No Need To Wait For Big Pharma’s Anti-Covid Protease-Inhibiting Drug

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by Bill Sardi, Lew Rockwell:

Just to steer clear of online censors and trolling bots that detect “misinformation,” and to avoid potential litigation, let’s just report a major manufacturer of vaccines and drugs now announces it will introduce an oral medicine that impedes the replication of COVID-19 coronavirus via enzyme inhibition.  The new drug will augment but not replace vaccines. Online links to the new drug won’t be provided here because the pharmaceutical company doesn’t need any free publicity.  You will realize why after reading the rest of this report.

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The enzyme is protease.  Proteases are enzymes that help to synthesize proteins in the body.  In regard to COVID-19, protease facilitates the replication of viruses.  Inhibit protease, diminish the threat of severe COVID coronavirus infection.

The drug is specifically intended for non-hospitalized, symptomatic adults who have a confirmed COVID-19 infection and are not believed to be at increased risk for progression to severe illness.  A controlled study is underway.

Should the public hold their breath for this medicine?  Does this drug supplant vaccination?

How protease inhibitors work

Protease inhibitors have a long history of use with a good safety profile.  Protease cuts chains of proteins to produce subunits that allow the virus to replicate. Protease inhibitors interfere with this protein-cutting process.  Protease inhibitors have made history in the battle against HIV.  Furthermore, protease inhibitors work with all variants of a virus.

Drug targets: obfuscation

The drug is said to target the main protease enzyme, – Mpro, of COVID-19.  Mpro is intentionally vague and stands for “main protease.”

Mpro is just a way of hiding the real protease enzyme (3C-like protease, formerly C30 endopeptidase) that facilitates the replication of viruses inside living cells.  Recall from Virology 101 that viruses can’t replicate until they enter the genetic machinery of a living cell.

Just to confuse everyone, so they won’t put two-and-two together and figure out this drug can be duplicated with vitamin and herbal remedies, alternative names are used for Mpro, such as 3CLpro, 3C-like protease, coronavirus 3C-like protease, Mpro, SARS 3C-like protease, SARS coronavirus 3CL protease, SARS coronavirus main peptidase, SARS coronavirus main protease, (this is the “guess the name of the enzyme” game), SARS-CoV 3CLpro enzyme, SARS-CoV main protease, SARS-CoV Mpro, and severe acute respiratory syndrome coronavirus main protease.

Papain-like enzyme, (PLpro), is another protein that is crucial in the viral replication process.  PLpro is said to be the Achilles’ heel of COVID-19.

An alternative pathway for viral entry into cells is TMPRSS2 (trans-membrane protease serine 2) that primes the spike protein on the surface of coronaviruses, thus facilitating the entry of the virus into cells.  A drug trial failed to demonstrate inhibition of this TMPRSS2 pathway.  However, fisetin, a strawberry molecule, was found to inhibit TMPRSS2.

Natural molecules abound

report in Nature magazine notes that pharmacologists assayed over 10,000 compounds, including natural and synthetic drug molecules, and found six that significantly inhibited replication of COVID-19.

Ebselen, a sulfur-based drug that mimics a natural antioxidant (glutathione peroxidase) prevailed in their screening of molecules to counter Mpro.

Vitamin E + the trace mineral selenium produces glutathione peroxidase, an internal antioxidant enzyme.

Ebselen (vitamin E + selenium) inhibits PLpro like it does Mpro.  Ebselen is an extremely safe drug.  Most people who take multivitamins get enough vitamin E and selenium to make glutathione peroxidase.

Fisetin: the strawberry molecule that clobbers COVID

A remarkable study conducted by University of Minnesota researchers showed the strawberry molecule fisetin as a protease inhibitor not only was effective against coronavirus-related mortality in lab animals, but it helped to abolish old senescent cells that render older adults vulnerable to viruses.

In one of their studies, 100% of old mice died within a 2-week period vs. only 36% of fisetin-treated male mice.  Targeting drivers of aging resulted in longer survival of lab animals.

According to these university-based researchers, writing in Science magazine, even if 95% effectiveness vaccine rate in health populations in borne out in elderly nursing home patients, still at least 1 out of 20 vaccinated elderly people can anticipate becoming ill due to COVID-19 and will need anti-senescent/ anti-COVID medication.  Fisetin may be very valuable for older age adults.  Fisetin is sold as a dietary supplement in health shops and online.

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