Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolism.
Article Details
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Terasaka T, Tsuji K, Kato T, Nakanishi I, Kinoshita T, Kato Y, Kuno M, Inoue T, Tanaka K, Nakamura K
Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolism.
J Med Chem. 2005 Jul 28;48(15):4750-3.
- PubMed ID
- 16033254 [ View in PubMed]
- Abstract
From metabolic considerations and prediction of an inhibitor-induced conformational change, novel adenosine deaminase (ADA) inhibitors with improved activities and oral bioavailability have been developed on the basis of our originally designed non-nucleoside ADA inhibitors. They demonstrated in vivo efficacy in models of inflammation and lymphoma. Furthermore, X-ray crystal structure analysis has revealed a novel induced fit to ADA.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) FR-234938 Adenosine deaminase IC 50 (nM) 16 N/A N/A Details FR230513 Adenosine deaminase IC 50 (nM) 570 N/A N/A Details FR239087 Adenosine deaminase IC 50 (nM) 15 N/A N/A Details