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1d
Activation of stimulator of interferon genes (STING) and inhibition of vascular endothelial growth factor receptor (VEGFR) by telatinib induce antitumor activity. (PubMed, J Biol Chem)
Moreover, we showed that telatinib-mediated STING activation contributed to the antitumor effects in tumor-bearing mouse models. In summary, our results reveal that telatinib, a previously identified VEGFR2 inhibitor, activates STING signaling, highlighting its potential in cancer immunotherapy.
Journal
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STING (stimulator of interferon response cGAMP interactor 1)
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telatinib (BAY 57- 9352)
1d
Loeffler Syndrome in FIP1L1-PDGFRA-Positive Myeloid Neoplasm. (PubMed, JACC Case Rep)
Cardiac involvement in hypereosinophilic syndromes requires multidisciplinary management combining cytoreductive therapy, anticoagulation when thrombus is present, and serial cardiac magnetic resonance. Testing for FIP1L1-platelet-derived growth factor receptor α is disease-defining and therapy-guiding given the marked response to imatinib.
Journal
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PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • FIP1L1 (Factor Interacting With PAPOLA And CPSF1)
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imatinib
1d
Primary extra-gastrointestinal stromal tumor of the gallbladder: A case report. (PubMed, World J Gastroenterol)
Primary gallbladder EGISTs are exceedingly rare, with insidious onset and nonspecific clinical manifestations. Histopathological examination combined with immunohistochemistry remains the cornerstone of definitive diagnosis.
Journal
|
KIT (KIT proto-oncogene, receptor tyrosine kinase) • CD34 (CD34 molecule) • ANO1 (Anoctamin 1)
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imatinib
1d
Coexistence of Philadelphia Chromosome in Acute Promyelocytic Leukaemia: Two Rare Cases, with A Literature Review. (PubMed, Eur J Case Rep Intern Med)
The rare genetic co-occurrence of t(15;17)/PML::RARA and t(9;22)/BCR::ABL1 translocations may be identified in a single patient with acute promyelocytic leukaemia (APL).Successful induction using all-trans retinoic acid (ATRA) together with imatinib achieved effective control of both leukemic clones.The patient demonstrated rapid haematologic remission and favourable clinical recovery, suggesting a positive outcome with this therapeutic approach.
Journal
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ABL1 (ABL proto-oncogene 1)
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Chr t(15;17)
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imatinib • idarubicin hydrochloride
2d
Dasatinib Produces Lengthy Remissions of Extramedullary Leukemia: A Retrospective Observational Study. (PubMed, Eur J Haematol)
Since 2004, patients receiving imatinib with relapse in non-marrow sites were given dasatinib to preserve control of leukemic marrow. Dasatinib is a potentially practice-changing targeted therapy for EML. Finding and eradicating EML could increase the possibility of lengthy disease-free survival.
Observational data • Retrospective data • Journal
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ABL1 (ABL proto-oncogene 1)
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dasatinib • imatinib
3d
Heterocyclic Compounds as Bcr-Abl Tyrosine Kinase Inhibitors Against Chronic Myeloid Leukemia. (PubMed, Med Chem)
However, the toxicity and resistance associated with the use of imatinib, a first-generation Bcr-Abl inhibitor, in cases where the T315I mutation exists, necessitates the need for new tyrosine kinase inhibitors...However, investigating different combined scaffolds enhances the chance of successfully developing novel drug candidates. Overall, the information provided in this review can be beneficial to researchers with an interest in chronic myeloid leukemia and tyrosine kinase inhibitors.
Review • Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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imatinib
3d
Disparities in management guidelines for gastrointestinal stromal tumors: A comparison of recommendations from the Chinese Society of Clinical Oncology, National Comprehensive Cancer Network, and European Society for Medical Oncology. (PubMed, Cancer)
The advent of targeted therapy, notably the first tyrosine kinase inhibitor (TKI) imatinib, has revolutionized the treatment landscape for GISTs...This commentary highlights discrepancies in the recommendations for managing GISTs as outlined in these major guidelines. Based on emerging new evidence from recent studies, the authors propose recommendations to be considered for inclusion in future guideline updates to optimize management strategies and ultimately improve the outcomes of patients with GISTs.
Clinical • Journal
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KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
|
KIT mutation
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imatinib
4d
Germ cell immunoprofile and KIT exon 17 mutation guide rectification of seminoma misclassified as epithelioid gastrointestinal stromal tumor: A case report. (PubMed, Biomed Rep)
Definitive diagnosis of seminoma was established through expanded immunohistochemistry (OCT4+/SALL4+/PLAP+/D2-40+) and molecular confirmation of the characteristic KIT p.D816Y mutation, which concurrently explains the observed imatinib resistance. In conclusion, the findings of the present study highlighted the imperative of integrating morphology, immunohistochemistry and context-specific molecular profiling to avoid diagnostic in CD117-positive tumors.
Journal
|
KIT (KIT proto-oncogene, receptor tyrosine kinase) • ALPP (Alkaline Phosphatase, Placental) • POU5F1 (POU Class 5 Homeobox 1) • SALL4 (Spalt Like Transcription Factor 4)
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KIT mutation
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imatinib
4d
Beyond COL1A1::PDGFB: Rare fusions and their clinical implications in dermatofibrosarcoma protuberans. (PubMed, World J Clin Cases)
This fusion drives tumorigenesis and forms the basis for imatinib treatment, which acts by blocking platelet-derived growth factor receptor-beta kinase activity...In this editorial commentary, we briefly highlight the ever-growing genomic landscape of DFSP, report rare fusions and their biological implications, and examine the role of expanded molecular diagnostics in refining diagnosis, guiding therapy, and informing prognosis. Incorporating comprehensive fusion analysis into routine workup may be critical for accurate classification, especially in unusual presentations where reliance on morphology alone risks misdiagnosis.
Journal
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PDGFRB (Platelet Derived Growth Factor Receptor Beta) • COL1A1 (Collagen Type I Alpha 1 Chain) • PDGFB (Platelet Derived Growth Factor Subunit B) • COL6A3 (Collagen Type VI Alpha 3 Chain)
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imatinib
4d
The structural requirements of 3,5-substituted oxindoles that determine selective AMPK or GSK3β inhibition. (PubMed, RSC Med Chem)
We have previously reported a structure-activity study of substituted oxindoles based on the multi-kinase inhibitor sunitinib to determine the structural requirements for AMPK inhibition and found that a 5-(2-cyanoethyl)-substituted oxindole displayed selectivity for AMPK over VEGFR-2...Here, we report a further series of 3,5-substituted oxindoles that demonstrate that 5-cyano-oxindoles can inhibit both GSK3β and AMPK, but the 5-(2-cyanoethyl)-substitution and the orientation of the 3-substituent of the oxindole are critical determinants for AMPK inhibition and selectivity. These findings could have critical importance in evaluating metabolic targeting in cancer as GSK3β promotes anabolic pathways and suppresses AMPK activity.
Journal
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KDR (Kinase insert domain receptor) • ACACB (Acetyl-CoA Carboxylase Beta) • AMPK (Protein Kinase AMP-Activated Catalytic Subunit Alpha 1)
|
sunitinib
5d
Comprehensive Molecular Screening by Next Generation Sequencing of Gastrointestinal Stromal Tumors (GISTs): In Silico Analysis and Classification of Rare KIT Exon 11 Mutations. (PubMed, Cancer Med)
Our findings highlight the clinical relevance of integrating NGS into routine GIST management, particularly for the identification and interpretation of rare genetic variants. The study underscores the importance of data sharing and collective variant annotation to support accurate molecular classification, prognostic assessment, and therapeutic decision-making for individual patients.
Retrospective data • Journal • Next-generation sequencing
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BRAF (B-raf proto-oncogene) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B)
|
BRAF mutation • KIT mutation • PDGFRA mutation
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imatinib
6d
Targeting Musashi-2 to counteract senescence and resistance in chronic myeloid leukemia: enhancing the efficacy of imatinib therapy. (PubMed, BMC Cancer)
In conclusion, MSI2 inhibition, in combination with TKI therapy, has shown to overcome drug resistance and mitigate senescence in preclinical CML models, and suggesting a potential strategy to target CML LSCs.
Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • IL6 (Interleukin 6) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • MSI2 (Musashi RNA Binding Protein 2)
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imatinib