Septerna 250 East Grand Avenue South San Francisco, CA 94080
Releasing the Full
Potential of GPCRs.
The GPCR Superfamily Has Yielded More Than 700 Drugs Across All Major Therapeutic Areas, Yet Vast Potential for New Medicines Remains.
Ubiquitous
GPCRs encompass the largest family of receptors and regulate nearly all physiological processes in 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
Our ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur Science
Our ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur ScienceOur Science
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 significantly 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 fundamental 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 all of the latest drug discovery tools that have previously been elusive for GPCRs because these proteins could not be isolated in functional form.
Septerna’s Native Complexes, enabled screening of vast chemical space (billions of compounds) and rapid solution of GPCR-ligand structures to enable true 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 Cryo-electron microscopy.
GPCR In Silico Screening
Using our structures to find new and better molecules through in silico approaches.
Join Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our Team
Join Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our TeamJoin Our Team
Join Our Growing
Team of Experts.
