PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 34167562-8 2021 We also observed strong synergy between MRK-560 and KPT-8602 (eltanexor) in all NOTCH1-dependent T-ALL cell lines. Eltanexor 62-71 mitogen-activated protein kinase kinase kinase 20 Homo sapiens 40-43 34165175-5 2021 The aim of the present study was to evaluate the combination of CAR T cells with the SINE compounds eltanexor and selinexor. Eltanexor 100-109 nuclear receptor subfamily 1 group I member 3 Homo sapiens 64-67 34165175-6 2021 As expected, eltanexor and selinexor were toxic to CD19-positive malignant cells and the sensitivity of cells towards SINEs correlated with the levels of XPO1-expression in ALL cell lines. Eltanexor 13-22 CD19 molecule Homo sapiens 51-55 34165175-6 2021 As expected, eltanexor and selinexor were toxic to CD19-positive malignant cells and the sensitivity of cells towards SINEs correlated with the levels of XPO1-expression in ALL cell lines. Eltanexor 13-22 exportin 1 Homo sapiens 154-158 34165175-9 2021 Due to CAR T-cell toxicity, sequential use of SINEs and CAR T cells was evaluated: Cytotoxicity of CAR T cells increased significantly when target cells were pre-treated with the SINE compound eltanexor. Eltanexor 193-202 nuclear receptor subfamily 1 group I member 3 Homo sapiens 56-59 34165175-10 2021 In addition, exhaustion of CAR T cells decreased when target cells were pre-treated with eltanexor. Eltanexor 89-98 nuclear receptor subfamily 1 group I member 3 Homo sapiens 27-30 34167562-4 2021 In this study, we developed combination treatment strategies with the PSEN1-selective gamma-secretase inhibitor MRK-560 and other targeted agents (kinase inhibitors ruxolitinib and imatinib; XPO-1 inhibitor KPT-8602/eltanexor) for the treatment of T-ALL. Eltanexor 207-215 exportin 1 Homo sapiens 191-196 34167562-8 2021 We also observed strong synergy between MRK-560 and KPT-8602 (eltanexor) in all NOTCH1-dependent T-ALL cell lines. Eltanexor 62-71 notch receptor 1 Homo sapiens 80-86 35489384-5 2022 In vitro treatment of TCL cell lines with KPT-8602, the second-generation selective inhibitor of nuclear export (SINE), inhibited XPO1 expression and showed significant anti-proliferative, cell-cycle arrest and pro-apoptotic efficacy. Eltanexor 42-50 exportin 1 Homo sapiens 130-134 34206543-3 2021 We also showed that a selective inhibitor of nuclear export (SINE) selinexor and second generation eltanexor (KPT-8602) could suppress mCRPC growth, reduce androgen receptor (AR), and re-sensitize to androgen deprivation therapy. Eltanexor 99-108 androgen receptor Homo sapiens 156-173 34206543-3 2021 We also showed that a selective inhibitor of nuclear export (SINE) selinexor and second generation eltanexor (KPT-8602) could suppress mCRPC growth, reduce androgen receptor (AR), and re-sensitize to androgen deprivation therapy. Eltanexor 99-108 androgen receptor Homo sapiens 175-177 34206543-3 2021 We also showed that a selective inhibitor of nuclear export (SINE) selinexor and second generation eltanexor (KPT-8602) could suppress mCRPC growth, reduce androgen receptor (AR), and re-sensitize to androgen deprivation therapy. Eltanexor 110-118 androgen receptor Homo sapiens 156-173 34206543-3 2021 We also showed that a selective inhibitor of nuclear export (SINE) selinexor and second generation eltanexor (KPT-8602) could suppress mCRPC growth, reduce androgen receptor (AR), and re-sensitize to androgen deprivation therapy. Eltanexor 110-118 androgen receptor Homo sapiens 175-177 35489384-6 2022 In mechanism, KPT-8602 restored the localization of cytoplasmic FOXO3A, p27, p21, IkappaBalpha and PP2A into the nucleus, leading to AKT and NF-kappaB deactivation. Eltanexor 14-22 forkhead box O3 Homo sapiens 64-70 35489384-6 2022 In mechanism, KPT-8602 restored the localization of cytoplasmic FOXO3A, p27, p21, IkappaBalpha and PP2A into the nucleus, leading to AKT and NF-kappaB deactivation. Eltanexor 14-22 dynactin subunit 6 Homo sapiens 72-75 35489384-6 2022 In mechanism, KPT-8602 restored the localization of cytoplasmic FOXO3A, p27, p21, IkappaBalpha and PP2A into the nucleus, leading to AKT and NF-kappaB deactivation. Eltanexor 14-22 H3 histone pseudogene 16 Homo sapiens 77-80 35489384-6 2022 In mechanism, KPT-8602 restored the localization of cytoplasmic FOXO3A, p27, p21, IkappaBalpha and PP2A into the nucleus, leading to AKT and NF-kappaB deactivation. Eltanexor 14-22 NFKB inhibitor alpha Homo sapiens 82-94 35489384-6 2022 In mechanism, KPT-8602 restored the localization of cytoplasmic FOXO3A, p27, p21, IkappaBalpha and PP2A into the nucleus, leading to AKT and NF-kappaB deactivation. Eltanexor 14-22 protein phosphatase 2 phosphatase activator Homo sapiens 99-103 35489384-6 2022 In mechanism, KPT-8602 restored the localization of cytoplasmic FOXO3A, p27, p21, IkappaBalpha and PP2A into the nucleus, leading to AKT and NF-kappaB deactivation. Eltanexor 14-22 AKT serine/threonine kinase 1 Homo sapiens 133-136 35489384-6 2022 In mechanism, KPT-8602 restored the localization of cytoplasmic FOXO3A, p27, p21, IkappaBalpha and PP2A into the nucleus, leading to AKT and NF-kappaB deactivation. Eltanexor 14-22 nuclear factor kappa B subunit 1 Homo sapiens 141-150 35367710-3 2022 Using the second-generation XPO1 inhibitor KPT-8602 as the lead compound, structure-based optimization provided D4 with high anti-proliferation efficacy (IC50 = 24 nM in MM.1S). Eltanexor 43-51 exportin 1 Rattus norvegicus 28-32 32826328-0 2020 The XPO1 inhibitor KPT-8602 synergizes with dexamethasone in acute lymphoblastic leukemia. Eltanexor 19-27 exportin 1 Homo sapiens 4-8 33887086-4 2021 Herein, we report clickable probes based on the XPO1 inhibitors selinexor and eltanexor for the labeling of XPO1 in live cells to assess target engagement and selectivity. Eltanexor 78-87 exportin 1 Homo sapiens 108-112 33745946-6 2021 Administration of KPT-8602, an XPO1 inhibitor, followed by AZD-6738, an ATR inhibitor, resulted in dramatic antitumor effects and prolonged survival in TP53-mutant models of CRC. Eltanexor 18-26 exportin 1 Homo sapiens 31-35 33745946-6 2021 Administration of KPT-8602, an XPO1 inhibitor, followed by AZD-6738, an ATR inhibitor, resulted in dramatic antitumor effects and prolonged survival in TP53-mutant models of CRC. Eltanexor 18-26 tumor protein p53 Homo sapiens 152-156 34012430-0 2021 The Second-Generation XPO1 Inhibitor Eltanexor Inhibits Human Cytomegalovirus (HCMV) Replication and Promotes Type I Interferon Response. Eltanexor 37-46 exportin 1 Homo sapiens 22-26 32826328-1 2020 PURPOSE: KPT-8602 (Eltanexor) is a second generation exportin-1 (XPO1) inhibitor with potent activity against acute lymphoblastic leukemia (ALL) in pre-clinical models and with minimal effects on normal cells. Eltanexor 9-17 exportin 1 Homo sapiens 53-63 32826328-1 2020 PURPOSE: KPT-8602 (Eltanexor) is a second generation exportin-1 (XPO1) inhibitor with potent activity against acute lymphoblastic leukemia (ALL) in pre-clinical models and with minimal effects on normal cells. Eltanexor 9-17 exportin 1 Homo sapiens 65-69 32826328-1 2020 PURPOSE: KPT-8602 (Eltanexor) is a second generation exportin-1 (XPO1) inhibitor with potent activity against acute lymphoblastic leukemia (ALL) in pre-clinical models and with minimal effects on normal cells. Eltanexor 19-28 exportin 1 Homo sapiens 53-63 32826328-1 2020 PURPOSE: KPT-8602 (Eltanexor) is a second generation exportin-1 (XPO1) inhibitor with potent activity against acute lymphoblastic leukemia (ALL) in pre-clinical models and with minimal effects on normal cells. Eltanexor 19-28 exportin 1 Homo sapiens 65-69 32826328-9 2020 CONCLUSION: Our pre-clinical study demonstrates that KPT-8602 enhances the effects of dexamethasone to inhibit B-ALL and T-ALL cells via NR3C1 and E2F mediated transcriptional complexes, allowing to achieve increased dexamethasone effects for patients. Eltanexor 53-61 nuclear receptor subfamily 3 group C member 1 Homo sapiens 137-142 27211268-0 2017 KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Eltanexor 0-8 exportin 1 Homo sapiens 43-47 30563936-7 2019 RESULTS: JAK2V617F-mutant HEL, SET-2, and HEL cells resistant to JAK inhibition are exquisitely sensitive to RAN knockdown or pharmacologic inhibition by KPT-330 or KPT-8602. Eltanexor 165-173 Janus kinase 2 Homo sapiens 9-13 30563936-7 2019 RESULTS: JAK2V617F-mutant HEL, SET-2, and HEL cells resistant to JAK inhibition are exquisitely sensitive to RAN knockdown or pharmacologic inhibition by KPT-330 or KPT-8602. Eltanexor 165-173 RAN, member RAS oncogene family Homo sapiens 109-112 29299164-7 2017 Studies comparing cytotoxicity and XPO1 occupancy in cell lines treated with selinexor or KPT-8602 indicated that XPO1 occupancy by both compounds could reach saturation regardless of drug sensitivity. Eltanexor 90-98 exportin 1 Homo sapiens 35-39 29299164-7 2017 Studies comparing cytotoxicity and XPO1 occupancy in cell lines treated with selinexor or KPT-8602 indicated that XPO1 occupancy by both compounds could reach saturation regardless of drug sensitivity. Eltanexor 90-98 exportin 1 Homo sapiens 114-118 27780859-0 2017 The Second-Generation Exportin-1 Inhibitor KPT-8602 Demonstrates Potent Activity against Acute Lymphoblastic Leukemia. Eltanexor 43-51 exportin 1 Homo sapiens 22-32 27211268-5 2017 Here we report the anti-leukemic efficacy and tolerability of KPT-8602, a second-generation XPO1 inhibitor. Eltanexor 62-70 exportin 1 Homo sapiens 92-96