Structure–activity relationships and colorimetric properties of specific probes for the putative cancer biomarker human arylamine N-acetyltransferase 1

…, PT Seden, N Laurieri, SP Lee, KS Hadavizadeh…

Index: Egleton, James E.; Thinnes, Cyrille C.; Seden, Peter T.; Laurieri, Nicola; Lee, Siu Po; Hadavizadeh, Kate S.; Measures, Angelina R.; Jones, Alan M.; Thompson, Sam; Varney, Amy; Wynne, Graham M.; Ryan, Ali; Sim, Edith; Russell, Angela J. Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 11 p. 3030 - 3054

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Citation Number: 5

Abstract

Abstract A naphthoquinone inhibitor of human arylamine N-acetyltransferase 1 (hNAT1), a potential cancer biomarker and therapeutic target, has been reported which undergoes a distinctive concomitant color change from red to blue upon binding to the enzyme. Here we describe the use of in silico modeling alongside structure–activity relationship studies to advance the hit compound towards a potential probe to quantify hNAT1 levels in tissues. ...