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ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

Amino acid transporter

ASCT2-mediated glutamine uptake promotes Th1 differentiation via ROS-EGR1-PAC1 pathway in oral lichen planus

86 views | Nov 11 2023

The study reveals that glutamine uptake mediated by ASCT2 plays a pivotal role in promoting Th1 differentiation through a ROS-EGR1-PAC1 pathway in oral lichen planus, suggesting that targeting ASCT2 could be a potential therapeutic approach for T cell-mediated autoimmune diseases by restoring redox balance. [Read the Full Post]

Targeting Glutaminolysis Shows Efficacy in Both Prednisolone-Sensitive and in Metabolically Rewired Prednisolone-Resistant B-Cell Chi

83 views | Aug 29 2023

The study revealed that prednisolone-resistant childhood acute lymphoblastic leukemia (cALL) cells exhibit significant alterations in metabolic pathways, including oxidative phosphorylation, glycolysis, amino acid metabolism, and activation of mTORC1 and MYC signaling, highlighting the potential therapeutic target of inhibiting glutamine metabolism. [Read the Full Post]

Selective Inhibition of L-type Amino Acid Transporter 1 Suppresses Cell Proliferation in Ovarian Clear Cell Carcinoma

73 views | Aug 20 2023

Selective inhibition of L-type amino acid transporter 1 (LAT1) using nanvuranlat (JPH203) effectively suppresses cell proliferation via the mTOR pathway by inhibiting leucine uptake in ovarian clear cell carcinoma (OCCC), suggesting LAT1 as a potential therapeutic target for this aggressive ovarian cancer. [Read the Full Post]

Pharmacologic inhibition of LAT1 predominantly suppresses transport of large neutral amino acids and downregulates global translation in cancer cells

79 views | Sep 17 2022

Kou Nishikubo et al. demonstrated a predominant contribution of LAT1 to the transport of large neutral amino acids in cancer cells and the suppression of protein synthesis by JPH203 supposed to underly its broad anti-proliferative effects across various types of cancer cells. [Read the Full Post]

LAT1 inhibitor JPH203 sensitizes cancer cells to radiation by enhancing radiation-induced cellular senescence

304 views | Oct 26 2021

Tomoki Bo et al. showed that JPH203 might be a potent anti-cancer drug in combination with radiation therapy. [Read the Full Post]

Small molecule inhibitors provide insights into the relevance of LAT1 and LAT2 in materno-foetal amino acid transport

361 views | Nov 04 2020

Jonas Zaugg et al. thought that differential specificity of the applied inhibitors allowed for estimation of the contribution of LAT1 and LAT2 in materno-foetal AA transfer and their potential impact in pregnancy diseases associated with impaired foetal growth. [Read the Full Post]

JPH203, a selective L-type amino acid transporter 1 inhibitor, induces mitochondria-dependent apoptosis in Saos2 human osteosarcoma cells

571 views | Jan 08 2020

Choi DW et al. suggested that the inhibition of LAT1 activity via JPH203, which may act as a potential novel anti-cancer agent, leads to apoptosis mediated by the mitochondria-dependent intrinsic apoptotic signaling pathway by inducing the intracellular depletion of neutral amino acids essential for cell growth in Saos2 human osteosarcoma cells. [Read the Full Post]

Inhibition of the amino-acid transporter LAT1 demonstrates anti-neoplastic activity in medulloblastoma

561 views | Aug 10 2019

Cormerais Y et al. demonstrated that a long-term treatment with JPH203 does not lead to resistance in MB cells. Therefore, this study suggests that targeting LAT1 with JPH203 is a promising therapeutic approach for MB treatment. [Read the Full Post]