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Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties.
Bono F, De Smet F, Herbert C, De Bock K, Georgiadou M, Fons P, Tjwa M, Alcouffe C, Ny A, Bianciotto M, Jonckx B, Murakami M, Lanahan AA, Michielsen C, Sibrac D, Dol-Gleizes F, Mazzone M, Zacchigna S, Herault JP, Fischer C, Rigon P, Ruiz de Almodovar C, Claes F, Blanc I, Poesen K, Zhang J, Segura I, Gueguen G, Bordes MF, Lambrechts D, Broussy R, van de Wouwer M, Michaux C, Shimada T, Jean I, Blacher S, Noel A, Motte P, Rom E, Rakic JM, Katsuma S, Schaeffer P, Yayon A, Van Schepdael A, Schwalbe H, Gervasio FL, Carmeliet G, Rozensky J, Dewerchin M, Simons M, Christopoulos A, Herbert JM, Carmeliet P. Bono F, et al. Among authors: christopoulos a. Cancer Cell. 2013 Apr 15;23(4):477-88. doi: 10.1016/j.ccr.2013.02.019. Cancer Cell. 2013. PMID: 23597562 Free article.
Allosteric targeting of receptor tyrosine kinases.
De Smet F, Christopoulos A, Carmeliet P. De Smet F, et al. Among authors: christopoulos a. Nat Biotechnol. 2014 Nov;32(11):1113-20. doi: 10.1038/nbt.3028. Nat Biotechnol. 2014. PMID: 25380447
Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery.
Harikumar KG, Wootten D, Pinon DI, Koole C, Ball AM, Furness SG, Graham B, Dong M, Christopoulos A, Miller LJ, Sexton PM. Harikumar KG, et al. Among authors: christopoulos a. Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18607-12. doi: 10.1073/pnas.1205227109. Epub 2012 Oct 22. Proc Natl Acad Sci U S A. 2012. PMID: 23091034 Free PMC article.
The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism.
Wootten D, Reynolds CA, Smith KJ, Mobarec JC, Koole C, Savage EE, Pabreja K, Simms J, Sridhar R, Furness SGB, Liu M, Thompson PE, Miller LJ, Christopoulos A, Sexton PM. Wootten D, et al. Among authors: christopoulos a. Cell. 2016 Jun 16;165(7):1632-1643. doi: 10.1016/j.cell.2016.05.023. Cell. 2016. PMID: 27315480 Free PMC article.
Overview of receptor allosterism.
Gregory KJ, Sexton PM, Christopoulos A. Gregory KJ, et al. Among authors: christopoulos a. Curr Protoc Pharmacol. 2010 Dec;Chapter 1:Unit 1.21. doi: 10.1002/0471141755.ph0121s51. Curr Protoc Pharmacol. 2010. PMID: 21935895
433 results