Petrera Agnese, Gassenhuber Johann, Ruf Sven, Gunasekaran Deepika, Esser Jennifer, Shahinian Jasmin Hasmik, Hübschle Thomas, Rütten Hartmut, Sadowski Thorsten, Schilling Oliver
Institute for Molecular Medicine and Cell Research, University of Freiburg, Stefan Meier Strasse 17, 79104, Freiburg, Germany.
Sanofi-Aventis Deutschland GmbH, Industriepark Höchst, 65926, Frankfurt Am Main, Germany.
J Transl Med. 2016 May 31;14(1):153. doi: 10.1186/s12967-016-0907-8.
Myocardial infarction (MI) is a major cause of heart failure. The carboxypeptidase cathepsin A is a novel target in the treatment of cardiac failure. We aim to show that recently developed inhibitors of the protease cathepsin A attenuate post-MI heart failure.
Mice were subjected to permanent left anterior descending artery (LAD) ligation or sham operation. 24 h post-surgery, LAD-ligated animals were treated with daily doses of the cathepsin A inhibitor SAR1 or placebo. After 4 weeks, the three groups (sham, MI-placebo, MI-SAR1) were evaluated.
Compared to sham-operated animals, placebo-treated mice showed significantly impaired cardiac function and increased plasma BNP levels. Cathepsin A inhibition prevented the increase of plasma BNP levels and displayed a trend towards improved cardiac functionality. Proteomic profiling was performed for the three groups (sham, MI-placebo, MI-SAR1). More than 100 proteins were significantly altered in placebo-treated LAD ligation compared to the sham operation, including known markers of cardiac failure as well as extracellular/matricellular proteins. This ensemble constitutes a proteome fingerprint of myocardial infarction induced by LAD ligation in mice. Cathepsin A inhibitor treatment normalized the marked increase of the muscle stress marker CA3 as well as of Igγ 2b and fatty acid synthase. For numerous further proteins, cathepsin A inhibition partially dampened the LAD ligation-induced proteome alterations.
Our proteomic and functional data suggest that cathepsin A inhibition has cardioprotective properties and support a beneficial effect of cathepsin A inhibition in the treatment of heart failure after myocardial infarction.
心肌梗死(MI)是心力衰竭的主要原因。羧肽酶组织蛋白酶A是治疗心力衰竭的新靶点。我们旨在证明,最近开发的组织蛋白酶A蛋白酶抑制剂可减轻心肌梗死后的心力衰竭。
对小鼠进行永久性左冠状动脉前降支(LAD)结扎或假手术。术后24小时,对LAD结扎的动物每日给予组织蛋白酶A抑制剂SAR1或安慰剂。4周后,对三组(假手术组、心肌梗死-安慰剂组、心肌梗死-SAR1组)进行评估。
与假手术动物相比,接受安慰剂治疗的小鼠心脏功能明显受损,血浆脑钠肽(BNP)水平升高。组织蛋白酶A抑制可防止血浆BNP水平升高,并显示出心脏功能改善的趋势。对三组(假手术组、心肌梗死-安慰剂组、心肌梗死-SAR1组)进行了蛋白质组分析。与假手术相比,接受安慰剂治疗的LAD结扎小鼠中有100多种蛋白质发生了显著变化,包括已知的心力衰竭标志物以及细胞外/基质细胞蛋白。这一组合构成了小鼠LAD结扎诱导的心肌梗死蛋白质组指纹图谱。组织蛋白酶A抑制剂治疗使肌肉应激标志物CA3以及Igγ 2b和脂肪酸合酶的显著升高恢复正常。对于许多其他蛋白质,组织蛋白酶A抑制部分减轻了LAD结扎诱导的蛋白质组改变。
我们的蛋白质组学和功能数据表明,组织蛋白酶A抑制具有心脏保护特性,并支持组织蛋白酶A抑制在治疗心肌梗死后心力衰竭中的有益作用。