When
Presenter
Dr. Chris Apostol
2021 Ph.D. from CBC, presently at SRI International, Menlo Park, CA.
Abstract
We recently reported a new mega-high-throughput screening technology that enables the rapid discovery and production of non-natural peptide libraries with potent binding against biological targets such as K-Ras, IL-6, and TNF-alpha. The screening method utilizes SRI’s proprietary Fiber-optic Array Scanning Technology (FAST) to identify binding interactions between one-bead-one-compound (OBOC) libraries and fluorescently labeled targets. With the flexibility of this platform, we have expanded the chemical space of these libraries beyond standard amino acid building blocks. Here we present a new class of non-natural peptide-mimetics called “Techneins”, which combine features of small molecule drugs with peptide backbones to produce foldamers with robust stability and tight binding towards their targets. Techneins feature dihydroisoquinoline (Dhq) monomers, which are a privileged scaffold for small molecule drugs, decorated with chemically diverse functional groups to promote binding interactions and promote 3D folding. We present case studies highlighting the application of Techneins as potential therapeutics and diagnostic tools for SARS-CoV-2 and as medical countermeasures combating the opioid crisis.
Short Bio
After starting research with PACAP-derived glycopeptide drug candidates Chris left the Polt Group to work with Dr. Nathan Collins at SRI. Nathan was a post-doc in Prof. Victor Hruby’s lab, and married another post-doc in the group, Maguy Letulle some time ago.
Here is a video that describes some related technology that was developed at SRI: Nathan Collins talks about how the SynFini automated chemistry platform is accelerating drug development and discovery.
Hosted by: Dr. Robin Polt