Abstract：
:The survival of patients with pulmonary arterial hypertension is closely related with right ventricular function. During the progression of right ventricular remodeling, energetic metabolism shifts from oxidative mitochondrial metabolism to glycolysis. In normal physiological conditions, cardiomyocytes use major sources of glucose and fatty acids to sustain a continuous systolic workload and energy supply. This allows the heart to choose the most efficient substrate to response to environmental stimuli. Therefore, ATP production of glucose is the preferred energy source than fatty acids in right ventricular remodeling. However, the metabolic fate of glucose altered because mitochondrial metabolism is actively suppressed. Metabolic shift towards aerobic glycolysis and down-regulation of mitochondrial oxidation, is called the Warburg effect. Studies on animal models and human RVF suggest that there is reduced glucose oxidation and increased glycolysis in both adaptive and maladaptive right ventricular failure. Accordingly, a gate-keeping enzyme, pyruvate dehydrogenase kinase (PDK) is activated and inhibited pyruvate into the mitochondria with increased lactate dehydrogenase. Therefore, augmentation of glucose oxidation is beneficial in right ventricular remodeling and can be achieved by inhibition of PDK and fatty acid oxidation. As a PDK inhibitor, Dicholoracetate (DCA) can reduce pyruvate dehydrogenase phosphorylation and partially restore RV structure and function by promoting glucose and mitochondrial oxidation. Moreover, the partial inhibitors of fatty acid oxidation would be offered the utilization to improve right ventricular function. Although metabolic targeting drugs can be beneficial to right ventricular remodeling, the advantage of modulating metabolic shift into an enhanced clinical performance still remains to be determined.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Zhang R,Jing ZCdoi
10.2174/1381612822666160614082712subject
Has Abstractpub_date
2016-01-01 00:00:00pages
4780-4795issue
31eissn
1381-6128issn
1873-4286pii
CPD-EPUB-76537journal_volume
22pub_type
杂志文章,评审abstract：:Since identifying a transmissible agent responsible for tumorigenesis in chickens, the v-Src oncogene, significant progress has been made in determining the functions of its cellular homologue. c-Src is the product of the SRC gene and has been found both over-expressed and highly activated in a number of human cancers...
journal_title：Current pharmaceutical design
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journal_title：Current pharmaceutical design
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更新日期：2013-01-01 00:00:00
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