A Rational Strategy for Transitioning Well Characterized Biology into Lead Stage Molecules
 
 

Protein-protein interactions are dominated by complex induced fit interactions that are further complicated by multiple touch points. These fluid interaction interfaces have frustrated standard screening techniques, and many clinically promising targets have been eventually labeled as intractable. Using high speed in silico denaturing and virtual binding algorithms, Serometrix is able to identify these critical "hot spots" and characterize the biochemistry of these complex interactions. In addition, the Serometrix drug discovery process provides lead stage agonists and/or antagonists that provide superior preclinical starting points for our partners.

 
 

 

 

 

In addition to great science, Serometrix has pioneered an early stage collaborative business model that pairs small biotech innovation with industry development capabilities. Serometrix works iteratively with its partners to provide an exclusive family of targeted lead stage molecules for preclinical drug development. These molecules, reverse engineered from natural biological processes discovered at these protein-protein interfaces, offer high quality templates for drug development.

Our process follows a gated development approach as outlined below:

Milestone 1 - IN SILICO DISCOVERY
Starting with protein interactions with known disease modifying potential, Serometrix applies its Peptimer™ Discovery Platform to identify interaction hot spots and identifies initial wild type ligands to be used as starting compounds. In addition, the platform identifies other proteins with potential for cross reactivity which may result in off target affects.

Milestone 2 - IN VITRO EXPERIMENTAL CONFIRMATION
In this phase, wild type ligands are synthesized and tested using in vitro binding and/or functional assays to quantify activity and correlate with in silico results. Serometrix seeks collaborative partners that possess validated in vitro assays that can support the iterative SARs process.

Milestone 3 - SARS OPTIMIZATION
This multi-step process analyzes the results of the wild type ligands to determine chemical modifications that can enhance binding activity and/or provide a preliminary understanding of the structure activity relationship at the interaction interface. This process is repeated until a family of compounds demonstrate efficacy at physiological concentrations. This method also provides a very rapid way to understand and quantify the complex induced fit biology at the interface.

Milestone 4 - IN VIVO CONFIRMATION
These assays are very program dependent. This phase is best designed, developed, and executed in close collaboration with a well-aligned strategic partner that has pre-established in vivo models.

Milestone 5 - LEAD STAGE MOLECULES
Success in Milestone 4 leads to a family of lead stage molecules with the specific activity, a further enhanced understanding of the underlying biology, and a highly refined intellectual property portfolio. This "family of compounds" approach provides advantages for IP protection and helps reduce late stage attrition. The underlying know how and IP may also be used to dramatically improve HTS methods, hit rates, and time to clinic.

Milestone 6 - PRECLINICAL & CLINICAL DRUG DEVELOPMENT
These families of compounds and their derivatives provide exclusive license opportunities for our development partners, which then move through industry standard preclinical development stages.

 

 
For more information on our early stage programs available for partnering,
visit the Partnering section of our website.