Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113215
Abstract: Feline McDonough sarcoma (FMS)-like tyrosine kinase 3 (FLT3) is one of the most pursued targets in the treatment of acute myeloid leukaemia (AML) as its gene amplification and mutations, particularly internal tandem duplication (ITD), contribute… read more here.
Keywords: flt3; myeloid leukaemia; azaaryl phenylpyrimidin; acute myeloid ... See more keywords
The role of FLT3 inhibitors as maintenance therapy following hematopoietic stem cell transplant
Sign Up to like & getrecommendations! Published in 2018 at "Leukemia Research Reports"
DOI: 10.1016/j.lrr.2018.06.003
Abstract: Activating mutations in FLT3 in acute myeloid leukemia (AML) portend a poor prognosis, and targeting FLT3 with a tyrosine kinase inhibitor has been an area of intense research recently. Most FLT3 mutated AML patients undergo… read more here.
Keywords: role; stem cell; flt3 inhibitors; hematopoietic stem ... See more keywords
Emerging FLT3 inhibitors for the treatment of acute myeloid leukemia.
Sign Up to like & getrecommendations! Published in 2022 at "Expert opinion on emerging drugs"
DOI: 10.1080/14728214.2021.2009800
Abstract: INTRODUCTION The FMS-like tyrosine kinase 3 (FLT3) gene is mutated in one-third of patients with Acute Myeloid Leukemia (AML). Midostaurin, quizartinib, and gilteritinib have been approved in the last years for the treatment of AML,… read more here.
Keywords: acute myeloid; flt3; myeloid leukemia; treatment ... See more keywords
Drug-drug interactions associated with FLT3 inhibitors for acute myeloblastic leukemia: current landscape
Sign Up to like & getrecommendations! Published in 2023 at "Expert Review of Clinical Pharmacology"
DOI: 10.1080/17512433.2023.2174523
Abstract: ABSTRACT Introduction FLT3 inhibitors (FLT3i) are drugs in which there is limited experience and not yet enough information on the mechanisms of absorption, transport, and elimination; but especially on the potential drug-drug interactions (DDIs). There… read more here.
Keywords: flt3 inhibitors; drug interactions; drug drug; leukemia ... See more keywords
The combination of FLT3 and SYK kinase inhibitors is toxic to leukaemia cells with CBL mutations
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Cellular and Molecular Medicine"
DOI: 10.1111/jcmm.14820
Abstract: Mutations in the E3 ubiquitin ligase CBL, found in several myeloid neoplasms, lead to decreased ubiquitin ligase activity. In murine systems, these mutations are associated with cytokine‐independent proliferation, thought to result from the activation of… read more here.
Keywords: mutant cbl; leukaemia cells; kinase; inhibition ... See more keywords
Abstract 1885: Selective Polo-like Kinase 1 (PLK1) inhibitor PCM-075 is highly active alone and shows synergy when combined with FLT3 inhibitors in models of acute myeloid leukemia (AML)
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-1885
Abstract: First generation FLT3 inhibitors have been useful in treating AML (sorafenib, midostaurin). Second generation inhibitors with more selectivity are currently in P3 trials in AML (quizartinib, gilteritinib). Despite the advances, resistance to FLT3 inhibitors and… read more here.
Keywords: plk1; inhibitor; pcm 075; aml ... See more keywords
Patterns of Resistance Differ in Patients with Acute Myeloid Leukemia Treated with Type I versus Type II FLT3 Inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Cancer discovery"
DOI: 10.1158/2643-3230.bcd-20-0143
Abstract: Despite promising results with FLT3 inhibitors (FLT3i), response durations remain short. We studied pretreatment and relapse bone marrow samples from patients with FLT3-mutated acute myeloid leukemia (AML) treated with FLT3i-based therapies (secondary resistance cohort), and… read more here.
Keywords: flt3 inhibitors; flt3i based; resistance; treated type ... See more keywords
Hematologists Demonstrate Sub-Optimal Knowledge of FLT3 Mutations in Acute Myeloid Leukemia
Sign Up to like & getrecommendations! Published in 2018 at "Blood"
DOI: 10.1182/blood-2018-99-115409
Abstract: Background: The objective of this study was to assess current clinical practices of hematologist/oncologist (hem/onc) specialists related to FLT3 mutations and FLT3 inhibitors used in acute myeloid leukemia (AML), in order to identify knowledge, competency,… read more here.
Keywords: hem onc; knowledge; flt3; flt3 mutations ... See more keywords
Rational polypharmacological targeting of FLT3, JAK2, ABL, and ERK1 suppresses the adaptive resistance to FLT3 inhibitors in AML
Sign Up to like & getrecommendations! Published in 2022 at "Blood Advances"
DOI: 10.1182/bloodadvances.2022007486
Abstract: Key Points • JAK2, ABL, and MAPK signaling drive adaptive resistance to FLT3 inhibitors.• Polypharmacological targeting of FLT3, JAK2, ABL, and MAPK signaling provides a durable response in AML. read more here.
Keywords: flt3 inhibitors; adaptive resistance; jak2 abl; targeting flt3 ... See more keywords
Effect of Fms-like tyrosine kinase 3 (FLT3) ligand (FL) on antitumor activity of gilteritinib, a FLT3 inhibitor, in mice xenografted with FL-overexpressing cells
Sign Up to like & getrecommendations! Published in 2019 at "Oncotarget"
DOI: 10.18632/oncotarget.27222
Abstract: Therapeutic effects of FLT3 inhibitors have been reported in acute myeloid leukemia (AML) with constitutively activating FLT3 mutations, including internal tandem duplication (ITD) and point mutation, which are found in approximately one-third of AML patients.… read more here.
Keywords: flt3; effect; gilteritinib flt3; flt3 inhibitors ... See more keywords
Classification of FLT3 inhibitors and SAR analysis by machine learning methods.
Sign Up to like & getrecommendations! Published in 2023 at "Molecular diversity"
DOI: 10.21203/rs.3.rs-2459483/v1
Abstract: FMS-like tyrosine kinase 3 (FLT3) is a type III receptor tyrosine kinase, which is an important target for anti-cancer therapy. In this work, we conducted a structure-activity relationship (SAR) study on 3867 FLT3 inhibitors we… read more here.
Keywords: flt3; subset subset; flt3 inhibitors; classification flt3 ... See more keywords