Genomes and Genes
Summary: A tyrosine kinase inhibitor and ANTINEOPLASTIC AGENT that inhibits the BCR-ABL kinase created by chromosome rearrangements in CHRONIC MYELOID LEUKEMIA and ACUTE LYMPHOBLASTIC LEUKEMIA, as well as PDG-derived tyrosine kinases that are overexpressed in gastrointestinal stromal tumors.
- de Lima L, Bueno C, Vivona D, Hirata R, Hirata M, Hungria V, et al. Relationship between SLCO1B3 and ABCA3 polymorphisms and imatinib response in chronic myeloid leukemia patients. Hematology. 2015;20:137-42 pubmed publisherGenetic variations in membrane transporters may contribute to imatinib mesylate (IM) resistance in chronic myeloid leukemia (CML)...
- Kim I, Rhee C, Yeo C, Kang H, Lee D, Lee S, et al. Effect of tyrosine kinase inhibitors, imatinib and nilotinib, in murine lipopolysaccharide-induced acute lung injury during neutropenia recovery. Crit Care. 2013;17:R114 pubmed publisher..Our data indicated that imatinib or nilotinib effectively attenuated LPS-induced ALI during neutropenia recovery. These results provide evidence for the therapeutic potential of imatinib and nilotinib in ALI during neutropenia recovery. ..
- Lu Y, Mao F, Li X, Zheng X, Wang M, Xu Q, et al. Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFR?) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). J Med Chem. 2017;60:5099-5119 pubmed publisher..It was worth noting that 31 inhibited GIST-T1 tumor growth (TGI = 81.5%) and even the BaF3-TEL-cKIT-T670I tumor progression (TGI = 41.9%, 1-resistant GISTs) at a dosage of 100 mg/kg/day without exhibiting apparent toxicity. ..
- Kurokawa Y, Yang H, Cho H, Ryu M, Masuzawa T, Park S, et al. Phase II study of neoadjuvant imatinib in large gastrointestinal stromal tumours of the stomach. Br J Cancer. 2017;117:25-32 pubmed publisher..Neoadjuvant imatinib treatment for 6-9 months is a promising treatment for large gastric GISTs, allowing a high R0 resection rate with acceptable toxicity. ..
- Wu B, Liu M, Li T, Lin H, Zhong H. An economic analysis of high-dose imatinib, dasatinib, and nilotinib for imatinib-resistant chronic phase chronic myeloid leukemia in China: A CHEERS-compliant article. Medicine (Baltimore). 2017;96:e7445 pubmed publisher..The results should be carefully explained due to the assumptions and limitations used in the study. ..
- Rókusz A, Veres D, Szücs A, Bugyik E, Mózes M, Paku S, et al. Ductular reaction correlates with fibrogenesis but does not contribute to liver regeneration in experimental fibrosis models. PLoS ONE. 2017;12:e0176518 pubmed publisher..No evidences support the persistent antifibrotic property of imatinib or erlotinib. ..
- Jiao Y, Li G, Li Q, Ali R, Qin L, Li W, et al. mTOR (Mechanistic Target of Rapamycin) Inhibition Decreases Mechanosignaling, Collagen Accumulation, and Stiffening of the Thoracic Aorta in Elastin-Deficient Mice. Arterioscler Thromb Vasc Biol. 2017;37:1657-1666 pubmed publisher..Our findings suggest that mTOR-sensitive perturbation of smooth muscle cell mechanosensing contributes to elastin aortopathy. ..
- O Connell E, Kamenyeva O, Lustigman S, Bell A, Nutman T. Defining the target and the effect of imatinib on the filarial c-Abl homologue. PLoS Negl Trop Dis. 2017;11:e0005690 pubmed publisher..loa microfilariae before they are treated within the context of conventional mass drug administration. ..
- Liu Q, Zhong G, Zhou W, Lin G. Initial application of transanal endoscopic microsurgery for high-risk lower rectal gastrointestinal stromal tumor after imatinib mesylate neoadjuvant chemotherapy: A case report. Medicine (Baltimore). 2017;96:e7538 pubmed publisher..Neoadjuvant therapy with imatinib mesylate (IM) has achieved great success in GIST, which potentially extends the applications of function-preserving ..
- Maharsy W, Aries A, Mansour O, Komati H, Nemer M. Ageing is a risk factor in imatinib mesylate cardiotoxicity. Eur J Heart Fail. 2014;16:367-76 pubmed..Chemotherapy-induced heart failure is increasingly recognized as a major clinical challenge. Cardiotoxicity of imatinib mesylate, a highly selective and effective anticancer drug belonging to the new class of tyrosine kinase inhibitors, ..
- Sharifnia T, Hong A, Painter C, Boehm J. Emerging Opportunities for Target Discovery in Rare Cancers. Cell Chem Biol. 2017;24:1075-1091 pubmed publisher..Together, these advances motivate consideration of new research frameworks to accelerate rare cancer target discovery. ..
- Joensuu H, Blay J, Comandone A, Martín Broto J, Fumagalli E, Grignani G, et al. Dovitinib in patients with gastrointestinal stromal tumour refractory and/or intolerant to imatinib. Br J Cancer. 2017;117:1278-1285 pubmed publisher..Dovitinib is an active treatment for patients with GIST who are intolerant to imatinib or whose GIST progresses on imatinib. ..
- Fischer J, Dalhoff C, Schrey A, Graebner O, Michaelis S, Andrich K, et al. Dasatinib, imatinib and staurosporine capture compounds - Complementary tools for the profiling of kinases by Capture Compound Mass Spectrometry (CCMS). J Proteomics. 2011;75:160-8 pubmed publisher..Besides sets of expected kinases we identified additional specific interactors; these off-targets may be of relevance in the view of the pharmacological profile of dasatinib and imatinib. ..
- Sotiropoulos G, Stamopoulos P, Kykalos S, Machairas N. Conventional transanal excision for a very low gastrointestinal stromal tumour. BMJ Case Rep. 2017;2017: pubmed publisher..We herein report on a young patient with a >5?cm rectal GIST localised at 1?cm from the anorectal junction. ..
- Egan J. Targeting Stem Cells in Chronic Myeloid Leukemia with a PPAR-? Agonist. N Engl J Med. 2015;373:1973-5 pubmed publisher..Combining a tyrosine kinase inhibitor (imatinib) and a thiazolidinedione (pioglitazone) is proposed for the treatment of chronic myeloid leukemia. ..
- Bixby D, Talpaz M. Mechanisms of resistance to tyrosine kinase inhibitors in chronic myeloid leukemia and recent therapeutic strategies to overcome resistance. Hematology Am Soc Hematol Educ Program. 2009;:461-76 pubmed publisher..This review will describe the efforts at understanding the pathogenesis of imatinib resistance and the molecular rationale for the development of second- and now third-generation therapies for patients with CML. ..
- Papageorgiou S, Pappa V, Economopoulou C, Tsirigotis P, Konsioti F, Ionnidou E, et al. Dasatinib induces long-term remission in imatinib-resistant Philadelphia chromosome-positive acute megakaryoblastic leukemia but fails to prevent development of central nervous system progression. Leuk Res. 2010;34:e254-6 pubmed publisher
- Chen W, Kuang Y, Qiu H, Cao Z, Tu Y, Sheng Q, et al. Dual Targeting of Insulin Receptor and KIT in Imatinib-Resistant Gastrointestinal Stromal Tumors. Cancer Res. 2017;77:5107-5117 pubmed publisher..Our findings suggest that combinatorial inhibition of IR and KIT warrants clinical evaluation as a novel therapeutic strategy in imatinib-resistant GISTs. Cancer Res; 77(18); 5107-17. Â©2017 AACR. ..
- Bellora F, Dondero A, Corrias M, Casu B, Regis S, Caliendo F, et al. Imatinib and Nilotinib Off-Target Effects on Human NK Cells, Monocytes, and M2 Macrophages. J Immunol. 2017;199:1516-1525 pubmed publisher..Our results contribute to better interpreting the off-target efficacy of TKIs in tumors and to envisaging strategies aimed at facilitating antitumor immune responses. ..
- Yap E, Norziha Z, Simbun A, Tumian N, Cheong S, Leong C, et al. MicroRNAs that affect the Fanconi Anemia/BRCA pathway are downregulated in imatinib-resistant chronic myeloid leukemia patients without detectable BCR-ABL kinase domain mutations. Leuk Res. 2017;59:32-40 pubmed publisherChronic myeloid leukemia (CML) patients who do not achieve landmark responses following treatment with imatinib mesylate (IM) are considered IM-resistant...
- Xie Q, Lin Q, Li D, Chen J. Imatinib induces autophagy via upregulating XIAP in GIST882 cells. Biochem Biophys Res Commun. 2017;488:584-589 pubmed publisher..The main effective treatment for GISTs is tyrosine kinase inhibitors, such as imatinib mesylate. However, GISTs respond to imatinib treatment eventually develop acquired resistance, which is a main ..
- Ubink I, Bloemendal H, Elias S, Brink M, Schwartz M, Holierhoek Y, et al. Imatinib treatment of poor prognosis mesenchymal-type primary colon cancer: a proof-of-concept study in the preoperative window period (ImPACCT). BMC Cancer. 2017;17:282 pubmed publisher..ClinicalTrials.gov: NCT02685046 . Registration date: February 9, 2016. ..
- Vasconcelos A, Azevedo I, Melo F, Neves W, Azevedo A, Melo R. BCR-ABL1 transcript types showed distinct laboratory characteristics in patients with chronic myeloid leukemia. Genet Mol Res. 2017;16: pubmed publisher..In agreement with published data, our results showed association of the BCR-ABL1 transcript e14a2 with thrombocytosis and the BCR-ABL1 transcript e13a2 with higher leukocytosis in patients with chronic myeloid leukemia. ..
- Silveira R, Fachel A, Moreira Y, de Souza C, Costa F, Verjovski Almeida S, et al. Protein-coding genes and long noncoding RNAs are differentially expressed in dasatinib-treated chronic myeloid leukemia patients with resistance to imatinib. Hematology. 2014;19:31-41 pubmed publisher..In addition to protein-coding genes, lncRNAs have been recently implicated in pathways leading to tumorigenesis. Our data point to new possible regulatory elements involved in dasatinib resistance in CML. ..
- Zhao Y, Wang J, Luo Y, Shi J, Zheng W, Tan Y, et al. Reduced-intensity allogeneic hematopoietic stem cell transplantation combined with imatinib has comparable event-free survival and overall survival to long-term imatinib treatment in young patients with chronic myeloid leukemia. Ann Hematol. 2017;96:1353-1360 pubmed publisher..However, RIST + IM was more affordable than IM alone in a 10-year scale. Thus, RIST + IM could be considered as an alternative treatment option, especially when the patients have low EBMT risk scores and demand a definite cure for CML. ..
- Reber L, Starkl P, Balbino B, Sibilano R, Gaudenzio N, Rogalla S, et al. The tyrosine kinase inhibitor imatinib mesylate suppresses uric acid crystal-induced acute gouty arthritis in mice. PLoS ONE. 2017;12:e0185704 pubmed publisher..Here we demonstrate that treatment with the tyrosine kinase inhibitor imatinib mesylate (imatinib) can suppress inflammation induced by injection of MSU crystals into subcutaneous air pouches or ..