PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 34599023-1 2021 BACKGROUND: Sitravatinib, a tyrosine kinase inhibitor that targets TYRO3, AXL, MERTK and the VEGF receptor family, is predicted to increase the M1 to M2-polarized tumor-associated macrophages ratio in the tumor microenvironment and have synergistic antitumor activity in combination with anti-programmed death-1/ligand-1 agents. sitravatinib 12-24 TYRO3 protein tyrosine kinase Homo sapiens 67-72 34599023-1 2021 BACKGROUND: Sitravatinib, a tyrosine kinase inhibitor that targets TYRO3, AXL, MERTK and the VEGF receptor family, is predicted to increase the M1 to M2-polarized tumor-associated macrophages ratio in the tumor microenvironment and have synergistic antitumor activity in combination with anti-programmed death-1/ligand-1 agents. sitravatinib 12-24 AXL receptor tyrosine kinase Homo sapiens 74-77 34599023-1 2021 BACKGROUND: Sitravatinib, a tyrosine kinase inhibitor that targets TYRO3, AXL, MERTK and the VEGF receptor family, is predicted to increase the M1 to M2-polarized tumor-associated macrophages ratio in the tumor microenvironment and have synergistic antitumor activity in combination with anti-programmed death-1/ligand-1 agents. sitravatinib 12-24 MER proto-oncogene, tyrosine kinase Homo sapiens 79-84 32525624-0 2020 Modulating the function of ABCB1: in vitro and in vivo characterization of sitravatinib, a tyrosine kinase inhibitor. sitravatinib 75-87 ATP binding cassette subfamily B member 1 Homo sapiens 27-32 32525624-2 2020 In this work, we evaluated the sensitizing effect of sitravatinib, a broad-spectrum tyrosine kinase inhibitor (TKI), on ATP-binding cassette subfamily B member 1 (ABCB1)- and ATP-binding cassette subfamily C member 10 (ABCC10)-mediated MDR. sitravatinib 53-65 ATP binding cassette subfamily B member 1 Homo sapiens 120-161 32525624-2 2020 In this work, we evaluated the sensitizing effect of sitravatinib, a broad-spectrum tyrosine kinase inhibitor (TKI), on ATP-binding cassette subfamily B member 1 (ABCB1)- and ATP-binding cassette subfamily C member 10 (ABCC10)-mediated MDR. sitravatinib 53-65 ATP binding cassette subfamily B member 1 Homo sapiens 163-168 32525624-2 2020 In this work, we evaluated the sensitizing effect of sitravatinib, a broad-spectrum tyrosine kinase inhibitor (TKI), on ATP-binding cassette subfamily B member 1 (ABCB1)- and ATP-binding cassette subfamily C member 10 (ABCC10)-mediated MDR. sitravatinib 53-65 ATP binding cassette subfamily C member 10 Homo sapiens 175-217 32525624-2 2020 In this work, we evaluated the sensitizing effect of sitravatinib, a broad-spectrum tyrosine kinase inhibitor (TKI), on ATP-binding cassette subfamily B member 1 (ABCB1)- and ATP-binding cassette subfamily C member 10 (ABCC10)-mediated MDR. sitravatinib 53-65 ATP binding cassette subfamily C member 10 Homo sapiens 219-225 32525624-6 2020 RESULTS: Sitravatinib considerably reversed MDR mediated by ABCB1 and partially antagonized ABCC10-mediated MDR. sitravatinib 9-21 ATP binding cassette subfamily B member 1 Homo sapiens 60-65 32525624-6 2020 RESULTS: Sitravatinib considerably reversed MDR mediated by ABCB1 and partially antagonized ABCC10-mediated MDR. sitravatinib 9-21 ATP binding cassette subfamily C member 10 Homo sapiens 92-98 32525624-7 2020 Our in silico docking simulation analysis indicated that sitravatinib strongly and stably bound to the transmembrane domain of ABCB1 human-mouse chimeric model. sitravatinib 57-69 ATP binding cassette subfamily B member 1 Homo sapiens 127-132 32525624-8 2020 Furthermore, sitravatinib inhibited hydrolysis of ATP and synchronously decreased the efflux function of ABCB1. sitravatinib 13-25 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 105-110 32525624-11 2020 More importantly, sitravatinib could remarkably restore the antitumor activity of vincristine in ABCB1-mediated xenograft model without observable toxic effect. sitravatinib 18-30 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 97-102 31941029-0 2020 Sitravatinib Sensitizes ABCB1- and ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs. sitravatinib 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 24-29 32477943-0 2020 Sitravatinib, a Tyrosine Kinase Inhibitor, Inhibits the Transport Function of ABCG2 and Restores Sensitivity to Chemotherapy-Resistant Cancer Cells in vitro. sitravatinib 0-12 TXK tyrosine kinase Homo sapiens 16-31 32477943-0 2020 Sitravatinib, a Tyrosine Kinase Inhibitor, Inhibits the Transport Function of ABCG2 and Restores Sensitivity to Chemotherapy-Resistant Cancer Cells in vitro. sitravatinib 0-12 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 78-83 32477943-1 2020 Sitravatinib, also called MGCD516 or MG-516, is a broad-spectrum tyrosine kinase inhibitor (TKI) under phase III clinical evaluation. sitravatinib 0-12 TXK tyrosine kinase Homo sapiens 65-80 32477943-1 2020 Sitravatinib, also called MGCD516 or MG-516, is a broad-spectrum tyrosine kinase inhibitor (TKI) under phase III clinical evaluation. sitravatinib 26-33 TXK tyrosine kinase Homo sapiens 65-80 32477943-1 2020 Sitravatinib, also called MGCD516 or MG-516, is a broad-spectrum tyrosine kinase inhibitor (TKI) under phase III clinical evaluation. sitravatinib 37-43 TXK tyrosine kinase Homo sapiens 65-80 32477943-2 2020 Herein, we explored the activity of sitravatinib toward multidrug resistance (MDR) by emphasizing its inhibitory effect on ATP-binding cassette super-family G member 2 (ABCG2). sitravatinib 36-48 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 123-167 32477943-2 2020 Herein, we explored the activity of sitravatinib toward multidrug resistance (MDR) by emphasizing its inhibitory effect on ATP-binding cassette super-family G member 2 (ABCG2). sitravatinib 36-48 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 169-174 32477943-5 2020 Also, an MTT assay indicated that sitravatinib at 3 muM had the ability to restore the antineoplastic effect of various ABCG2 substrates in both drug-selected and gene-transfected ABCG2-overexpressing cell lines. sitravatinib 34-46 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 120-125 32477943-5 2020 Also, an MTT assay indicated that sitravatinib at 3 muM had the ability to restore the antineoplastic effect of various ABCG2 substrates in both drug-selected and gene-transfected ABCG2-overexpressing cell lines. sitravatinib 34-46 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 180-185 32477943-6 2020 In further tritium-labeled mitoxantrone transportation study, sitravatinib at 3 muM blocked the efflux function mediated by ABCG2 and as a result, increased the intracellular concentration of anticancer drugs. sitravatinib 62-74 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 124-129 32477943-8 2020 An ATPase assay demonstrated that ATPase activity of ABCG2 was inhibited in a concentration-dependent manner with sitravatinib; thus, the energy source to pump out compounds was interfered. sitravatinib 114-126 dynein axonemal heavy chain 8 Homo sapiens 3-9 32477943-8 2020 An ATPase assay demonstrated that ATPase activity of ABCG2 was inhibited in a concentration-dependent manner with sitravatinib; thus, the energy source to pump out compounds was interfered. sitravatinib 114-126 dynein axonemal heavy chain 8 Homo sapiens 34-40 32477943-8 2020 An ATPase assay demonstrated that ATPase activity of ABCG2 was inhibited in a concentration-dependent manner with sitravatinib; thus, the energy source to pump out compounds was interfered. sitravatinib 114-126 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 53-58 32477943-9 2020 Collectively, the results of this study open new avenues for sitravatinib working as an ABCG2 inhibitor which restores the antineoplastic activity of anticancer drugs known to be ABCG2 substrates. sitravatinib 61-73 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 88-93 32477943-9 2020 Collectively, the results of this study open new avenues for sitravatinib working as an ABCG2 inhibitor which restores the antineoplastic activity of anticancer drugs known to be ABCG2 substrates. sitravatinib 61-73 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 179-184 31941029-5 2020 We discovered that at submicromolar concentrations, sitravatinib re-sensitizes ABCB1- and ABCG2-overexpressing multidrug-resistant cancer cells to chemotherapeutic drugs. sitravatinib 52-64 ATP binding cassette subfamily B member 1 Homo sapiens 79-84 31941029-5 2020 We discovered that at submicromolar concentrations, sitravatinib re-sensitizes ABCB1- and ABCG2-overexpressing multidrug-resistant cancer cells to chemotherapeutic drugs. sitravatinib 52-64 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 90-95 31941029-6 2020 We found that sitravatinib blocks the drug efflux function of ABCB1 and ABCG2 in a concentration-dependent manner but does not significantly alter the protein expression of ABCB1 or ABCG2 in multidrug-resistant cancer cells. sitravatinib 14-26 ATP binding cassette subfamily B member 1 Homo sapiens 62-67 31941029-6 2020 We found that sitravatinib blocks the drug efflux function of ABCB1 and ABCG2 in a concentration-dependent manner but does not significantly alter the protein expression of ABCB1 or ABCG2 in multidrug-resistant cancer cells. sitravatinib 14-26 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 72-77 31941029-7 2020 In conclusion, we reveal a potential drug repositioning treatment option for multidrug-resistant cancers by targeting ABCB1 and ABCG2 with sitravatinib and should be further investigated in future clinical trials. sitravatinib 139-151 ATP binding cassette subfamily B member 1 Homo sapiens 118-123 31941029-7 2020 In conclusion, we reveal a potential drug repositioning treatment option for multidrug-resistant cancers by targeting ABCB1 and ABCG2 with sitravatinib and should be further investigated in future clinical trials. sitravatinib 139-151 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 128-133 31941029-0 2020 Sitravatinib Sensitizes ABCB1- and ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs. sitravatinib 0-12 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 35-40 31941029-4 2020 In the present study, we investigated the effect of sitravatinib, a novel multitargeted receptor tyrosine kinase inhibitor, on human ABCB1 and ABCG2 in multidrug-resistant cancer cell lines. sitravatinib 52-64 ATP binding cassette subfamily B member 1 Homo sapiens 133-138 31941029-4 2020 In the present study, we investigated the effect of sitravatinib, a novel multitargeted receptor tyrosine kinase inhibitor, on human ABCB1 and ABCG2 in multidrug-resistant cancer cell lines. sitravatinib 52-64 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 143-148 31369645-3 2019 Here we examined sitravatinib (MGCD516), a spectrum-selective TKI able to block MET, TAM (TYRO3, AXL, MerTK) and multiple receptor families (including PDGFRs, VEGFRs, and Ephs). sitravatinib 17-29 Myeloproliferative syndrome, transient (transient abnormal myelopoiesis) Homo sapiens 85-88 31369645-3 2019 Here we examined sitravatinib (MGCD516), a spectrum-selective TKI able to block MET, TAM (TYRO3, AXL, MerTK) and multiple receptor families (including PDGFRs, VEGFRs, and Ephs). sitravatinib 17-29 TYRO3 protein tyrosine kinase Homo sapiens 90-95 31369645-3 2019 Here we examined sitravatinib (MGCD516), a spectrum-selective TKI able to block MET, TAM (TYRO3, AXL, MerTK) and multiple receptor families (including PDGFRs, VEGFRs, and Ephs). sitravatinib 17-29 AXL receptor tyrosine kinase Homo sapiens 97-100 31369645-3 2019 Here we examined sitravatinib (MGCD516), a spectrum-selective TKI able to block MET, TAM (TYRO3, AXL, MerTK) and multiple receptor families (including PDGFRs, VEGFRs, and Ephs). sitravatinib 17-29 MER proto-oncogene, tyrosine kinase Homo sapiens 102-107 31369645-3 2019 Here we examined sitravatinib (MGCD516), a spectrum-selective TKI able to block MET, TAM (TYRO3, AXL, MerTK) and multiple receptor families (including PDGFRs, VEGFRs, and Ephs). sitravatinib 31-38 Myeloproliferative syndrome, transient (transient abnormal myelopoiesis) Homo sapiens 85-88 31369645-3 2019 Here we examined sitravatinib (MGCD516), a spectrum-selective TKI able to block MET, TAM (TYRO3, AXL, MerTK) and multiple receptor families (including PDGFRs, VEGFRs, and Ephs). sitravatinib 31-38 TYRO3 protein tyrosine kinase Homo sapiens 90-95 31369645-3 2019 Here we examined sitravatinib (MGCD516), a spectrum-selective TKI able to block MET, TAM (TYRO3, AXL, MerTK) and multiple receptor families (including PDGFRs, VEGFRs, and Ephs). sitravatinib 31-38 AXL receptor tyrosine kinase Homo sapiens 97-100 31369645-3 2019 Here we examined sitravatinib (MGCD516), a spectrum-selective TKI able to block MET, TAM (TYRO3, AXL, MerTK) and multiple receptor families (including PDGFRs, VEGFRs, and Ephs). sitravatinib 31-38 MER proto-oncogene, tyrosine kinase Homo sapiens 102-107 30385724-3 2018 Sitravatinib is a spectrum-selective tyrosine kinase inhibitor targeting TAM (TYRO3, AXL, MerTK) and split tyrosine-kinase domain-containing receptors (VEGFR and PDGFR families and KIT) plus RET and MET, targets that contribute to the immunosuppressive tumor microenvironment. sitravatinib 0-12 TYRO3 protein tyrosine kinase Homo sapiens 78-83 30385724-3 2018 Sitravatinib is a spectrum-selective tyrosine kinase inhibitor targeting TAM (TYRO3, AXL, MerTK) and split tyrosine-kinase domain-containing receptors (VEGFR and PDGFR families and KIT) plus RET and MET, targets that contribute to the immunosuppressive tumor microenvironment. sitravatinib 0-12 AXL receptor tyrosine kinase Homo sapiens 85-88 30385724-3 2018 Sitravatinib is a spectrum-selective tyrosine kinase inhibitor targeting TAM (TYRO3, AXL, MerTK) and split tyrosine-kinase domain-containing receptors (VEGFR and PDGFR families and KIT) plus RET and MET, targets that contribute to the immunosuppressive tumor microenvironment. sitravatinib 0-12 MER proto-oncogene, tyrosine kinase Homo sapiens 90-95 30385724-3 2018 Sitravatinib is a spectrum-selective tyrosine kinase inhibitor targeting TAM (TYRO3, AXL, MerTK) and split tyrosine-kinase domain-containing receptors (VEGFR and PDGFR families and KIT) plus RET and MET, targets that contribute to the immunosuppressive tumor microenvironment. sitravatinib 0-12 kinase insert domain receptor Homo sapiens 152-157 30385724-3 2018 Sitravatinib is a spectrum-selective tyrosine kinase inhibitor targeting TAM (TYRO3, AXL, MerTK) and split tyrosine-kinase domain-containing receptors (VEGFR and PDGFR families and KIT) plus RET and MET, targets that contribute to the immunosuppressive tumor microenvironment. sitravatinib 0-12 platelet derived growth factor receptor beta Homo sapiens 162-167 30385724-3 2018 Sitravatinib is a spectrum-selective tyrosine kinase inhibitor targeting TAM (TYRO3, AXL, MerTK) and split tyrosine-kinase domain-containing receptors (VEGFR and PDGFR families and KIT) plus RET and MET, targets that contribute to the immunosuppressive tumor microenvironment. sitravatinib 0-12 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 181-184 30385724-3 2018 Sitravatinib is a spectrum-selective tyrosine kinase inhibitor targeting TAM (TYRO3, AXL, MerTK) and split tyrosine-kinase domain-containing receptors (VEGFR and PDGFR families and KIT) plus RET and MET, targets that contribute to the immunosuppressive tumor microenvironment. sitravatinib 0-12 ret proto-oncogene Homo sapiens 191-194