noncompetitive mechanism of inhibition by rosmarinic acid.

TL;DR: It has been found that macrolides and small molecules have similar lipophilicity profiles, though macrolide show weaker PPB and have better solubility than small discovery molecules.