Description |
-
Abstract:
Receptor-interacting protein kinase 2 (RIPK2) mediates inflammatory signaling by the
bacteria-sensing receptors Nucleotide-binding oligomerization domain-containing protein
1 and 2 (NOD1 and NOD2). Kinase inhibitors targeting RIPK2 are a proposed strategy to
ameliorate NOD-mediated pathologies. Such as Crohn's diseases, Sarcoidosis, and
inflammatory arthritis. For the further ... read moreinvestigation of the RIPK2 function, finding or
designing potent inhibitors is pretty important. Here we designed several inhibitors. To
test their activity, we had three different methods, which can fully expose the activity
of RIPK2 inhibitors. According to the HEK-BLUE assay, ADP-Glo assay as well as the
Nano-BRET assay, we found several CSLP compounds show potent activity. Based on the
residence time, we found there is no direct connection between the IC50 and the
residence time. This project can provide strong date for further investigation of the
function of the RIPK2 as well as the in-vivo
experiment.
Thesis (M.S.)--Tufts University,
2018.
Submitted to the Dept. of Pharmacology and
Drug Development.
Advisor: Alexei
Degterev.
Committee: David
Greenblatt.
Keyword:
Pharmacology.read less
|
This object is in collection