Drug Discovery

About GM6
For drug development purposes, a drug target smaller than 33 amino acids is desirable. Within the original MNTF 33mer sequence, Genervon further identified nine active sites and multiple drug targets. In vitro and in vivo experiments have confirmed that all identified targets have statistically similar biological effects with variations as the 33mer. Genervon discovered MNTF, a novel patented family of 9 human master regulators of the nervous system highly expressed during week 9 of embryonic development. These Master Regulators are potent disease modification drug candidates modulating many pathways including inflammation, apoptotic, hypoxia etc. GM600, one of the master regulators is the chosen drug candidate because its size was proven to be able to penetrate the crucial blood-brain barrier.

GM6 has all the advantages of a peptide-based drug: very high potency and activity, low toxicity, minimum drug-to-drug interaction, low accumulation in tissues (i.e., a short half-life), extremely high specificity, and little to no unspecific binding to molecular structures other than the desired targets. GM6 is small enough that it does not have the disadvantages of large peptides in terms of stability, solubility, mutagenicity, immunogenicity, or the high cost of manufacturing through transgenic or recombinant methods.

From Function to Pathways: 1,600 Genes Activated
Recent genomic, proteomic, and systems biology studies suggest that CNS disorders and diseases implicate a highly complex, multi-factorial process that involves the interplay of many non-dominant effectors in an interwoven dynamic network. That expounds the futile efforts of single action drugs.

MNTF is a specific, functional, regulatory, endogenous peptide for the protection of the nervous system from disorders and diseases including neurovascular and neurodegenerative diseases. Having discovered MNTF by its function, Genervon used DNA micro-array analysis to find the genes that are activated by its analogue GM6. That analysis indicated that GM6 up or down regulates, by at least two fold, more than 1,600 genes. Many of the modulated genes are related to nervous system disorders and diseases, and neurodegenerative diseases, including those in command of pathways for apoptosis, oxidative stress, inflammation, lipid and immune response.

These analyses showed that GM6 activates genes involved in neurogenesis, neural development, neuronal signaling plus many specific biological functions. GM6 modulated significantly genes through many important pathways.

GM6’s coordinated modulation of such a large number of genes suggests a master-regulator that effects on this extremely intricate network of disease-related pathways.


 
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