Crenolanib is a selective type I pan-FLT3 inhibitor
CC Smith, EA Lasater, KC Lin… - Proceedings of the …, 2014 - National Acad Sciences
Tyrosine kinase inhibitors (TKIs) represent transformative therapies for several
malignancies. Two critical features necessary for maximizing TKI tolerability and response …
malignancies. Two critical features necessary for maximizing TKI tolerability and response …
Discovery of oxindole‐based FLT3 inhibitors as a promising therapeutic lead for acute myeloid leukemia carrying the oncogenic ITD mutation
FMS‐like tyrosine kinase 3 (FLT3) mutations occur in approximately 30% of acute myeloid
leukemia (AML) patients. In the current study, the oxindole chemotype is employed as a …
leukemia (AML) patients. In the current study, the oxindole chemotype is employed as a …
FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia
Y Zhang, CP Hsu, JF Lu, M Kuchimanchi… - … of pharmacokinetics and …, 2014 - Springer
FLT3 ITD subtype acute myeloid leukemia (AML) has a poor prognosis with currently
available therapies. A number of small molecule inhibitors of FLT3 and/or CDK4/6 are …
available therapies. A number of small molecule inhibitors of FLT3 and/or CDK4/6 are …
Design of Novel FLT-3 Inhibitors Based on Dual-Layer 3D-QSAR Model and Fragment-Based Compounds in Silico
KC Shih, CY Lin, HC Chi, CS Hwang… - Journal of chemical …, 2012 - ACS Publications
FMS-like tyrosine kinase 3 (FLT-3) is strongly correlated with acute myeloid leukemia, but no
FLT-3–inhibitor cocomplex structure is available to assist the design of therapeutic inhibitors …
FLT-3–inhibitor cocomplex structure is available to assist the design of therapeutic inhibitors …
Investigating the ibrutinib resistance mechanism of L528W mutation on Brutonʼs tyrosine kinase via molecular dynamics simulations
B Xu, L Liang, Y Jiang, Z Zhao - Journal of Molecular Graphics and …, 2024 - Elsevier
Drug resistance to Bruton's Tyrosine Kinase (BTK) inhibitors presents a challenge in treating
B-cell malignancies, and the mechanism behind drug resistance remains unclear. In this …
B-cell malignancies, and the mechanism behind drug resistance remains unclear. In this …
Pharmacological impact of FLT3 mutations on receptor activity and responsiveness to tyrosine kinase inhibitors
V Marensi, KR Keeshan, DJ MacEwan - Biochemical pharmacology, 2021 - Elsevier
Acute myelogenous leukaemia (AML) is an aggressive blood cancer characterized by the
rapid proliferation of immature myeloid blast cells, resulting in a high mortality rate. The 5 …
rapid proliferation of immature myeloid blast cells, resulting in a high mortality rate. The 5 …
[HTML][HTML] Computational analysis revealing that K634 and T681 mutations modulate the 3D-structure of PDGFR-β and lead to sunitinib resistance
Platelet-derived growth factor receptor-beta (PDGFR-β) is expressed by endothelial cells
(ECs) of tumor-associated blood vessels and regulates primarily early hematopoiesis …
(ECs) of tumor-associated blood vessels and regulates primarily early hematopoiesis …
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit
H Nakano, T Hasegawa, R Imamura, N Saito… - Bioorganic & Medicinal …, 2016 - Elsevier
Abstract A non-selective inhibitor (1) of FMS-like tyrosine kinase-3 (FLT3) was identified by
fragment screening and systematically modified to afford a potent and selective inhibitor 26 …
fragment screening and systematically modified to afford a potent and selective inhibitor 26 …
[HTML][HTML] The structural basis for autoinhibition of FLT3 by the juxtamembrane domain
J Griffith, J Black, C Faerman, L Swenson, M Wynn… - Molecular cell, 2004 - cell.com
FLT3 is a type III receptor tyrosine kinase that is thought to play a key role in hematopoiesis.
Certain classes of FLT3 mutations cause constitutively activated forms of the receptor that …
Certain classes of FLT3 mutations cause constitutively activated forms of the receptor that …
[HTML][HTML] The molecular mechanisms behind activation of FLT3 in acute myeloid leukemia and resistance to therapy by selective inhibitors
R Friedman - Biochimica et Biophysica Acta (BBA)-Reviews on …, 2022 - Elsevier
Acute myeloid leukemia is an aggressive cancer, which, in spite of increasingly better
understanding of its genetic background remains difficult to treat. Mutations in the FLT3 gene …
understanding of its genetic background remains difficult to treat. Mutations in the FLT3 gene …