PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 26622180-3 2015 Nintedanib is a small-molecule tyrosine kinase inhibitor that targets receptors for vascular endothelial growth factor, platelet-derived growth factor, and fibroblast growth factor as well as RET (rearranged during transfection) and Flt3. nintedanib 0-10 ret proto-oncogene Homo sapiens 192-195 26677336-6 2015 Nintedanib (formally known as BIBF 1120) is a triple angiokinase inhibitor of VEGF, fibroblast growth factor, platelet-derived growth factor signaling with lesser activity against RET, Flt-3, and Src. nintedanib 0-10 ret proto-oncogene Homo sapiens 180-183 26677336-6 2015 Nintedanib (formally known as BIBF 1120) is a triple angiokinase inhibitor of VEGF, fibroblast growth factor, platelet-derived growth factor signaling with lesser activity against RET, Flt-3, and Src. nintedanib 30-39 ret proto-oncogene Homo sapiens 180-183 26622180-3 2015 Nintedanib is a small-molecule tyrosine kinase inhibitor that targets receptors for vascular endothelial growth factor, platelet-derived growth factor, and fibroblast growth factor as well as RET (rearranged during transfection) and Flt3. nintedanib 0-10 ret proto-oncogene Homo sapiens 197-227 25012508-1 2014 BACKGROUND: Nintedanib is a potent, oral angiokinase inhibitor that targets VEGF, PDGF and FGF signalling, as well as RET and Flt3. nintedanib 12-22 ret proto-oncogene Homo sapiens 118-121 31118272-0 2019 Structural basis of resistance of mutant RET protein-tyrosine kinase to its inhibitors nintedanib and vandetanib. nintedanib 87-97 ret proto-oncogene Homo sapiens 41-44 31118272-4 2019 Nintedanib is a RET TKI that inhibits the vandetanib-resistant RET(G810A) mutant. nintedanib 0-10 ret proto-oncogene Homo sapiens 16-19 31118272-4 2019 Nintedanib is a RET TKI that inhibits the vandetanib-resistant RET(G810A) mutant. nintedanib 0-10 ret proto-oncogene Homo sapiens 63-66 31118272-5 2019 Here, we determined the X-ray co-crystal structure of RET kinase domain-nintedanib complex to 1.87 A resolution and a RET(G810A) kinase domain crystal structure to 1.99 A resolution. nintedanib 72-82 ret proto-oncogene Homo sapiens 54-57 31118272-7 2019 Drug-sensitivity profiling of RET(L881V) revealed that it remains sensitive to nintedanib. nintedanib 79-89 ret proto-oncogene Homo sapiens 30-33 31118272-8 2019 The RET-nintedanib co-crystal structure disclosed that Leu-730 in RET engages in hydrophobic interactions with the piperazine, anilino, and phenyl groups of nintedanib, providing a structural basis for explaining that the p.L730V mutation identified in nine independently isolated cell lines resistant to nintedanib. nintedanib 8-18 ret proto-oncogene Homo sapiens 4-7 31118272-8 2019 The RET-nintedanib co-crystal structure disclosed that Leu-730 in RET engages in hydrophobic interactions with the piperazine, anilino, and phenyl groups of nintedanib, providing a structural basis for explaining that the p.L730V mutation identified in nine independently isolated cell lines resistant to nintedanib. nintedanib 8-18 ret proto-oncogene Homo sapiens 66-69 31118272-8 2019 The RET-nintedanib co-crystal structure disclosed that Leu-730 in RET engages in hydrophobic interactions with the piperazine, anilino, and phenyl groups of nintedanib, providing a structural basis for explaining that the p.L730V mutation identified in nine independently isolated cell lines resistant to nintedanib. nintedanib 157-167 ret proto-oncogene Homo sapiens 4-7 31118272-8 2019 The RET-nintedanib co-crystal structure disclosed that Leu-730 in RET engages in hydrophobic interactions with the piperazine, anilino, and phenyl groups of nintedanib, providing a structural basis for explaining that the p.L730V mutation identified in nine independently isolated cell lines resistant to nintedanib. nintedanib 157-167 ret proto-oncogene Homo sapiens 66-69 31118272-8 2019 The RET-nintedanib co-crystal structure disclosed that Leu-730 in RET engages in hydrophobic interactions with the piperazine, anilino, and phenyl groups of nintedanib, providing a structural basis for explaining that the p.L730V mutation identified in nine independently isolated cell lines resistant to nintedanib. nintedanib 157-167 ret proto-oncogene Homo sapiens 4-7 31118272-8 2019 The RET-nintedanib co-crystal structure disclosed that Leu-730 in RET engages in hydrophobic interactions with the piperazine, anilino, and phenyl groups of nintedanib, providing a structural basis for explaining that the p.L730V mutation identified in nine independently isolated cell lines resistant to nintedanib. nintedanib 157-167 ret proto-oncogene Homo sapiens 66-69 34725737-0 2021 How does nintedanib overcome cancer drug-resistant mutation of RET protein-tyrosine kinase: insights from molecular dynamics simulations. nintedanib 9-19 ret proto-oncogene Homo sapiens 63-66 34725737-5 2021 Nintedanib can effectively inhibit the RET L881V mutant, whereas its analog compound 1 is unable to combat this mutant. nintedanib 0-10 ret proto-oncogene Homo sapiens 39-42 34725737-7 2021 Here, molecular dynamics (MD) simulations, binding free energy calculations, and structural analysis were performed to uncover the mechanism of overcoming the resistance of RET L881V mutant to nintedanib. nintedanib 193-203 ret proto-oncogene Homo sapiens 173-176 31118272-9 2019 Comparisons of RET-nintedanib, RET(G810A), and RET-vandetanib crystal structures suggested that the solvent-front Ala-810 makes hydrophobic contacts with a methyl group and aniline in nintedanib and blocks water access to two oxygen atoms of vandetanib, resulting in an energetic penalty for burying polar groups. nintedanib 19-29 ret proto-oncogene Homo sapiens 15-18 31118272-10 2019 Of note, even though the p.L881V mutation did not affect sensitivity to nintedanib, RET(L881V) was resistant to nintedanib analogs lacking a phenyl group. nintedanib 112-122 ret proto-oncogene Homo sapiens 84-87 31118272-11 2019 These results provide structural insights into resistance of RET mutants against the TKIs nintedanib and vandetanib. nintedanib 90-100 ret proto-oncogene Homo sapiens 61-64 29908090-3 2018 EXPERIMENTAL APPROACH: We identified and analysed mutations in the RET kinase domain that conferred resistance to the TKIs cabozantinib, lenvatinib, vandetanib and nintedanib using RET kinase-dependent BaF3/KIF5B-RET (BaF3/KR) cells. nintedanib 164-174 ret proto-oncogene Homo sapiens 181-184