Discovery of varlaxins, new aeruginosin-type inhibitors of human trypsins
Lassi Matti Petteri Heinilä, Jouni Jokela, Muhammad N. Ahmed, Matti Wahlsten, Kumar Saurav, Pavel Hrouzek, Perttu Permi, Hannu Koistinen, David P. Fewer, Kaarina Sivonen
Abstract
of 0.62-3.6 nM and 97-230 nM, respectively, including a prometastatic trypsin-3, which is a therapeutically relevant target in several types of cancer. These results substantially broaden the genetic and chemical diversity of the aeruginosin family and provide evidence that the aeruginosin family is a source of strong inhibitors of human serine proteases.
Topics & Concepts
Computational biologyKey (lock)Drug discoveryChemistryBiologyBiochemistryEcologyFree Radicals and AntioxidantsNeurobiology and Insect Physiology ResearchProtein Hydrolysis and Bioactive Peptides