Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0004153 (atherosclerosis)
 77,401 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Serine protease inhibitors, or serpins, function as central regulators for many vital processes in the mammalian body, maintaining homeostasis for clot formation and breakdown, immune responses, lung function, and hormone or central nervous system activity, among many others. When serine protease activity or serpin-mediated regulation becomes unbalanced or dysfunctional, then severe disease states and pathogenesis can ensue. With serpinopathies, genetic mutations lead to inactive serpins or protein aggregation with loss of function. With other disorders, such as sepsis, atherosclerosis, cancer, obesity, and the metabolic syndrome, the thrombotic and thrombolytic cascades and/or inflammatory responses become unbalanced, with excess bleeding and clotting and upregulation of adverse immune responses. Returning overall balance can be engineered through introduction of a beneficial serpin replacement as a therapeutic or through blockade of serpins that are detrimental. Several drugs have been developed and are currently in use and/or in development both to replace dysfunctional serpins and to block adverse effects induced by aberrant protease or serpin actions.With this chapter, we provide a general overview of the development of a virus-derived serpin, Serp-1, and serpin reactive center loop (RCL) peptides, as therapeutics. Serp-1 is a virus-derived serpin developed as a new class of immune modulator. We will use the development of Serp-1 as a general introduction to serpin-based drug development.
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PMID:Serpins: Development for Therapeutic Applications. 3019 6

Serine proteases and its inhibitors are involved in physiological process and its deregulation lead to various diseases like Chronic Obstructive Pulmonary Disease (COPD), pulmonary emphysema, skin diseases, atherosclerosis, coagulation diseases, cancer, inflammatory diseases, neuronal disorders and other diseases. Serine protease inhibitors have been described in many species, as well as in plants, including cowpea beans (Vigna unguiculata (L.) Walp). Here, we purified and characterized a protease inhibitor, named VuEI (Vigna unguiculata elastase inhibitor), from Vigna unguiculata, with inhibitory activity against HNE (human neutrophil elastase) and chymotrypsin but has no inhibitory activity against trypsin and thrombin. VuEI was obtained by alkaline protein extraction followed by three different chromatographic steps in sequence. First, an ion exchange chromatography using Hitrap Q column was employed, followed by two reversed-phase chromatography using Source15RPC and ACE18 columns. The molecular mass of VuEI was estimated in 10.99 kDa by MALDI-TOF mass spectrometry. The dissociation constant (Ki) to HNE was 9 pM. These data indicate that VuEI is a potent inhibitor of human neutrophil elastase, besides to inhibit chymotrypsin.
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PMID:Neutrophil elastase inhibitor purification strategy from cowpea seeds. 3160 Mar 23


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