Protease substrates

Ultra-high-specificity enzyme substrates:  Artificial enzyme substrates (protease and kinase substrate peptides, etc.) have been the key to many advances in modern biology and biotechnology.  Yet, useful as they are, many of these substrates have sub-optimal specificity.  There is too much cross-reaction with non-target enzymes.  This makes the analysis of complex biochemical pathways difficult.  It makes the creation of proteomic microarrays for complex enzymatic pathways nearly impossible.

Molecular Pathways has devised generalized methods for rapidly developing new, ultra-high-specificity, enzyme substrates patent 7,291,698, (a CIP, 11/872,012 which covers both enzyme substrates and enzyme inhibitors, is currently pending).  These ultra-high-specificity substrates may be used for improved proteomic microarrays, traditional microwell assays, or any application where improved specificity is desired. 

 
High specificity substrates

Diagram showing a matrix metalloprotein artifical peptide substrate (RPFS-MIMG) and Molecular Pathway's proprietary "steric blocker" groups (blue chains).    

These "steric blocker" groups extend beyond the MMP-3 enzyme's active site.  They prevent some MMP's from getting access to the substrate, and thus increase specificity

High specificity inhibitors:

These same concepts can also be used to produce higher specificity enzyme inhibitors, which could potentially be useful for higher specificity drugs and drug candidates.  Such inhibitors might exhibit fewer unwanted side effects.  This application is pending.

 A PowerPoint presentation with animated graphics, illustrating the concept, can be downloaded here.

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