絞り込み

16530

広告

大飯原発訴訟 住民側が上告断念 敗訴確定へ

福井県にある大飯原子力発電所3号機と4号機について、住民らが関西電力に運転しないよう求めた裁判で、住民側は、17日、最高裁判所に上告しない方針を明らかにしました...

  1. 西日本豪雨の災害ごみ、中川環境相「広域処...
  2. ジェームズ・ウェッブ宇宙望遠鏡、今年2度...
  3. 版画・彫刻家の浜田知明さん死去 戦争テー...
  4. 俳優の生田悦子さん死去 (NHK)

ニュース一覧

Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1.

著者 Koide H , Tsujimoto M , Takeuchi A , Tanaka M , Ikegami Y , Tagami M , Abe S , Hashimoto M , Minegaki T , Nishiguchi K
Xenobiotica.2017 Oct 16 ; ():1-37.
この記事をPubMed上で見るPubMedで表示
この記事をGoogle翻訳上で見る Google翻訳で開く

スターを付ける スターを付ける     (42view , 0users)

Full Text Sources

1. Organic anion-transporting polypeptide 1B1 (OATP1B1) plays an important role in the hepatic uptake of a broad range of substrate drugs. In vitro experiments show that molecular-targeted agents do not always have similar effects on OATP1B1 activity. 2. The purpose of this study was to clarify whether the effects of molecular-targeted agents on OATP1B1 are substrate-dependent. We used OATP1B1-transfected cells to compare the effects of molecular-targeted agents on OATP1B1-mediated uptake of fluorescein (FL), 2',7'-dichlorofluorescein (DCF), atorvastatin, SN-38, and valsartan. 3. Cabozantinib, cediranib, neratinib, pazopanib, regorafenib, sorafenib, and tivantinib did not affect or only slightly affected OATP1B1-mediated substrate uptake. Nilotinib and lenvatinib moderately and strongly inhibited OATP1B1-mediated substrate uptake, respectively. In contrast, afatinib stimulated OATP1B1-mediated uptake of fluorescein and SN-38, ceritinib stimulated that of valsartan, and nintedanib stimulated that of fluorescein and valsartan. In addition, the effects of afatinib, ceritinib, and nintedanib on OATP1B1 activity differed markedly depending on the type of substrate. Afatinib, ceritinib, and nintedanib had a substrate-dependent effect on OATP1B1 activity. 4. We conclude that the evaluation of OATP1B1 activity using only a single probe substrate for some molecular-targeted agents may lead to a faulty understanding of their mechanisms of drug interactions.
PMID: 29034773 [PubMed - as supplied by publisher]
印刷用ページを開く Endnote用テキストダウンロード