Investigation of an OATP1B inhibitory effect by a cyclic peptide using the endogenous biomarker coproporphyrin-I in monkeys [0.03%]
应用内源性生物标志物粪卟啉I检测猴模型中环形多肽OATP1B抑制作用的研究
Hiromi Sawada,Yasuto Kido,Makoto Iwasaki et al.
Hiromi Sawada et al.
Peptide drugs are expected to be a new modality that will replace traditional small molecule drugs. As the number of approved peptide drugs increases, they are being co-administered with various drugs, but there is a limited number of repor...
Continuous exposure to therapeutic drugs doxorubicin and vincristine reduces drug efficacy through transcriptional and post-transcriptional regulation of P-glycoprotein in follicular lymphoma [0.03%]
朵塞和长春新碱的连续暴露通过转录和转录后调节乳腺癌耐药蛋白降低疗法治效性
Kentaro Yano,Yumiko Iwase,Takuo Ogihara et al.
Kentaro Yano et al.
Resistance to drugs used at the onset of follicular lymphoma could develop after continued drug treatment or at the time of recurrence. Therefore, we investigated how the continuous exposure to therapeutic drugs affects P-gp and drug resist...
Drug-drug interaction between trastuzumab emtansine (T-DM1) and orally administered tacrolimus in a patient and in rats [0.03%]
一种患者和大鼠体内的曲妥珠单抗_emtsene与口服他克莫司之间的药物相互作用研究
Tomohiro Nakamura,Moeko Shimada,Makiko Takabayashi et al.
Tomohiro Nakamura et al.
We have experienced a 2.3-fold increase in the trough concentration of orally administered tacrolimus in a patient for 7 days after intravenous administration of trastuzumab emtansine (T-DM1), an antibody-drug conjugate. Retrospective clini...
Investigation of pilocarpine oxidative and hydrolytic metabolism in chimeric mice with humanized liver [0.03%]
人源化肝胆的小鼠体内物理酸碱代谢的氧化和水解研究
Shotaro Uehara,Yuichiro Higuchi,Nao Yoneda et al.
Shotaro Uehara et al.
Chimeric mice with humanized liver (humanized-liver mice) are an attractive alternative to conventional animals for predicting pharmacokinetics in humans. We aimed to investigate the role of CYP2A6 and PON1 on pilocarpine biotransformation ...
Human aldo-keto reductase (AKR) 1C1 and 1C2 act as coactivators of pregnane X receptor, a master regulator of drug-metabolizing and gluconeogenesis enzymes [0.03%]
人醛酮还原酶（AKR）1C1和1C2是孕烷X受体的共激活物，孕烷X受体是一种药物代谢和糖异生酶的主要调节物
Rei Mitamura,Seiya Takemoto,Yuka Aoyama et al.
Rei Mitamura et al.
The aldo-keto reductase (AKR) 1C subfamily, comprising AKR1C1-1C4, plays a crucial role in drug metabolism and hormone biosynthesis. Recent studies have identified AKR1C3 as a co-activator of the androgen receptor. This study aimed to inves...
Functional characteristics of equilibrative nucleoside transporter 2 (ENT2/SLC29A2) for the transport of urate as a newly identified substrate [0.03%]
尿酸作为新型底物的平衡核苷转运蛋白2（ENT2/SLC29A2）的功能特征
Isamu Matake,Tomoya Yasujima,Hirotaka Matsuo et al.
Isamu Matake et al.
Equilibrative nucleoside transporters (ENTs) are known to be involved in the membrane transport of nucleosides and nucleobases. We here report our finding that ENT2/SLC29A2 can also transport urate, which is the final metabolite of purine n...
Current status of Imaging Mass Spectrometry in drug discovery and development: A survey highlighting technical challenges and future directions [0.03%]
成像质谱在药物发现和开发中的现状：技术挑战及未来方向的调查研究
Yukari Tanaka,Hiroyuki Yokoi,Hidefumi Kaji et al.
Yukari Tanaka et al.
Imaging mass spectrometry (IMS) is used in various fields of pharmaceutical research and development, including the targeted delivery of administered drugs, drug distribution in tissues, drug toxicity analysis, and disease mechanisms. Howev...
Buffer compositions strongly impact the in vitro assessment of CYP fraction metabolized using human liver microsomes or expressed isoenzymes [0.03%]
缓冲液组成对使用人肝微粒体或表达同工酶体外评估CYP代谢分数的影响很大
Yuta Tamemoto,Yukihiro Shibata,Natsumi Hashimoto et al.
Yuta Tamemoto et al.
We systematically evaluated the effects of different buffer compositions on the activities of cytochrome P450 (CYP)1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A in human liver microsomes and in recombinant human CYP expres...
Ichiro Fukunaga,Takanori Takebe
Ichiro Fukunaga
Drug-induced liver injury (DILI) presents a major challenge not only in new drug development but also in post-marketing withdrawals and the safety of food, cosmetics, and chemicals. Experimental model organisms such as the rodents have been...