PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 34079014-7 2021 Ispinesib, a KIF11-inhibitor, effectively inhibited tumor proliferation in all seven cell lines. ispinesib 0-9 kinesin family member 11 Mus musculus 13-18 34944800-8 2021 Interestingly, ispinesib and cabozantinib prevent activation of AXL, a key driver and mechanism of drug resistance in FLT3-ITD+ AML patients. ispinesib 15-24 AXL receptor tyrosine kinase Homo sapiens 64-67 34944800-8 2021 Interestingly, ispinesib and cabozantinib prevent activation of AXL, a key driver and mechanism of drug resistance in FLT3-ITD+ AML patients. ispinesib 15-24 fms related receptor tyrosine kinase 3 Homo sapiens 118-122 32911668-8 2020 Therapeutic targeting of Kif11 to block the Id1-Kif11 axis was carried out using small molecular inhibitor ispinesib. ispinesib 107-116 kinesin family member 11 Homo sapiens 25-30 33652084-0 2021 KIF11 inhibitors filanesib and ispinesib inhibit meningioma growth in vitro and in vivo. ispinesib 31-40 kinesin family member 11 Mus musculus 0-5 33652084-9 2021 We identified substantial in vitro and in vivo anti-tumor effects of the KIF11 inhibitors filanesib and ispinesib, with filanesib demonstrating better tolerability, suggesting future use of filanesib for the treatment of aggressive meningioma. ispinesib 104-113 kinesin family member 11 Mus musculus 73-78 35588495-0 2022 Ispinesib as an Effective Warhead for the Design of Autophagosome-Tethering Chimeras: Discovery of Potent Degraders of Nicotinamide Phosphoribosyltransferase (NAMPT). ispinesib 0-9 nicotinamide phosphoribosyltransferase Homo sapiens 159-164 35588495-4 2022 As a conceptual validation study, the first generation of autophagic degraders of nicotinamide phosphoribosyltransferase (NAMPT) were developed by connecting the NAMPT inhibitor and LC3-binding ispinesib through a flexible linker. ispinesib 194-203 nicotinamide phosphoribosyltransferase Homo sapiens 82-120 35588495-4 2022 As a conceptual validation study, the first generation of autophagic degraders of nicotinamide phosphoribosyltransferase (NAMPT) were developed by connecting the NAMPT inhibitor and LC3-binding ispinesib through a flexible linker. ispinesib 194-203 nicotinamide phosphoribosyltransferase Homo sapiens 122-127 32911668-8 2020 Therapeutic targeting of Kif11 to block the Id1-Kif11 axis was carried out using small molecular inhibitor ispinesib. ispinesib 107-116 inhibitor of DNA binding 1, HLH protein Homo sapiens 44-47 32911668-9 2020 We finally leveraged our findings to target the Id/Kif11 pathway using the small molecule inhibitor ispinesib in the Id+ CSC results combined with chemotherapy for better response in TNBC subtypes. ispinesib 100-109 kinesin family member 11 Homo sapiens 51-56 32300151-4 2020 One such target is the mitotic kinesin KIF11, which can be inhibited with ispinesib, a potent molecularly-targeted drug. ispinesib 74-83 kinesin family member 11 Mus musculus 39-44 32300151-6 2020 Our results demonstrate that the delivery of ispinesib is restricted by P-gp and Bcrp efflux at BBB. ispinesib 45-54 phosphoglycolate phosphatase Mus musculus 72-76 32300151-6 2020 Our results demonstrate that the delivery of ispinesib is restricted by P-gp and Bcrp efflux at BBB. ispinesib 45-54 ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus 81-85 32300151-8 2020 We further find that elacridar-a P-gp and Bcrp inhibitor-improves brain accumulation of ispinesib, resulting in remarkably reduced tumor growth and extended survival in a rodent model of glioblastoma. ispinesib 88-97 phosphoglycolate phosphatase Mus musculus 33-37 32300151-8 2020 We further find that elacridar-a P-gp and Bcrp inhibitor-improves brain accumulation of ispinesib, resulting in remarkably reduced tumor growth and extended survival in a rodent model of glioblastoma. ispinesib 88-97 ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus 42-46 31488701-6 2019 Surprisingly, when the cells were challenged with ispinesib, another Eg5 inhibitor, the Eg5(D130A) cells were resistant, but those expressing Eg5(L214A) were strikingly sensitive. ispinesib 50-59 kinesin family member 11 Homo sapiens 69-72 31488701-6 2019 Surprisingly, when the cells were challenged with ispinesib, another Eg5 inhibitor, the Eg5(D130A) cells were resistant, but those expressing Eg5(L214A) were strikingly sensitive. ispinesib 50-59 kinesin family member 11 Homo sapiens 88-91 31488701-6 2019 Surprisingly, when the cells were challenged with ispinesib, another Eg5 inhibitor, the Eg5(D130A) cells were resistant, but those expressing Eg5(L214A) were strikingly sensitive. ispinesib 50-59 kinesin family member 11 Homo sapiens 88-91 22248262-6 2012 Evaluation of their druglike properties reveals favorable profiles for future development and, in the clinical candidate ispinesib, moderate hERG and CYP inhibition. ispinesib 121-130 ETS transcription factor ERG Homo sapiens 141-145 30410329-7 2018 Results: Results are obtained to depict the dynamics induced by ispinesib, when used as an inhibitor of kinesin Eg5, on cancer cell lines. ispinesib 64-73 kinesin family member 11 Homo sapiens 112-115 23658017-0 2013 "Snapshots" of ispinesib-induced conformational changes in the mitotic kinesin Eg5. ispinesib 15-24 kinesin family member 11 Homo sapiens 79-82 23658017-4 2013 This loop is longest in the mitotic kinesin Eg5 and is the target for a number of small molecule inhibitors, including ispinesib, which is being used in clinical trials in patients with cancer. ispinesib 119-128 kinesin family member 11 Homo sapiens 44-47 23658017-5 2013 In this study, we have used x-ray crystallography to identify a new structure of an Eg5-ispinesib complex and have combined this with transient state kinetics to identify a plausible sequence of conformational changes that occur in response to ispinesib binding. ispinesib 88-97 kinesin family member 11 Homo sapiens 84-87 23658017-6 2013 Our results demonstrate that ispinesib-induced structural changes in L5 from Eg5 lead to subsequent changes in the conformation of the switch II loop and helix and in the neck linker. ispinesib 29-38 kinesin family member 11 Homo sapiens 77-80 23875972-2 2013 The aim of this study was to investigate the underlying molecular mechanism of resistance developed by the mitotic kinesin Eg5 against the potent second-generation ispinesib analogue SB743921 (1), a phase I/II clinical candidate. ispinesib 164-173 kinesin family member 11 Homo sapiens 123-126 23444224-6 2013 Phenotypes that were observed following siRNA-mediated knockdown of KIF11 (kinesin family member 11) were reproduced by inhibition of KIF11 using the small-molecule inhibitor ispinesib (SB-715992). ispinesib 175-184 kinesin family member 11 Mus musculus 68-73 23444224-6 2013 Phenotypes that were observed following siRNA-mediated knockdown of KIF11 (kinesin family member 11) were reproduced by inhibition of KIF11 using the small-molecule inhibitor ispinesib (SB-715992). ispinesib 175-184 kinesin family member 11 Mus musculus 75-99 23444224-6 2013 Phenotypes that were observed following siRNA-mediated knockdown of KIF11 (kinesin family member 11) were reproduced by inhibition of KIF11 using the small-molecule inhibitor ispinesib (SB-715992). ispinesib 175-184 kinesin family member 11 Mus musculus 134-139 23444224-6 2013 Phenotypes that were observed following siRNA-mediated knockdown of KIF11 (kinesin family member 11) were reproduced by inhibition of KIF11 using the small-molecule inhibitor ispinesib (SB-715992). ispinesib 186-195 kinesin family member 11 Mus musculus 68-73 23444224-6 2013 Phenotypes that were observed following siRNA-mediated knockdown of KIF11 (kinesin family member 11) were reproduced by inhibition of KIF11 using the small-molecule inhibitor ispinesib (SB-715992). ispinesib 186-195 kinesin family member 11 Mus musculus 75-99 23444224-6 2013 Phenotypes that were observed following siRNA-mediated knockdown of KIF11 (kinesin family member 11) were reproduced by inhibition of KIF11 using the small-molecule inhibitor ispinesib (SB-715992). ispinesib 186-195 kinesin family member 11 Mus musculus 134-139 22993085-5 2012 In this study, the crystal structure of the Eg5 motor domain in complex with ispinesib, supported by kinetic and thermodynamic binding data, is reported. ispinesib 77-86 kinesin family member 11 Homo sapiens 44-47 22993085-6 2012 Ispinesib occupies the same induced-fit pocket in Eg5 as other allosteric inhibitors, making extensive hydrophobic interactions with the protein. ispinesib 0-9 kinesin family member 11 Homo sapiens 50-53 22248262-6 2012 Evaluation of their druglike properties reveals favorable profiles for future development and, in the clinical candidate ispinesib, moderate hERG and CYP inhibition. ispinesib 121-130 peptidylprolyl isomerase G Homo sapiens 150-153 19545421-6 2009 Due to the brain location of the tumor, the potential target inhibition for anticancer therapy must exhibit a manageable neurotoxicity profile in the concentration range in which the compounds show anti-proliferative activity.Kinesin KIF11 inhibition by small molecules such as Monastrol or Ispinesib is currently under investigation in the field of malignant tumors. ispinesib 291-300 kinesin family member 11 Homo sapiens 234-239 19545421-8 2009 RESULTS: In this study the target was validated using a set of well characterised and potentially specific small molecule inhibitors of KIF11: an ispinesib analog, Monastrol, a Merck compound and 3 simplified derivatives of the Merck compound. ispinesib 146-155 kinesin family member 11 Homo sapiens 136-141 19545421-12 2009 Furthermore, ispinesib analog increased caspase 3/7-induced apoptosis in U87MG cells. ispinesib 13-22 caspase 3 Homo sapiens 40-49