Septerna 250 East Grand Avenue South San Francisco, CA 94080
Unlocking the Full
Potential of GPCRs
The GPCR Superfamily Has Yielded ~500 Drugs Across All Major Therapeutic Areas, Yet Vast Potential for New Medicines Remains.
Ubiquitous
GPCRs encompass the largest family of receptors and regulate physiological processes in nearly every organ system of the human body
Productive
GPCRs have proven to be the most prolific class of drug targets for pharmaceutical R&D
Untapped
Significant unrealized potential remains, with drug discovery success to date limited to a small number of GPCR families
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Harnessing GPCRs in Their Native States to Power Drug Discovery
GPCR Complexity: Previously Inaccessible to Drug Discovery Approaches Which Rely on Purified Proteins
GPCRs are characterized by their seven transmembrane domains, and function in ternary complexes that form with extracellular ligands and intracellular transducer proteins. Extracellular ligand binding initiates intracellular signaling pathways which control many aspects of cell biology.
Each step in GPCR activation involves subtle conformational changes that have historically been challenging to reproduce outside of the cell, and this has limited the application of many enabling modern drug discovery technologies.
Septerna’s Solution: The Native Complex
GPCRs in Their Native States
Septerna’s scientists have developed the foundational technologies needed to isolate, purify and reconstitute full-length, properly folded GPCR proteins in ternary complexes with ligands and transducer proteins in a defined membrane lipid environment.
Septerna’s Native Complexes faithfully recapitulate the natural structure, function and dynamics of GPCRs outside of cells for the very first time. The Native Complexes are modular assemblies, and different transducer and ligand combinations can be used to construct multiple different states for each receptor.
Receptors are expressed and purified from cells grown in the laboratory.
Purified receptors are reconstituted in synthetic membranes and purified G proteins and ligands can be added to form a functional Native Complex.
Septerna has industrialized processes for creating Native Complexes.
Native Complexes can be systematically produced for a wide array of GPCRs.
Enabling the Full Repertoire of Modern Drug Discovery Technologies
Septerna’s unique platform now unlocks the potential to utilize the latest drug discovery tools that have previously been elusive for GPCRs because these proteins could not be isolated in functional forms outside of cells.
Septerna’s Native Complexes, enable screening of vast chemical space (billions of compounds) and rapid solution of GPCR-ligand structures to enable rapid and iterative structure-based drug design for the first time.
Drug Discovery Powered by
the Native Complex Platform™
GPCR Structural Biology:
Revealing how molecules change receptor function at the atomic level with Cryogenic electron microscopy.
GPCR In Silico Screening:
Using our structures to find new and better molecules through in silico approaches.
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