| http://purl.uniprot.org/citations/21481795 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/21481795 | http://www.w3.org/2000/01/rdf-schema#comment | "Acquired resistance to ABL1 tyrosine kinase inhibitors (TKIs) through ABL1 kinase domain mutations, particularly the gatekeeper mutant T315I, is a significant problem for patients with chronic myeloid leukemia (CML). Using structure-based drug design, we developed compounds that bind to residues (Arg386/Glu282) ABL1 uses to switch between inactive and active conformations. The lead "switch-control" inhibitor, DCC-2036, potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant CML-resistance mutants, including T315I. DCC-2036 inhibits BCR-ABL1(T315I)-expressing cell lines, prolongs survival in mouse models of T315I mutant CML and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing T315I in vitro and in vivo, supporting its clinical development in TKI-resistant Ph(+) leukemia."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.ccr.2011.03.003"xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Stewart L.J."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Clark R."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Lu W.P."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Miller D."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Van Etten R.A."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Jones J."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Yao T."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Chun L."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Smith B.D."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Ahn Y.M."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Haack T."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Gavrilescu L.C."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Patt W.C."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Kaufman M.D."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Chan W.W."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Petillo P.A."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Evangelista P."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Lazarides K."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Zaleskas V.M."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Ensinger C.L."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Flynn D.L."xsd:string |
| http://purl.uniprot.org/citations/21481795 | http://purl.uniprot.org/core/author | "Hood M.M."xsd:string |