Our Platform
Native Complex Platform™
The Platform
Septerna is a clinical-stage biotechnology company powered by our proprietary Native Complex Platform™
The Opportunity
GPCRs are Important for Cellular Signaling and Crucial Regulators of Normal Human Physiology
G protein-coupled receptors (GPCRs) represent the largest and most diverse family of cell membrane receptors, with hundreds of different GPCRs regulating physiological processes in nearly every organ system of the human body. They have been the most productive target class in drug discovery history, accounting for approximately one-third of all FDA-approved drugs. However, around 75% of potential GPCR therapeutic targets remain undrugged, representing a substantial untapped opportunity for future drug discovery. At Septerna, we are pioneering new technologies aimed at unlocking previously difficult-to-drug GPCRs.
Our Technology
Septerna’s Native Complex Platform™ Enables New Approaches to GPCR Drug Discovery
We have developed proprietary technologies to isolate, purify, and reconstitute GPCRs outside of cells into complexes with ligands, transducer proteins, and lipid bilayers which mimic cell membranes. We call these reconstituted assemblies Native Complexes because they replicate the natural structure, function, and dynamics of GPCRs in purified biochemical formats.
Our Native Complex Platform™ is powered by a suite of tools and technologies that have been optimized and integrated into proprietary, industrialized workflows. These include workflows for rapid determination of high-resolution 3D GPCR structures using cryogenic electron microscopy and workflows to screen billions of candidate molecules with both ultra-large-scale computational screens and databases and biochemical screens utilizing DNA-encoded libraries.
Drug Discovery
The Native Complex Platform™ Powers the Discovery and Optimization of Drug Candidates
Our Native Complex Platform™ is designed to enable us to target specific GPCRs, uncover novel binding pockets for validated receptors, and pursue a wide spectrum of pharmacologies, including agonists (which activate GPCR signaling), antagonists (which inhibit GPCR signaling), and allosteric modulators (which either increase or decrease the degree of GPCR activation by endogenous ligands), to affect GPCR signaling in different ways to achieve desired therapeutic effects.
High-resolution Native Complex GPCR structures are used to reveal previously unknown binding pockets, provide novel insights into mechanisms for GPCR modulation with small molecules, and drive rapid and iterative structure-based drug design and optimization cycles toward the discovery of new drug candidates.