Kazuto Yasuda

Abstract 4360: Development of a novel mithramycin analogue with improved pharmacokinetics and therapeutic window for targeted inhibition of EWS-FLI1 in Ewing sarcoma

Y. Rajesh, Srijan Acharya, Kumar Kulldeep Niloy, Kazuto Yasuda et autres

Background: Ewing Sarcoma (EWS) is characterized by aberrant activity of the oncogenic EWS-FLI1 transcription. Mithramycin (MTM) has been identified to be a specific inhibitor of transcription mediated by the EWS-FLI1. A phase I/II trial and PK study in Ewing sarcoma patients demonstrated …

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The Position of Indole Methylation Controls the Structure, DNA Binding, and Cellular Functions of Mithramycin SA‐Trp Analogues

Caixia Hou, Suhas S. Bhosale, Kazuto Yasuda, Y. Rajesh et autres

Mithramycin (MTM) is a polyketide anticancer natural product, which functions by noncovalent binding to DNA in the minor groove without intercalation, resulting in inhibiting transcription at G/C-rich promoters. MTM is a potent inhibitor of cancer cells, such as Ewing sarcoma, driven by …

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Abstract B150: Targeting EWS-FLI1 with mithramycin analogues for Ewing sarcoma treatment

Markos Leggas, Kumar Kulldeep Niloy, Rajesh Yetijaram, Jamie Horn et autres

Abstract Ewing Sarcoma, a devastating malignancy affecting mainly pediatric and young adult populations, is characterized by the aberrant activity of the oncogenic EWS-FLI1 transcription. However, the development of treatments against EWS-FLI1 is lacking. Mithramycin analogues, exhibiting specificity towards EWS-FLI1, have been posited …

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小学校低学年児童のための学校適応感尺度

Shin Tatsumoto, Shinobu Muta, Yohei Ajikawa, Kazuto Yasuda et autres

本研究は，385名の小学校1・2年生の児童の回答をもとに，17項目からなる自己報告尺度を作成し，因子妥当性，内的整合性，GP分析による弁別力の確認を行った。下位因子は，担任の先生や友達との関わりから得られた学校や教室への適応としての「サポート感」，学校や教室で学び生活する中で得られた自己についての感覚である「自尊感情」，学校や教室に対する感情的な適応感である「環境適応感」の3因子で構成されている。適応感が低い児童を発見し適切な対応を検討するために，また，スクールワイドPBSやプログラム化された予防開発的な生徒指導の実践などの効果査定のために用いていくことが望まれる。

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Vitamin D levels do not cause vitamin-drug interactions with dexamethasone or dasatinib in mice

Kavya Annu, Kazuto Yasuda, William Caufield, Burgess B. Freeman et autres

Vitamin D3 (VD3) induces intestinal CYP3A that metabolizes orally administered anti-leukemic chemotherapeutic substrates dexamethasone (DEX) and dasatinib potentially causing a vitamin-drug interaction. To determine the impact of VD3 status on systemic exposure and efficacy of these chemotherapeutic agents, we used VD3 sufficient …

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Metabolomic and transcriptomic analysis reveals endogenous substrates and metabolic adaptation in rats lacking Abcg2 and Abcb1a transporters

Samit Ganguly, David Finkelstein, Timothy I. Shaw, Ryan D. Michalek et autres

Abcg2/Bcrp and Abcb1a/Pgp are xenobiotic efflux transporters limiting substrate permeability in the gastrointestinal system and brain, and increasing renal and hepatic drug clearance. The systemic impact of Bcrp and Pgp ablation on metabolic homeostasis of endogenous substrates is incompletely understood. We performed …

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In-situ annealing of MOVPE grown CdTe layers on n + -(211)Si substrate

Toshiki Matsubara, Tatsuhiro Kobayashi, Hayata Goto, Seiya Fujii et autres

Role of Vitamins A and D in BCR-ABL Arf−/− Acute Lymphoblastic Leukemia

Kavya Annu, Cynthia Cline, Kazuto Yasuda, Samit Ganguly et autres

Abstract The effects of vitamin A and/or vitamin D deficiency were studied in an Arf−/− BCR-ABL acute lymphoblastic leukemia murine model. Vitamin D sufficient mice died earlier (p = 0.003) compared to vitamin D deficient (VDD) mice. Vitamin A deficient (VAD) mice …

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Pheophorbide A: Fluorescent Bcrp Substrate to Measure Oral Drug-Drug Interactions in Real-Time In Vivo

Kazuto Yasuda, Samit Ganguly, Erin G. Schuetz

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CRISPR/Cas9 Genetic Modification of CYP3A5 *3 in HuH-7 Human Hepatocyte Cell Line Leads to Cell Lines with Increased Midazolam and Tacrolimus Metabolism

Casey R. Dorr, Rory P. Remmel, Amutha Muthusamy, James W. Fisher et autres

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In Vivo Imaging of Human MDR1 Transcription in the Brain and Spine of MDR1-Luciferase Reporter Mice

Kazuto Yasuda, Cynthia Cline, Yvonne S. Lin, Rachel Scheib et autres

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Genetic variation in aldo‐keto reductase 1D1 (AKR1D1) affects expression and activity of multiple cytochrome P450s (LB595)

Amarjit S. Chaudhry, Ranjit K. Thirumaran, Kazuto Yasuda, Xia Yang et autres

Human liver gene regulatory network analysis identified a cytochrome P450 subnetwork with AKR1D1 as its key regulatory driver. This study assessed the biologic importance of AKR1D1 [key enzyme in synthesis of bile acids, ligand activators of FXR, PXR and CAR, known P450 …

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