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Sorrento Announces Publication of a Series of Novel SARS-CoV-2 Main Protease (MPRO) Inhibitors for Potential Treatment of COVID-19 Patients Infected With SARS-CoV-2 Variants Of Concern, Including Omicron

  • A representative of novel MPro inhibitor series, MPI8, dually inhibits MPro and cathepsin L, a key viral entry enzyme, with high potency and selectivity.
  • Other analogs of the series have been evaluated by Sorrento to develop an oral antiviral drug for treatment of patients infected with existing and emerging SARS-CoV-2 variants of concern, including Omicron.
  • A promising candidate of the series with unique features distinguished from SARS-CoV-2 MPro inhibitors published by others has been systematically evaluated and advanced to late stage of pre-clinical phase.

SAN DIEGO, Dec. 05, 2021 (GLOBE NEWSWIRE) -- Sorrento Therapeutics, Inc. (Nasdaq: SRNE, “Sorrento”) today announced the peer-reviewed publication of a series of novel SARS-CoV-2 MPro inhibitors with potent activities for both MPro and cathepsin L, a key host enzyme for SARS-CoV-2 entry into host cells, authored by Dr. Wenshe Ray Liu, professor at Texas A&M University.

The full manuscript is available at: https://pubmed.ncbi.nlm.nih.gov/34242492/

SARS-CoV-2 main protease (MPro) is a key enzyme for the viral life cycle including virus entry, replication and packaging. MPro is highly conserved in all discovered SARS CoV-2 variants and is identified as a critical target for developing broad-spectrum antiviral drugs. In addition, experimental evidence has shown that certain host proteases prime the SARS-CoV-2 spike protein for viral packaging, interactions with ACE2, and viral entry into the host. These include two serine proteases, furin and transmembrane protease serine 2 (TMPRSS2) and a cysteine protease cathepsin L. Small molecule medications that inhibit furin, TMPRSS2 and cathepsin L have shown efficacy in inhibiting SARS-CoV-2 replication. In the publication, a representative analog of the series, MPI8, demonstrated dual inhibition of MPro and cathepsin L with high potency and selectivity (IC50 values for MPro and cathepsin L are 105 nM and 1.2 nM, respectively). Sorrento has collaborated with Professor Liu’s lab at Texas A&M University to evaluate analogs in the series to develop an oral anti-COVID drug. A promising analog with features distinguished from current reported SARS-CoV-2 MPro inhibitors has been systematically evaluated and advanced to a late stage of pre-clinical phase. “We are pleased to work with Prof. Liu’s group at Texas A&M University to develop a more effective oral MPro inhibitor to meet the urgent need for treatment of COVID-19 patients infected with existing and emerging variants. The oral MPro inhibitor together with Sorrento’s other ongoing therapeutic intervention approaches reflect our efforts to create a ‘mutation-agnostic’ global anti-COVID strategy to combat COVID-19 variants of concern, including the emerging Omicron variant,” stated Dr. Henry Ji, Chairman and CEO of Sorrento.

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05.12.2021, 20:28  |  141   |   |   

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Sorrento Announces Publication of a Series of Novel SARS-CoV-2 Main Protease (MPRO) Inhibitors for Potential Treatment of COVID-19 Patients Infected With SARS-CoV-2 Variants Of Concern, Including Omicron A representative of novel MPro inhibitor series, MPI8, dually inhibits MPro and cathepsin L, a key viral entry enzyme, with high potency and selectivity.Other analogs of the series have been evaluated by Sorrento to develop an oral antiviral drug …

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