Integral Molecular Expands Its Epitope Mapping Platform to Identify Small Molecule Binding Sites on Multipass Membrane Proteins

Integral Molecular, the industry leader in the expression and characterization of multipass membrane proteins, has expanded its mapping capabilities to include small molecules. This was achieved using Integral Molecular's Shotgun Mutagenesis platform, now the leading industry technology for understanding how antibodies interact with complex membrane proteins, with over 500 epitopes mapped at a >95% success rate. By combining this platform with its functional analysis capabilities, Integral Molecular has now extended this mapping capability to small molecules, which comprise 50% of drugs in development.

A recent study, published by Integral Molecular in Scientific Reports (Thomas et al., 2017), identified the precise binding sites for four different small molecules that bind to a human GPCR protein (TAS2R16). Small molecule binding sites are usually very difficult to map in the absence of protein co-crystal structures, as is the case for TAS2R16 and most other multipass membrane proteins. This study extends similar work that Integral Molecular has completed internally and for partners, mapping small molecule drug binding sites on GPCRs and other multi-pass membrane proteins, including mapping the binding site of a peptide on the GPCR CXCR4 (Wescott, et al, 2016 PNAS).

"This method for identifying individual amino acids that are critical for binding or function in structurally complex proteins is particularly valuable since it does not require traditional structural information," said Dr. Joseph Rucker, VP of Research and Development at Integral Molecular. "The small molecules we mapped are also very low affinity, making them even more challenging for more traditional analytical techniques. With this new ability, our mapping expertise now covers antibodies, peptides, and small molecules."

About Integral Molecular

Integral Molecular is a research-driven biotechnology company creating innovative technologies and a pipeline of therapeutic antibodies against under-exploited membrane protein targets, including GPCRs, ion channels, transporters, immuno-oncology targets, and viral envelope proteins. Integral Molecular has a long-standing interest in the structure and function of taste receptors such as TAS2R16, which are important for taste but also have specific roles in numerous non-taste physiological processes. The company utilizes its Shotgun Mutagenesis Epitope Mapping platform technology to rapidly map binding sites on structurally complex targets. Integral Molecular offers Epitope Mapping services on a fee-for-service basis, for mapping antibody, ligand, or small molecule binding sites.

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