681802-79-9Relevant academic research and scientific papers
Structure-based de novo design of ligands using a three-dimensional model of the insulin receptor
Tan, Christopher,Wei, Lianhu,Ottensmeyer, F. Peter,Goldfine, Ira,Maddux, Betty A.,Yip, Cecil C.,Batey, Robert A.,Kotra, Lakshmi P.
, p. 1407 - 1410 (2004)
For the first time, a three-dimensional model of the insulin receptor is used in the de novo design of novel ligands that potentially mimic interactions of insulin at its receptor. Compound 4 competed with insulin as seen in autophosphorylation assays and inhibited up to 68% of IR autophosphorylation at 300 μM of 4 in 3T3IR cells induced by 1 nM insulin. This model provides a basis for the design of potent insulin receptor ligands.
