Compugen Ltd. (NASDAQ: CGEN)
announced today the development and validation of its Intracellular Drug
Delivery (IDD) discovery platform for identification of cell penetrating
peptides. Compugen also announced that as part of the validation process
for the new platform, more than twenty novel peptides, predicted and
selected in silico, demonstrated the predicted cell penetrating
properties in initial experimental validation studies.
The delivery of biological molecules across selectively permeable cell
membranes and into the cells represents a major challenge for the
pharmaceutical industry. Furthermore, important classes of biological
drugs now under development, such as therapeutic peptides and siRNA,
need to enter the cell to be effective. Since most are unlikely to cross
the surrounding protective membranes of cells on their own, they will
require some type of delivery methodology. Cell penetrating peptides
offer the opportunity to provide the required intracellular targeting of
therapy, either by delivery of a therapeutic molecule as “cargo”, or by
the peptide itself.
Compugen’s newly developed Intracellular Drug Delivery discovery
platform enables the in silico identification of novel peptide
sequences that are predicted to have the potential to penetrate the cell
membrane. This new platform consists of various components from
Compugen’s existing computational biology infrastructure and a series of
proprietary machine learning algorithms specifically designed for this
platform. In a validation run of the platform, a number of peptides
having various physico-chemical properties potentially relevant for
different specific uses were predicted and experimentally evaluated.
Their ability to penetrate into cells was assessed by two independent
well-accepted in-vitro assay systems. In these evaluations, more than
twenty of these peptides were shown to possess cell penetrating activity
both by visual image analysis through confocal microscopy and
quantitative measures performed by flow cytometry analysis.
The last two decades have seen an increasing research interest in cell
membrane penetration and the discovery of various cell penetrating
peptides. In addition, the potential “cargo-carrying” capability of
certain of these known cell penetrating peptides has been demonstrated
in the lab by various experimental techniques; however, this capability
was only recently introduced to the clinic. Looking to the future, it is
forecasted that the availability of a much wider portfolio of cell
penetrating peptides with improved properties will be required in order
for this delivery methodology to meet the needs of the large number of
biological molecules now being evaluated industry wide for therapeutic
purposes. In this regard, Compugen intends to utilize its IDD platform
to create a library of cell penetrating peptides with properties
specific to different cargos and/or tissues.
In addition to the substantial opportunity represented by “therapeutic
cargo-carrying”, Compugen intends to integrate its Intracellular Drug
Delivery discovery platform with its other in silico therapeutic
peptide discovery capabilities, such as the DAC Blockers platform, in
order to create dual function peptides. These dual function peptides
will be designed to both penetrate the cell membrane, and provide the
required therapeutic intervention.
Zurit Levine, PhD, Compugen’s vice president of research and development
stated, “The efficient intracellular delivery of therapeutic molecules
is already presenting a hurdle for the biopharma industry, and will only
become more of a problem with the advancement of intracellular target
based therapeutic technologies such as RNAi, peptides and other classes
of biological molecules. We expect our Intracellular Drug Delivery
discovery platform to play a key role in both meeting this challenge and
providing the potential for dual function peptides thereby contributing
to a new and fruitful era of intracellular approaches to therapy.”
Anat Cohen-Dayag, PhD, Compugen’s president and CEO added, “The use of
peptides for human therapy is one of the fastest growing segments of
pharmaceuticals. Therefore the predictive discovery of peptides for
important therapeutic needs has been a focus of our research efforts for
the past few years and we are extremely pleased by our continued
broadening and deepening capabilities in peptide discovery. In addition
to the cell penetrating peptide platform being announced today, we
previously announced validated platforms for the predictive discovery of
peptide ligands for GPCRs - which are by far the largest family of
receptors for drugs, peptides that block proteins from disease
associated conformations, viral peptides for human diseases and
therapeutic peptides in various fields of therapy. We have no doubt that
our widely applicable peptide discovery capabilities are unique in our
industry.”
Liver cell aging can trigger multi-organ failure