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Cardiovascular disease is the most common cause of morbidity and mortality in the developed countries, and it accounted for over 600,000 deaths (25% of total mortality) in the U.S. in 2006 [1]. However, despite significant progress in the treatment of cardiovascular diseases, the mortality rate from heart failure still remains very high. Because cardiac hypertrophy is associated with most forms of heart failure, the mechanisms and related therapies for cardiac hypertrophy have remained a central focus of basic and clinical research [2, 3]. Cardiovascular pharmacology is a rapidly developing field with numerous new cardiovascular drugs continually being discovered, and being tested in preclinical studies and clinical trials. In this issue, we will review novel therapies that are on the horizon for the treatment of cardiac hypertrophy and heart failure. Review of these new and emerging pharmacological therapies will not only be interesting, but also will be important for clinical practice. Although complete list of all novel pharmacological therapies is not possible, this review series compile those therapies that hold promise in the near future. Specialists in various fields will contribute their expertise, experience and knowledge on current and emerging cardiovascular pharmacological therapies. Leading off the series, Xia and Vanhoutte, an internationally renowned authority on nitric oxide, will review current status of nitric oxide (NO) inhibition for hypertension and cardiac hypertrophy. They will specifically focus on the role of NO in ischemic myocardial protection with emphasis on its contribution to ischemic pre-and post-conditioning cardioprotection. Singh and Kang will review emerging therapies to inhibit apoptosis in cardiovascular diseases. We will discuss what is currently known about the molecular mechanisms of cardiac apoptosis, and review the potential uses of anti-apoptotic therapies for heart failure. Wu-Wong will review our current understanding of vitamin D signaling in cardiovascular diseases. She will discuss preclinical and clinical studies that support (or argue against) the potential use of vitamin D therapy for left ventricular hypertrophy and heart failure, as well as its broad use for end stage renal disease and vascular diseases. Yan and Morgan, experts on pharmacological therapy for heart failure, will review the current knowledge of the neuregulin 1 (NRG1) and eukaryotic ribosome biogenesis protein 1 (Erb1) signaling in the heart and discuss the potential use of NRG1s as novel therapy for heart failure. Ayogi and Matsui will review the role of phosphatidylinositol 3-kinases (PI3K) signaling in the treatment of cardiac hypertrophy and heart failure. They will discuss the reciprocal regulation of PI3K, serine/threonine protein kinase Akt/PKB and the mammalian target of rapamycin (mTOR) in cardiomyocytes and their association with cardiac disease. For our final review in the series, Kim and Lee will review the role of nanotechnology in medicine. Particularly, they will discuss several novel strategies to use nanomaterial-based diagnosis and therapy in cardiovascular and neurovascular diseases.