Discovery Engine

Isoforms of PKC are strongly conserved, especially in their catalytic and ATP-binding regions, making selectivity problematic. Further, the full crystal structure of PKC has not been determined. 

To overcome this difficulty, the Company has developed a proprietary series of unique, dynamic computer models of select PKC isoforms, providing PharmaGap researchers with an in silico “toolkit”. This allows for targeting of unique moieties on each PKC isoform, thereby conferring isoform selectivity into PharmaGap’s drug design process.

Careful, methodical attention is expended upfront by way of computer modeling and careful analysis of the molecular structure of the PKC target of interest to design the Company’s drug candidates. In this way, PharmaGap researchers look to design compounds for pre-clinical testing with the desired potency and safety required for a successful drug therapeutic.

The computer modeling techniques used to develop the Company’s lead drug candidate PhGα1 support the Company’s design of other peptidic and small molecule modulators of additional PKC isoforms of clinical interest – the PharmaGap pipeline.  The Company’s use of proprietary computer models of PKC form the basis of its competitive advantage, patent estate and rich pipeline of drug compounds.

Representative image of PKC molecule created by PharmaGap researchers

(Note: this image was not used in the design process for PhGα1).