Platform

Releasing the Full

Potential of GPCRs.

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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

  • Hundreds of GPCRs
  • Expressed on every cell in the body
  • Regulate function of all human organ systems

Productive

GPCRs have proven to be the most prolific class of drug targets for pharmaceutical R&D

  • 1/3 of all approved drugs target GPCRs
  • Treatments span all major therapeutic areas
  • Blockbuster drugs with combined annual revenue >$180B

Untapped

Significant unrealized potential remains, with drug discovery success to date limited to a small number of GPCR families

  • 80% of all GPCR drugs target just 6 GPCR subfamilies
  • >85% of potential therapeutic GPCR targets remain undrugged

 

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Our Science

Harnessing GPCRs in Their 
Native States to Power 
Drug Discovery

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GPCRs are highly complex and important targets for medicines

02

Septerna’s solution:
The Native Complex

03

Enabling modern drug discovery with the Native Complex Platform™

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01

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.

GPCRs are in all cells of the body and control important biological processes.
GPCRs sit in the cell membrane and couple to a G protein complex inside the cell.
Signals from outside the cell arrive in the form of receptor-specific ligands.
When the ligand binds its receptor, the receptor changes shape and becomes activated.
The G protein complex binds to the activated GPCR and itself becomes activated.
The activated complex dissociates from the receptor and sets off a signal transduction cascade inside the cell.
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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.

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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 Affinity Screening

Discovering new molecules by screening the Native Complex

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.

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