Fluorescence-based probes applied to sulfoxidases activity and phosphatases inhibition

• Grant number: 09/09489-7
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• Start date: April 01, 2010
• End date: March 31, 2012
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Anita Jocelyne Marsaioli
• Grantee: Caroline da Costa Silva Gonçalves
• Host Institution: Instituto de Química (IQ). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil
• Associated research grant: 09/51602-5 - Chemical biology: new natural and synthetic molecular targets against cancer, structural studies, biological evaluation and mode of action, AP.TEM

Abstract

The enzymatic assays based on fluorescence can be used to monitor enzymatic activity and activity modulation (inhibition or activation) by compounds of interest In view of these assays importance , selectivity and simplicity, new methodologies extending this technique is fundamental. In this context, the first part of the project aims at the development of an HTS umbelliferone-based probe to detect sulfoxidases and evaluate Brazilian microorganisms enzymatic potential. Multibioreaction methodology will validate the HTS hits. Additionally, enzymatic assays can be conveniently used in the processes of identification and improvement of lead compounds in the drug discovery field. Thus, considering the importance of proteins tyrosine phosphatase (PTPs) as therapeutical target, the second part of the project aims the application of the enzymatic fluorescence based assay to monitor Phosphatase 1B (Human, Recombinant Protein Tyrosine - Calbichem, MR. 5440-1102) and Tyrosine Phosphatase (bovine kidney)activity inhibition by a collection of compounds (of synthetic and natural origin). The hits with large inhibition potential will be further investigated by NMR.