San Diego State University Heart Institute and the Department of Biology, San Diego State University, San Diego, CA 92182, USA.
Proc Natl Acad Sci U S A. 2013 Jul 30;110(31):12661-6. doi: 10.1073/pnas.1301455110. Epub 2013 Jul 10.
Mechanistic target of rapamycin complex 1 (mTORC1), necessary for cellular growth, is regulated by intracellular signaling mediating inhibition of mTORC1 activation. Among mTORC1 regulatory binding partners, the role of Proline Rich AKT Substrate of 40 kDa (PRAS40) in controlling mTORC1 activity and cellular growth in response to pathological and physiological stress in the heart has never been addressed. This report shows PRAS40 is regulated by AKT in cardiomyocytes and that AKT-driven phosphorylation relieves the inhibitory function of PRAS40. PRAS40 overexpression in vitro blocks mTORC1 in cardiomyocytes and decreases pathological growth. Cardiomyocyte-specific overexpression in vivo blunts pathological remodeling after pressure overload and preserves cardiac function. Inhibition of mTORC1 by PRAS40 preferentially promotes protective mTORC2 signaling in chronic diseased myocardium. In contrast, strong PRAS40 phosphorylation by AKT allows for physiological hypertrophy both in vitro and in vivo, whereas cardiomyocyte-specific overexpression of a PRAS40 mutant lacking capacity for AKT-phosphorylation inhibits physiological growth in vivo, demonstrating that AKT-mediated PRAS40 phosphorylation is necessary for induction of physiological hypertrophy. Therefore, PRAS40 phosphorylation acts as a molecular switch allowing mTORC1 activation during physiological growth, opening up unique possibilities for therapeutic regulation of the mTORC1 complex to mitigate pathologic myocardial hypertrophy by PRAS40.
雷帕霉素靶蛋白复合物 1(mTORC1)是细胞生长所必需的,其活性受到细胞内信号的调节,这些信号介导了 mTORC1 激活的抑制。在 mTORC1 的调节结合伴侣中,富脯氨酸 AKT 底物 40kDa(PRAS40)在调节心脏病理和生理应激下的 mTORC1 活性和细胞生长中的作用尚未得到阐明。本报告表明 PRAS40 在心肌细胞中受 AKT 调节,AKT 驱动的磷酸化可解除 PRAS40 的抑制功能。体外过表达 PRAS40 可阻断心肌细胞中的 mTORC1,减少病理性生长。体内心肌细胞特异性过表达可减轻压力超负荷后的病理性重构,保护心脏功能。PRAS40 通过抑制 mTORC1 可优先促进慢性病变心肌中的保护性 mTORC2 信号。相反,AKT 对 PRAS40 的强烈磷酸化可促进体外和体内的生理性肥大,而 AKT 磷酸化能力缺失的 PRAS40 突变体的心肌细胞特异性过表达则抑制体内的生理性生长,表明 AKT 介导的 PRAS40 磷酸化是诱导生理性肥大所必需的。因此,PRAS40 磷酸化可作为分子开关,允许 mTORC1 在生理性生长过程中激活,为通过 PRAS40 调节 mTORC1 复合物来减轻病理性心肌肥大提供了独特的治疗调控可能性。