Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family.

ABSTRACT:

Background

In vitro pharmacology of ligands is typically assessed using a variety of molecular assays based on predetermined molecular events in living cells. Many ligands including opioid ligands pose the ability to bind more than one receptor, and can also provide distinct operational bias to activate a specific receptor. Generating an integrative overview of the binding and functional selectivity of ligands for a receptor family is a critical but difficult step in drug discovery and development. Here we applied a newly developed label-free integrative pharmacology on-target (iPOT) approach to systematically survey the selectivity of a library of fifty-five opioid ligands against the opioid receptor family. All ligands were interrogated using dynamic mass redistribution (DMR) ass

SUBMITTER: Morse M 

PROVIDER: S-EPMC3602246 | biostudies-literature | 2013 Mar

REPOSITORIES: biostudies-literature