Nature reviews. Endocrinology
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Review
Cardiovascular endocrinology in 2012: PCSK9-an exciting target for reducing LDL-cholesterol levels.
Systemic administration of anti-PCSK9 antibodies induces dramatic reductions in LDL-cholesterol levels, and the effect of this therapy on LDL-receptor activity seems to be additive to that of statin therapy. Inhibition of PCSK9 is potentially very important to the clinician, and should enable more patients to achieve their LDL-cholesterol-level goal.
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In healthy humans, the incretin glucagon-like peptide 1 (GLP-1) is secreted after eating and lowers glucose concentrations by augmenting insulin secretion and suppressing glucagon release. Additional effects of GLP-1 include retardation of gastric emptying, suppression of appetite and, potentially, inhibition of β-cell apoptosis. Native GLP-1 is degraded within ~2-3 min in the circulation; various GLP-1 receptor agonists have, therefore, been developed to provide prolonged in vivo actions. ⋯ The short-acting GLP-1 receptor agonists primarily lower postprandial blood glucose levels through inhibition of gastric emptying, whereas the long-acting compounds have a stronger effect on fasting glucose levels, which is mediated predominantly through their insulinotropic and glucagonostatic actions. The adverse effect profiles of these compounds also differ. The individual properties of the various GLP-1 receptor agonists might enable incretin-based treatment of type 2 diabetes mellitus to be tailored to the needs of each patient.