Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01715
Abstract: The cytosolic Hsp90-selective inhibitor TAS-116 has an acceptable safety profile and promising antitumor activity in clinical trials. We examined the binding characteristics of TAS-116 and its analogs to determine the impact of the ligand binding… read more here.
Keywords: potency selectivity; hsp90; cytosolic hsp90; selectivity cytosolic ... See more keywords
Discovery of a Small Side Cavity in Sphingosine Kinase 2 that Enhances Inhibitor Potency and Selectivity.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01508
Abstract: The sphingosine-1-phosphate (S1P) signaling pathway is an attractive drug target due to its involvement in immune cell chemotaxis and vascular integrity. The formation of S1P is catalyzed by sphingosine kinase 1 or 2 (SphK1 or… read more here.
Keywords: potency selectivity; sphingosine kinase; inhibitor; potency ... See more keywords
Tuning ITAM multiplicity on T cell receptors can control potency and selectivity to ligand density
Sign Up to like & getrecommendations! Published in 2018 at "Science Signaling"
DOI: 10.1126/scisignal.aan1088
Abstract: Modeling the responses of synthetic receptors in T cells identifies new ways to optimize CAR–T cell activity. ITAM abundance increases receptor potency T cells transduce extracellular signals by phosphorylating immunoreceptor tyrosine-based activation motifs (ITAMs) within… read more here.
Keywords: potency selectivity; potency; receptor; cell ... See more keywords