Characterization, structure and inhibition of the human succinyl-CoA:glutarate-CoA transferase, a genetic modifier of glutaric aciduria type 1

人类琥珀酰辅酶 A:戊二酸辅酶 A 转移酶(1 型戊二酸尿症的遗传修饰剂)的表征、结构和抑制

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作者:Susmita Khamrui, Tetyana Dodatko, Ruoxi Wu, João Leandro, Amanda Sabovic, Sara Violante, Justin R Cross, Eric Marsan, Kunal Kumar, Robert J DeVita, Michael B Lazarus, Sander M Houten

Abstract

Glutaric Aciduria Type 1 (GA1) is a serious inborn error of metabolism with no pharmacological treatments. A novel strategy to treat this disease is to divert the toxic biochemical intermediates to less toxic or non-toxic metabolites. Here, we report a novel target, SUGCT, which we hypothesize suppresses the GA1 metabolic phenotype through decreasing glutaryl-CoA. We report the structure of SUGCT, the first eukaryotic structure of a type III CoA transferase, develop a high-throughput enzyme assay and a cell-based assay, and identify valsartan and losartan carboxylic acid as inhibitors of the enzyme validating the screening approach. These results may form the basis for future development of new pharmacological intervention to treat GA1.

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