A semi-quantitative translational pharmacology analysis to understand the relationship between in vitro ENT1 inhibition and the clinical incidence of dyspnoea and bronchospasm
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- 作者：Lyn Rosenbrier Ribeiro ; Lyn.Rosenbrierribeiro@AstraZeneca.com ; R. Ian Storer
- 关键词：COPD ; chronic pulmonary disease ; ENT ; equilibrative nucleoside transporter ; CNT ; concentrative nucleoside transporter ; NT ; nucleoside transporter ; NBTI ; nitrobenzylthioinosine
- 刊名：Toxicology and Applied Pharmacology
- 出版年：2017
- 出版时间：15 February 2017
- 年：2017
- 卷：317
- 期：Complete
- 页码：41-50
- 全文大小：569 K
- 卷排序：317
文摘
ENT1 inhibition causes bronchospasm and severe dyspnoea in respiratory patients. Neutral or basic compounds with clogP > 5 have increased promiscuity to bind ENT1. ENT1 should be assessed within safety strategies for respiratory research programs. Quantitative translation enables informed risk-assessment of off-target ENT1 activity.