This is the first step towards understanding the biological pathways of historically undruggable targets like MYC, unlocking new opportunities for future cancer therapies.
SAN DIEGO (PRWEB) August 07, 2018
Nanomedical Diagnostics, leading manufacturer of graphene biosensors that accelerate pharmaceutical and biotherapeutics development, announces a new publication titled, “Synthetic Molecules for Disruption of the Myc Protein-Protein Interface” in the Elsevier journal Bioorganic & Medicinal Chemistry. The paper prominently features use of Agile R100, described as a “field-effect transistor (Bio-FET) platform,” to produce a new lead compound of significantly increased in vivo stability and solubility.
MYC is a prominent regulator gene that is a recognized actor in cancer initiation and maintenance, and thus a promising target for anti-cancer drugs. An intrinsically disordered protein, MYC can bind nonspecifically to and aggregate on dextran surfaces, making small molecule interaction studies for this “undruggable target” difficult to perform using traditional platforms. Agile R100 biosensors employ graphene surfaces that reduce nonspecific binding and enable direct binding measurements of challenging proteins such as MYC.
The paper describes the development of a screening platform incorporating Agile R100 as part of a blind structure-activity-relationship (SAR) study. “Our first attempts to characterize the interactions of MYC by surface plasmon resonance (SPR) gave us too high of a background due to non-specific interactions of the protein with the chip surface,” says Dr. Nicholas Jacob, lead author of the study. “In contrast, Agile R100’s graphene surface proved significantly less prone to these nonspecific interactions, and we were able to achieve a higher signal-to-noise ratio. The system allowed us to measure affinities for small molecule interactions with MYC in a label-free manner where other standard methods had failed.”
In the study, binding data from Agile R100 correlated well with data from in vivo microtumor formation inhibition assays using chicken embryo fibroblasts (CEF), as opposed to SPR data, which did not. The publication goes on to reference additional advantages of Agile R100: The system has a much lower limit of detection than SPR or isothermal calorimetry (ITC), and its site-specific functionalization decreased aggregation on the chip which further reduced nonspecific noise.
Agile R100 is a novel optics-free binding assay platform for the kinetic characterization of biomolecular interactions. As a graphene biosensor, Agile R100 monitors changes in electrical conductivity to gain sensitive label-free measurements, enabling real-time quantitative analysis of difficult-to-study molecules. “Agile R100 uses a novel electrical sensing mechanism that enables researchers to characterize difficult, disordered targets with less time and resources,” says Nanomedical Diagnostics CEO, Ross Bundy. “This is the first step towards understanding the biological pathways of historically undruggable targets like MYC, unlocking new opportunities for future cancer therapies.”
About Nanomedical Diagnostics
Nanomedical Diagnostics (“Nanomed”) is a life science company based in San Diego, CA. Nanomed has developed a breakthrough electrical assay based on proprietary Field Effect Biosensing (FEB) technology that delivers sensitive label-free kinetic characterization of biomolecular interactions for accelerated drug discovery. As the world’s leading developer and manufacturer of next-generation graphene biosensors, Nanomed’s mission is to transform the healthcare industry with innovative new products that enable cutting-edge life science research, drug discovery applications, and portable diagnostic and health monitoring platforms.