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Discovery and Development of Prolylcarboxypeptidase Inhibitors for Cardiometabolic Disorders-Chapter Seven

Elsevier Science & Technology
DOI: 10.1016/b978-0-12-417150-3.00007-7
  • 4-Hydroxytamoxifen
  • Alpha-Melanocyte-Stimulating Hormone
  • Aminocylopentane
  • Angiotensin
  • Antiobesity
  • Benzimidazole
  • Benzodihydroisofuran
  • Bradykinin
  • Cardiovascular
  • Endothelin B Receptor-Like Protein 2
  • Exopeptidase
  • Ghrelin
  • Kallikrein–Kinin System
  • Melanocortin
  • Proopiomelanocortin
  • Prolylcarboxypeptidase
  • Pyrimidine-4
  • 6-Diamine
  • Renin–Angiotensin System
  • Serine Protease
  • Um8190
  • Design
  • Medicine


Abstract The serine protease prolylcarboxypeptidase (PRCP) is a unique exopeptidase with regulatory functions in the renin–angiotensin system, the kallikrein–kinin system (KKS), and in hypothalamic proopiomelanocortin downstream processing of alpha-melanocyte-stimulating hormone (α-MSH1–13). PRCP levels have been linked to hypertension, inflammation, and metabolic disorders such as obesity and diabetes. The regulation of hypothalamic melanocortin signaling (via PRCP inhibition of α-MSH1–13 inactivation) represents a novel therapeutic approach in the development of antiobesity agents. Using a combination of rational design approaches and high-throughput screening efforts, a number of potent and protease-selective PRCP inhibitors have been identified and evaluated in animal models.

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