Effects of Phosphodiesterase Variants on Angiogenic Functions of Vascular Endothelial Cells

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Monteith, Katie

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thesis

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eng

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angiogenesis , phosphodiesterase splice variant , cAMP , endothelial cells

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Angiogenesis, the biological process of new vessel growth from already existing vasculature, occurs physiologically and pathologically. Previous studies have linked insufficient angiogenic activity to ischemic disease and excessive angiogenesis to cancer. These disease states have a massive global burden. During angiogenic sprouting, a select few endothelial cells (ECs) develop a tip cell phenotype and function to guide cell migration towards angiogenic factors to form the new growth. While angiogenesis is a highly regulated process, the precise molecular mechanisms dictating individual EC functions like migration are not fully identified. The cAMP second messenger is involved in regulating EC angiogenic activity. Macromolecular complexes containing unique combinations of cAMP effectors and individual phosphodiesterase isoforms, provide signal specificity by allowing control of local pools of cAMP to mediate distinct functions. A PDE3B/ protein kinase A (PKA) signalling complex regulating angiogenesis has previously been defined and more recently, it has been shown that impairment of PDE4D signalling induces a hyper-migratory EC phenotype. The studies presented in this thesis investigated the individual PDE4D splice variant responsible for regulating EC migration in telomerase-immortalized ECs. We identified that PDE4D5, not pan-PDE4D or PDE4D7, silencing impedes EC migration. We further identified unique sequences in the N-terminal region of PDE3B and PDE4D isoforms that can be targeted using CRISPR-Cas9 to create stable variant selective knockout cell lines; though due to time constraints, we opted to use other strategies to elucidate individual splice variant function. We additionally found that the creation of a cell line stably expressing a dominant negative PDE4D5 is possible, while PDE4D7 is not. Overall, this work supports the concept that individual PDE isoforms regulate distinct functional pools of cAMP activity and indicates that translation would lead to increased efficacy and decreased side effect profiles of therapeutics targeting dysregulated PDE signalling.

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