Saquinavir: From HIV to COVID-19 and Cancer Treatment

Saquinavir was the first protease inhibitor developed for HIV therapy, and it changed the standard of treatment for this disease to a combination of drugs that ultimately led to increased survival of this otherwise deadly condition. Inhibiting the HIV protease impedes the virus from maturing and rep...

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Main Authors: Mariana Pereira, Nuno Vale
Format: Article
Language:English
Published: MDPI AG 2022-07-01
Series:Biomolecules
Subjects:
Online Access:https://www.mdpi.com/2218-273X/12/7/944
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author Mariana Pereira
Nuno Vale
author_facet Mariana Pereira
Nuno Vale
author_sort Mariana Pereira
collection DOAJ
description Saquinavir was the first protease inhibitor developed for HIV therapy, and it changed the standard of treatment for this disease to a combination of drugs that ultimately led to increased survival of this otherwise deadly condition. Inhibiting the HIV protease impedes the virus from maturing and replicating. With this in mind, since the start of the COVID-19 outbreak, the research for already approved drugs (mainly antivirals) to repurpose for treatment of this disease has increased. Among the drugs tested, saquinavir showed promise in silico and in vitro in the inhibition of the SARS-CoV-2 main protease (3CLpro). Another field for saquinavir repurposing has been in anticancer treatment, in which it has shown effects in vitro and in vivo in several types of cancer, from Kaposi carcinoma to neuroblastoma, demonstrating cytotoxicity, apoptosis, inhibition of cell invasion, and improvement of radiosensibility of cancer cells. Despite the lack of follow-up in clinical trials for cancer use, there has been a renewed interest in this drug recently due to COVID-19, which shows similar pharmacological pathways and has developed superior in silico models that can be translated to oncologic research. This could help further testing and future approval of saquinavir repurposing for cancer treatment.
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spelling doaj.art-2182f35398dd4b8fb2ed6fb5441d80642023-11-30T22:52:19ZengMDPI AGBiomolecules2218-273X2022-07-0112794410.3390/biom12070944Saquinavir: From HIV to COVID-19 and Cancer TreatmentMariana Pereira0Nuno Vale1OncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Doutor Plácido da Costa, 4200-450 Porto, PortugalOncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Doutor Plácido da Costa, 4200-450 Porto, PortugalSaquinavir was the first protease inhibitor developed for HIV therapy, and it changed the standard of treatment for this disease to a combination of drugs that ultimately led to increased survival of this otherwise deadly condition. Inhibiting the HIV protease impedes the virus from maturing and replicating. With this in mind, since the start of the COVID-19 outbreak, the research for already approved drugs (mainly antivirals) to repurpose for treatment of this disease has increased. Among the drugs tested, saquinavir showed promise in silico and in vitro in the inhibition of the SARS-CoV-2 main protease (3CLpro). Another field for saquinavir repurposing has been in anticancer treatment, in which it has shown effects in vitro and in vivo in several types of cancer, from Kaposi carcinoma to neuroblastoma, demonstrating cytotoxicity, apoptosis, inhibition of cell invasion, and improvement of radiosensibility of cancer cells. Despite the lack of follow-up in clinical trials for cancer use, there has been a renewed interest in this drug recently due to COVID-19, which shows similar pharmacological pathways and has developed superior in silico models that can be translated to oncologic research. This could help further testing and future approval of saquinavir repurposing for cancer treatment.https://www.mdpi.com/2218-273X/12/7/944saquinavirdrug repurposingHIVCOVID-19cancer
spellingShingle Mariana Pereira
Nuno Vale
Saquinavir: From HIV to COVID-19 and Cancer Treatment
Biomolecules
saquinavir
drug repurposing
HIV
COVID-19
cancer
title Saquinavir: From HIV to COVID-19 and Cancer Treatment
title_full Saquinavir: From HIV to COVID-19 and Cancer Treatment
title_fullStr Saquinavir: From HIV to COVID-19 and Cancer Treatment
title_full_unstemmed Saquinavir: From HIV to COVID-19 and Cancer Treatment
title_short Saquinavir: From HIV to COVID-19 and Cancer Treatment
title_sort saquinavir from hiv to covid 19 and cancer treatment
topic saquinavir
drug repurposing
HIV
COVID-19
cancer
url https://www.mdpi.com/2218-273X/12/7/944
work_keys_str_mv AT marianapereira saquinavirfromhivtocovid19andcancertreatment
AT nunovale saquinavirfromhivtocovid19andcancertreatment