PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 32657579-4 2020 Herein, we systematically designed a set of unique PROTACs by globally targeting all the three binding sites of BCR-ABL, including dasatinib-, ponatinib-, and asciminib-based PROTACs. asciminib 159-168 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 112-119 33096322-0 2020 The specificity of asciminib, a potential treatment for chronic myeloid leukemia, as a myristate-pocket binding ABL inhibitor and analysis of its interactions with mutant forms of BCR-ABL1 kinase. asciminib 19-28 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 112-115 33096322-0 2020 The specificity of asciminib, a potential treatment for chronic myeloid leukemia, as a myristate-pocket binding ABL inhibitor and analysis of its interactions with mutant forms of BCR-ABL1 kinase. asciminib 19-28 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 184-188 33096322-1 2020 Asciminib is a potent, orally bioavailable, investigational drug that specifically and potently inhibits the tyrosine kinase activity of native ABL1, together with that of the chimeric BCR-ABL1 oncoprotein which causes chronic myeloid leukemia (CML). asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 144-148 33096322-2 2020 In contrast to ATP-competitive BCR-ABL1 kinase inhibitors employed to treat CML that target multiple kinases, asciminib binds to the myristate binding pocket on the kinase domains of ABL1 and BCR-ABL1. asciminib 110-119 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 183-187 33096322-2 2020 In contrast to ATP-competitive BCR-ABL1 kinase inhibitors employed to treat CML that target multiple kinases, asciminib binds to the myristate binding pocket on the kinase domains of ABL1 and BCR-ABL1. asciminib 110-119 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 183-187 33096322-6 2020 However, in vitro studies in cells have identified BCR-ABL1 mutations that reduce the anti-proliferative activity of asciminib, some of which are associated with clinical resistance towards the drug in patients. asciminib 117-126 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 55-59 33096322-7 2020 Here we review effects of asciminib on mutant forms of BCR-ABL1, analyse their sensitivity towards the drug from a structural perspective and affirm support for employing combinations with ATP-competitive inhibitors to impede the reactivation of BCR-ABL1 kinase activity in patients receiving monotherapy. asciminib 26-35 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 59-63 30927708-0 2019 Molecular dynamics investigation on the Asciminib resistance mechanism of I502L and V468F mutations in BCR-ABL. asciminib 40-49 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 103-110 32380976-3 2020 Two of these are (I) Axitinib, which inhibits the T315I mutation of BCR-ABL1, a main source of drug resistance, and (II) Asciminib, which has been developed as an allosteric BCR-ABL1 inhibitor, targeting an entirely different binding site, and as such does not compete for binding with other drugs. asciminib 121-130 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 178-182 31448223-5 2019 This includes the use asciminib as first in class inhibitor targeting the myristoyl pocket of BCR-ABL, combination treatments with established non-TKI drugs such as interferon and drugs with novel targets relevant to CML biology such as gliptins and thiazolidinediones. asciminib 22-31 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 94-101 30927708-1 2019 Asciminib, a highly selective non-ATP competitive inhibitor of BCR-ABL, has demonstrated to be a promising drug for patients with chronic myeloid leukemia. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 63-70 30927708-4 2019 The obtained results indicate that the mutations have adversely influence on the binding of Asciminib to BCR-ABL, as the nonpolar contributions decline in the two mutants. asciminib 92-101 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 105-112 30927708-7 2019 Our results provide the molecular insights of Asciminib resistance mechanism in BCR-ABL mutants, which may help the design of novel inhibitors. asciminib 46-55 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 80-87 29522367-8 2018 Asciminib, an allosteric ABL1 inhibitor, could demonstrate a higher capacity in overcoming common TKIs resistant mutations, including T315I, but clinical findings are needed. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 25-29 31250767-4 2019 OBJECTIVE: In recent studies, the dual inhibition of BCR-ABL by Nilotinib and Asciminib has been shown to overcome drug resistance. asciminib 78-87 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 53-60 30137981-4 2018 We describe the discovery of asciminib (ABL001), the first allosteric BCR-ABL1 inhibitor to reach the clinic. asciminib 29-38 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 74-78 30137981-4 2018 We describe the discovery of asciminib (ABL001), the first allosteric BCR-ABL1 inhibitor to reach the clinic. asciminib 40-46 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 74-78 30137981-5 2018 Asciminib binds to the myristate pocket of BCR-ABL1 and maintains activity against TKI-resistant ATP-site mutations. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 47-51 29325229-3 2018 Moreover, allosteric targeting has been identified to consequentially inhibit Bcr-Abl activity, which led to the recent development of ABL-001 (asciminib) that selectively binds the myristoyl pocket. asciminib 144-153 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 78-85 28329763-5 2017 Here we characterize ABL001 (asciminib), a potent and selective allosteric ABL1 inhibitor that is undergoing clinical development testing in patients with CML and Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukaemia. asciminib 21-27 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 75-79 28329763-5 2017 Here we characterize ABL001 (asciminib), a potent and selective allosteric ABL1 inhibitor that is undergoing clinical development testing in patients with CML and Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukaemia. asciminib 29-38 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 75-79 33971041-0 2021 Overcoming TKI resistance in a patient with chronic myeloid leukemia using combination BCR-ABL inhibition with asciminib and bosutinib. asciminib 111-120 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 87-94 34659899-0 2021 Asciminib and ponatinib exert synergistic anti-neoplastic effects on CML cells expressing BCR-ABL1 T315I-compound mutations. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 94-98 34115385-1 2021 Asciminib is an investigational, first-in-class, Specifically Targeting the ABL Myristoyl Pocket (STAMP), inhibitor of BCR-ABL1 with a new mechanism of action compared with approved ATP-competitive tyrosine kinase inhibitors. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 123-127 34659899-3 2021 Asciminib is a novel drug capable of targeting most BCR-ABL1 mutant-forms, including BCR-ABL1T315I, but remains ineffective against most BCR-ABL1T315I+ compound mutation-bearing sub-clones. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 56-60 34659899-8 2021 Most importantly, we were able to show that the combinations "asciminib+ponatinib" and "asciminib+ponatinib+HU" produce synergistic apoptosis-inducing effects in CD34+/CD38- CML stem cells obtained from patients with chronic phase CML or BCR-ABL1 T315I+ CML blast phase. asciminib 62-71 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 242-246 34659899-8 2021 Most importantly, we were able to show that the combinations "asciminib+ponatinib" and "asciminib+ponatinib+HU" produce synergistic apoptosis-inducing effects in CD34+/CD38- CML stem cells obtained from patients with chronic phase CML or BCR-ABL1 T315I+ CML blast phase. asciminib 88-97 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 242-246 34659899-9 2021 Together, asciminib, ponatinib and HU synergize in producing anti-leukemic effects in multi-resistant CML cells, including cells harboring T315I+ BCR-ABL1 compound mutations and CML stem cells. asciminib 10-19 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 150-154 35468180-1 2022 Asciminib, a first-in-class allosteric inhibitor of BCR::ABL1 kinase activity, is now approved for the treatment of chronic phase CML patients who failed 2 lines of therapy or in patients with the T315I mutation. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 57-61 35583386-4 2022 Asciminib, a first-in-class BCR::ABL1 inhibitor Specifically Targeting the ABL Myristoyl Pocket (STAMP), has the potential to overcome resistance/intolerance to prior TKI treatment. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 33-37 35616006-1 2022 Asciminib is a first-in-class inhibitor of BCR::ABL1, specifically targeting the ABL myristoyl pocket. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 48-52 35616006-1 2022 Asciminib is a first-in-class inhibitor of BCR::ABL1, specifically targeting the ABL myristoyl pocket. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 81-84 35129779-2 2022 Asciminib has been recently (2021) approved for patients resistant to former TKIs, and because the binding site of this drug (the myristoyl pocket in the ABL1 kinase) is different from that of other TKIs (ATP-binding sites), it is, therefore, effective against T315I mutation of BCR-ABL oncoprotein. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 154-158 35129779-2 2022 Asciminib has been recently (2021) approved for patients resistant to former TKIs, and because the binding site of this drug (the myristoyl pocket in the ABL1 kinase) is different from that of other TKIs (ATP-binding sites), it is, therefore, effective against T315I mutation of BCR-ABL oncoprotein. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 279-286 35021069-0 2022 Development of Asciminib, a Novel Allosteric Inhibitor of BCR-ABL1. asciminib 15-24 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 62-66 35021069-4 2022 Asciminib is a promising investigational agent in development that allosterically targets BCR-ABL1 in a non-ATP-competitive manner. asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 94-98 35041175-1 2022 Asciminib (Scemblix ) is an orally administered, small molecule, selective allosteric inhibitor that targets the myristoyl pocket of the BCR-ABL1 tyrosine kinase and is being developed by Novartis for the treatment of haematological malignancies, including Philadelphia chromosome-positive (Ph+) chronic myeloid leukaemia (CML). asciminib 0-9 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 141-145 35041175-1 2022 Asciminib (Scemblix ) is an orally administered, small molecule, selective allosteric inhibitor that targets the myristoyl pocket of the BCR-ABL1 tyrosine kinase and is being developed by Novartis for the treatment of haematological malignancies, including Philadelphia chromosome-positive (Ph+) chronic myeloid leukaemia (CML). asciminib 11-19 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 141-145