Esteve and Enzymlogic join together to drive GPCR drug discovery
Jan, 19th 2017
Enzymlogic has entered into a research collaboration agreement with Esteve whereby Enzymlogic will direct its novel Binding Kinetics Platform to characterize selected compounds against mu-Opioid receptor.
The collaboration combines Enzymlogic’s unique Binding Kinetics Platform and vast experience kinetically screening kinase inhibitors with the GPCR expertise from Esteve. GPCRs are the largest class of membrane proteins in the human genome and an estimated 40% of marketed drugs modulate these targets. Pharmacological characterization of GPCR ligands has traditionally focused on potency and efficacy, where concentration-dependent parameters are measured at equilibrium. There is, however, a growing evidence for the physiological relevance of the temporal aspects of ligand-GPCRs interactions.
The two companies recently completed a pilot study whereby the Enzymlogic’s Binding Kinetics Platform was applied to kinetically analyze a selected subset of small molecules against mu-Opioid Receptor. This pilot resulted in promising initial results, demonstrating the ability of Enzymlogic’s Binding Kinetics Platform to rapidly characterize compounds with different kinetic profiles upon binding to GPCR targets. This successful initial validation of the GPCR Binding Kinetics Platform, and subsequent enhancements of the platform, will allow Enzymlogic to expand its binding kinetics portfolio to a broad range of GPCR assays and bring to the industry novel solutions in the field of GPCR drug discovery.
Enzymlogic offers in vitro biochemical and cell-based assays to the biotechnological and pharmaceutical companies, life science laboratories and academic groups. Our binding kinetics, kinetic selectivity, assay development, profiling and screening services enable faster and cost-effective drug discovery by identifying the most promising drug candidates as well as withdrawing those compounds likely to fail in pre-clinical development. Additionally, Enzymlogic’s pioneering approach provides predictive tools that deliver physiologically relevant insights earlier in the drug discovery process.
ESTEVE is an international pharmaceutical chemical group that focuses its efforts on innovation and excellence in the field of health, striving daily to achieve customer satisfaction and to contribute to the wellbeing of society. Founded in 1929 and presided over by Joan Esteve, the Company currently employs 2,279 people, has a presence in Europe, USA, Mexico and China. Since then, thanks to intensive research, an international approach and an active policy of strategic alliances with other companies, ESTEVE has established itself as a leading business group in the area of health. Research being ESTEVE’s hallmark, a portfolio of highly innovative projects ultimately aims to provide response to unmet medical needs.Back