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A series of potent PDGFR inhibitors has been identified. The series was optimized for duration of action in the lung. A novel kinase occupancy assay was used to directly measure target occupancy after i.t. dosing. Compound 25 shows 24 h occupancy of the PDGFR kinase domain, after a single i.t. dose and has efficacy at 0.03 mg/kg, in the rat moncrotaline(More)
BACKGROUND Routine apolipoprotein (apo) measurements for cardiovascular disease (CVD) are restricted to apoA-I and apoB. Here, the authors measured an unprecedented range of apolipoproteins in a prospective, population-based study and relate their plasma levels to risk of CVD. OBJECTIVES This study sought to measure apolipoproteins directly by mass(More)
AIMS Extracellular matrix remodelling has been implicated in a number of vascular conditions, including venous hypertension and varicose veins. However, to date, no systematic analysis of matrix remodelling in human veins has been performed. METHODS AND RESULTS To understand the consequences of venous hypertension, normal and varicose veins were evaluated(More)
Fibrosis is a hallmark of many cardiovascular diseases and is associated with the exacerbated secretion and deposition of the extracellular matrix (ECM). Using proteomics, we have previously identified more than 150 ECM and ECM-associated proteins in cardiovascular tissues. Notably, many ECM proteins are glycosylated. This post-translational modification(More)
While lipid abnormalities continue to account for over 60% of the population attributable risk for myocardial infarction, the well-known inverse correlation between plasma high-density lipoprotein (HDL) cholesterol and cardiovascular risk has failed to deliver clinically useful therapeutic interventions. Thus, there is an unmet need to better understand the(More)
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