京都大学 · 医学
Fumiyoshi Yamashita教授の研究室は、医薬候補化合物の創出とその臨床応用可能性を高めるために、in silicoによるADME予測技術の開発を主眼としています。特に、薬物代謝酵素CYP3A4の発現誘導機構を解明し、薬物相互作用のリスクを低減するための予測モデルの構築を進めています。また、環境由来の有害物質が胎児に与える影響(例:PCBによる胎児PCB症候群)の臨床的・代謝的メカニズムの解明にも貢献しています。
Figures are computed from collected data and may differ slightly.
Combinatorial chemistry and high-throughput screening have increased the possibility of finding new lead compounds at much shorter time periods than conventional medicinal chemistry. However, too much promising drug candidates often fail because of unsatisfactory ADME properties. In silico ADME studies are expected to reduce the risk of late-stage attrition of drug development and to optimize screening and testing by looking at only the promising compounds. To this end, many in silico approaches
Pregnant mothers with yusho in Fukuoka, Nagasaki and Kochi Prefectures delivered babies with a peculiar clinical manifestation which will be called fetal PCB syndrome (FPS). The birth rate incidences were 3.6% (Fukuoka Prefecture), 4% (Nagasaki Prefecture), 2.9% (Kochi Prefecture) and 3.9% (total). The manifestations consisted of dark brown pigmentation of the skin and the mucous membrane, gingival hyperplasia, exophthalmic edematous eye, dentition at birth, abnormal calcification of the skull a
Induction of cytochrome P450 3A4 (CYP3A4) expression is often implicated in clinically relevant drug-drug interactions (DDI), as metabolism catalyzed by this enzyme is the dominant route of elimination for many drugs. Although several DDI models have been proposed, none have comprehensively considered the effects of enzyme transcription/translation dynamics on induction-based DDI. Rifampicin is a well-known CYP3A4 inducer, and is commonly used as a positive control for evaluating the CYP3A4 indu
Fumio Yamashita, Masao Hayashi, Fetal PCB Syndrome: Clinical Features, Intrauterine Growth Retardation and Possible Alteration in Calcium Metabolism, Environmental Health Perspectives, Vol. 59 (Feb., 1985), pp. 41-45
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