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SGX393 inhibits the CML mutant Bcr-AblT315I and preempts in vitro resistance when combined with nilotinib or dasatinib.
O'Hare T, Eide CA, Tyner JW, Corbin AS, Wong MJ, Buchanan S, Holme K, Jessen KA, Tang C, Lewis HA, Romero RD, Burley SK, Deininger MW. O'Hare T, et al. Among authors: romero rd. Proc Natl Acad Sci U S A. 2008 Apr 8;105(14):5507-12. doi: 10.1073/pnas.0800587105. Epub 2008 Mar 26. Proc Natl Acad Sci U S A. 2008. PMID: 18367669 Free PMC article.
Structures of a minimal human CFTR first nucleotide-binding domain as a monomer, head-to-tail homodimer, and pathogenic mutant.
Atwell S, Brouillette CG, Conners K, Emtage S, Gheyi T, Guggino WB, Hendle J, Hunt JF, Lewis HA, Lu F, Protasevich II, Rodgers LA, Romero R, Wasserman SR, Weber PC, Wetmore D, Zhang FF, Zhao X. Atwell S, et al. Protein Eng Des Sel. 2010 May;23(5):375-84. doi: 10.1093/protein/gzq004. Epub 2010 Feb 11. Protein Eng Des Sel. 2010. PMID: 20150177