GW-788,388 explained

GW 788388 is a synthetic compound which acts as a potent and selective inhibitor for TGF beta receptor 1.[1] It has applications in research into various disorders such as liver, kidney and heart disease (especially associated with Chagas disease),[2] [3] [4] [5] [6] [7] and potential antiviral properties.[8]

See also

Notes and References

  1. Gellibert F, de Gouville AC, Woolven J, Mathews N, Nguyen VL, Bertho-Ruault C, Patikis A, Grygielko ET, Laping NJ, Huet S . 6 . Discovery of 4--N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor . Journal of Medicinal Chemistry . 49 . 7 . 2210–2221 . April 2006 . 16570917 . 10.1021/jm0509905 .
  2. de Oliveira FL, Araújo-Jorge TC, de Souza EM, de Oliveira GM, Degrave WM, Feige JJ, Bailly S, Waghabi MC . 6 . Oral administration of GW788388, an inhibitor of transforming growth factor beta signaling, prevents heart fibrosis in Chagas disease . PLOS Neglected Tropical Diseases . 2012 . 6 . 6 . e1696 . 22720109 . 10.1371/journal.pntd.0001696 . 3373641 . free .
  3. McMillin M, Grant S, Frampton G, Petrescu AD, Williams E, Jefferson B, DeMorrow S . The TGFβ1 Receptor Antagonist GW788388 Reduces JNK Activation and Protects Against Acetaminophen Hepatotoxicity in Mice . Toxicological Sciences . 170 . 2 . 549–561 . May 2019 . 31132129 . 10.1093/toxsci/kfz122 . 6821297 .
  4. Petersen M, Thorikay M, Deckers M, van Dinther M, Grygielko ET, Gellibert F, de Gouville AC, Huet S, ten Dijke P, Laping NJ . 6 . Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis . Kidney International . 73 . 6 . 705–715 . March 2008 . 18075500 . 10.1038/sj.ki.5002717 . free .
  5. Tan SM, Zhang Y, Connelly KA, Gilbert RE, Kelly DJ . Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction . American Journal of Physiology. Heart and Circulatory Physiology . 298 . 5 . H1415–H1425 . May 2010 . 20154262 . 10.1152/ajpheart.01048.2009 .
  6. Ferreira RR, Abreu RD, Vilar-Pereira G, Degrave W, Meuser-Batista M, Ferreira NV, da Cruz Moreira O, da Silva Gomes NL, Mello de Souza E, Ramos IP, Bailly S, Feige JJ, Lannes-Vieira J, de Araújo-Jorge TC, Waghabi MC . 6 . TGF-β inhibitor therapy decreases fibrosis and stimulates cardiac improvement in a pre-clinical study of chronic Chagas' heart disease . PLOS Neglected Tropical Diseases . 13 . 7 . e0007602 . July 2019 . 31365537 . 10.1371/journal.pntd.0007602 . 6690554 . free .
  7. Lho Y, Do JY, Heo JY, Kim AY, Kim SW, Kang SH . Effects of TGF-β1 Receptor Inhibitor GW788388 on the Epithelial to Mesenchymal Transition of Peritoneal Mesothelial Cells . International Journal of Molecular Sciences . 22 . 9 . April 2021 . 4739 . 33947038 . 10.3390/ijms22094739 . 8124410 . free .
  8. Teixeira GS, Andrade AA, Torres LR, Couto-Lima D, Moreira OC, Abreu R, Waghabi MC, de Souza EM . 6 . Suppression of TGF-β/Smad2 signaling by GW788388 enhances DENV-2 clearance in macrophages . Journal of Medical Virology . 94 . 9 . 4359–4368 . September 2022 . 35596058 . 10.1002/jmv.27879 . 9544077 . 250497172 .

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