Discovery of Novel Insulin-Like Growth Factor-1 Receptor Inhibitors with Unique Time-Dependent Binding Kinetics

[Image: see text] This letter describes a series of small molecule inhibitors of IGF-1R with unique time-dependent binding kinetics and slow off-rates. Structure–activity and structure–kinetic relationships were elucidated and guided further optimizations within the series, culminating in compound 2...

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Autori principali: Jin, Meizhong, Petronella, Brenda A., Cooke, Andy, Kadalbajoo, Mridula, Siu, Kam W., Kleinberg, Andrew, May, Earl W., Gokhale, Prafulla C., Schulz, Ryan, Kahler, Jennifer, Bittner, Mark A., Foreman, Kenneth, Pachter, Jonathan A., Wild, Robert, Epstein, David, Mulvihill, Mark J.
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2013
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027544/
https://ncbi.nlm.nih.gov/pubmed/24900721
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml400160a
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