Nanotechnology – Peixuan Guo, Dan Shu, University of Kentucky Research Foundation
Abstract for “Method to design compounds and compositions that are useful for targeting high-stoichiometric complexes for treating conditions, including the treatment of bacteria and viruses which have acquired drug resistance.”
“A method for identifying multi-subunit biocomplex drug targets is described. This method involves identifying a target capable of performing a biological function. The target must contain one or more components. A minimum number of these subunits must be inactivated to inhibit this biological function. This method involves selecting a drug that binds to the specific subunits of each subunit with a target probability. This method uses a binomial distribution to describe the relationship between the inhibition efficiency of the drug, and the total number of subunits. The inhibition efficiency is a probability that the delivered drug will block the biological function. This method involves empirically confirming the relationship by using an experimental target. The drug is administered to the target in order to treat multi-drug resistant diseases.
Background for “Method to design compounds and compositions that are useful for targeting high-stoichiometric complexes for treating conditions, including the treatment of bacteria and viruses which have acquired drug resistance.”
“The currently-disclosed subject material meets some or all the above-identified requirements, as will be evident to those with ordinary skill in art after a review of this document.”
“Disclosed is a method of designing compounds that are useful in treating conditions that can easily be treated with high stoichiometric complicatedes. This is useful for, for example, designing drugs against viruses, bacteria and cancers that have acquired drug resistance.”
“Phi29 DNA-packaging Motor components were used to validate the method’s suitability for use with targets of different Stoichiometries. Yang Hui’s Triangle was used to measure virion assembly efficiency.
“( p + q ) Z = ? M = 0 Z ( Z M?) p Z -? q M?,nwhere Z=stoichiometry and M=drugged units in each biocomplex. p and Q represent the respective fractions of drugged or non-drugged population subunits.
“Inhibition efficiency is governed by a power function, as reported herein. If K=1 is the number of drugged subunits that block the function, the fraction of uninhibited biocomplex equals Qz. Toxicology has a multiplicative effect upon inhibition. The highest inhibition effect was observed in targets tested with 1000 subunits. This was followed by targets that had six or one subunit. Z=6 was the threshold for complete inhibition of virus replication.
“The stoichiometry or nano-machine of the target components determines drug inhibition potency,” according to the disclosures herein. The power function of the target biocomplex’s stoichiometry determines the inhibition effect.
Summary for “Method to design compounds and compositions that are useful for targeting high-stoichiometric complexes for treating conditions, including the treatment of bacteria and viruses which have acquired drug resistance.”
“The currently-disclosed subject material meets some or all the above-identified requirements, as will be evident to those with ordinary skill in art after a review of this document.”
“Disclosed is a method of designing compounds that are useful in treating conditions that can easily be treated with high stoichiometric complicatedes. This is useful for, for example, designing drugs against viruses, bacteria and cancers that have acquired drug resistance.”
“Phi29 DNA-packaging Motor components were used to validate the method’s suitability for use with targets of different Stoichiometries. Yang Hui’s Triangle was used to measure virion assembly efficiency.
“( p + q ) Z = ? M = 0 Z ( Z M?) p Z -? q M?,nwhere Z=stoichiometry and M=drugged units in each biocomplex. p and Q represent the respective fractions of drugged or non-drugged population subunits.
“Inhibition efficiency is governed by a power function, as reported herein. If K=1 is the number of drugged subunits that block the function, the fraction of uninhibited biocomplex equals Qz. Toxicology has a multiplicative effect upon inhibition. The highest inhibition effect was observed in targets tested with 1000 subunits. This was followed by targets that had six or one subunit. Z=6 was the threshold for complete inhibition of virus replication.
“The stoichiometry or nano-machine of the target components determines drug inhibition potency,” according to the disclosures herein. The power function of the target biocomplex’s stoichiometry determines the inhibition effect.
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