Proteinase Inhibitor Screening Expertise

Pharmahungary Group has filed a patent application in 2011, for ‘Novel inhibitors of matrix metalloproteinases’, US patent publication ID: US20130303572A1 in collaboration with TargetEx Ltd. Pharmahungary Group and TargetEx Ltd. has over 20 years of cumulative experience in screening and developing proteinase inhibitor compounds, focusing on but not limited to ischemic diseases, e.g. ischemic heart disease such as myocardial infarction. Therefore, Pharmahungary Group is uniquely positioned to support the development of your proteinase inhibitor compounds by various assays, including e.g.: MMP activities, protein content and localization of MMPs and TIMPs in vivo and ex vivo by zymography, in situ zymography and Western blot from tissue and perfusate samples. MMP inhibition assay using whole MMP proteins by a zymography based assay. TargetEx can use in-house produced recombinant MMP enzymes (catalytic fragments) for this purpose using synthetic peptides as substrates in FRET assay. TargetEx has also developed assays for other members of the proteinase family (such as 3CLPro, C1s, C1r, MASPs etc.), that could be considered as off-targets. Selectivity against these targets could be identified.


See selected references:

  • Giricz Z et al, J Pharmacol Exp Ther, 2006 (PMID: 16166272)
  • Dormán Gy et al, Recent Pat Cardiovasc Drug Discov, 2007 (PMID: 18221118)
  • Dormán Gy et al, Drugs, 2010 (PMID: 20481653)
  • Bencsik P, et al, Front Pharmacol, 2018 (PMID: 29674965)
  • Gömöri, K. et al, Int J Mol Sci, 2020 (PMID: 32977437)