| Title : Discovery of arginine-containing tripeptides as a new class of pancreatic lipase inhibitors - Stefanucci_2019_Future.Med.Chem_11_5 |
| Author(s) : Stefanucci A , Luisi G , Zengin G , Macedonio G , Dimmito MP , Novellino E , Mollica A |
| Ref : Future Med Chem , 11 :5 , 2019 |
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Abstract :
AIM: The inhibition of pancreatic lipase (PL) represents one of the most promising strategies in the search for novel antiobesity drugs. We propose here a pioneering course by exploring tripeptide scaffolds in the way to selective PL inhibitors. METHODOLOGY/RESULTS: The peptide series exhibited good PL inhibitory properties in vitro, with all the strongest inhibitors sharing a central arginine, shown in silico to be relevant for the active site-directed activity. The compounds were found devoid of inhibitory properties on acetylcholinesterase. CONCLUSION: Present results disclosed that basic tripeptides are able to interact efficiently with the PL-binding pocket, where they adopt a binding pose suitable for functional-to-inhibition interactions with key amino acids. Main inhibitor MALA4 may be selected as lead for further optimization. |
| PubMedSearch : Stefanucci_2019_Future.Med.Chem_11_5 |
| PubMedID: 30526045 |
Stefanucci A, Luisi G, Zengin G, Macedonio G, Dimmito MP, Novellino E, Mollica A (2019)
Discovery of arginine-containing tripeptides as a new class of pancreatic lipase inhibitors
Future Med Chem
11 :5
Stefanucci A, Luisi G, Zengin G, Macedonio G, Dimmito MP, Novellino E, Mollica A (2019)
Future Med Chem
11 :5