Activador do plasminóxeno

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Os activadores do plasminóxeno son serina proteases que catalizan a activación da plasmina ao clivar proteoliticamente o seu cimóxeno precursor, o plasminóxeno.[1] A plasmina é un importante factor na fibrinólise, a degradación dos polímeros de fibrina formados durante a coagulación do sangue (destrución de coágulos). Existen dous activadores do plasminóxeno:

Os activadores do plasminóxeno úsanse en medicina. O activador do plasminóxeno tisular utilízase para tratar ictus embólicos ou trombóticos, infarto de miocardio e embolia pulmonar.[2] Prodúcese en forma recombinante, o rtPA.[3] A uroquinase utilízase para tratar embolias pulmonares.[4]

Os activadores do plasminóxeno son inhibidos polo inhibidor do activador do plasminóxeno 1 (PAI-1)[5][6], o inhibidor do activador do plasminóxeno 2 (PAI-2, producido só na placenta),[7] e o inhibidor da proteína C.[8]

Estrutura tridimensional do tPA
Estrutura tridimensional da uPA

Notas[editar | editar a fonte]

  1. Law RH, Caradoc-Davies T, Cowieson N, Horvath AJ, Quek AJ, Encarnacao JA, Steer D, Cowan A, Zhang Q, Lu BG, Pike RN, Smith AI, Coughlin PB, Whisstock JC (March 2012). "The X-ray crystal structure of full-length human plasminogen". Cell Reports 1 (3): 185–90. PMID 22832192. doi:10.1016/j.celrep.2012.02.012. 
  2. Rivera-Bou WL (15 December 2016). "Thrombolytic Therapy". MedScape. Consultado o 28 February 2017. 
  3. Gurman P, Miranda OR, Nathan A, Washington C, Rosen Y, Elman NM (March 2015). "Recombinant tissue plasminogen activators (rtPA): a review". Clinical Pharmacology and Therapeutics 97 (3): 274–85. PMID 25670034. doi:10.1002/cpt.33. 
  4. "LABEL: KINLYTIC- urokinase injection, powder, lyophilized, for solution". DailyMed: US National Library of Medicine. 8 June 2007. 
  5. Declerck PJ, Gils A (June 2013). "Three decades of research on plasminogen activator inhibitor-1: a multifaceted serpin". Seminars in Thrombosis and Hemostasis 39 (4): 356–64. PMID 23504606. doi:10.1055/s-0033-1334487. 
  6. Mimuro J (May 1991). "[Type 1 plasminogen activator inhibitor: its role in biological reactions]". [Rinsho Ketsueki] the Japanese Journal of Clinical Hematology 32 (5): 487–9. PMID 1870265. 
  7. Mikus P, Urano T, Liljeström P, Ny T (December 1993). "Plasminogen-activator inhibitor type 2 (PAI-2) is a spontaneously polymerising SERPIN. Biochemical characterisation of the recombinant intracellular and extracellular forms". European Journal of Biochemistry 218 (3): 1071–82. PMID 7506655. doi:10.1111/j.1432-1033.1993.tb18467.x. 
  8. Laurell M, Christensson A, Abrahamsson PA, Stenflo J, Lilja H (April 1992). "Protein C inhibitor in human body fluids. Seminal plasma is rich in inhibitor antigen deriving from cells throughout the male reproductive system". The Journal of Clinical Investigation 89 (4): 1094–101. PMC 442965. PMID 1372913. doi:10.1172/JCI115689.