Enzymes in the time of COVID‐19: An overview about the effects in the human body, enzyme market, and perspectives for new drugs

Fé, Luana Xavier Soares Gomes Moura; Cipolatti, Eliane Pereira; Pinto, Martina Costa Cerqueira; Branco, Suema; Nogueira, Fábio César Sousa; Ortiz, Gisela Maria Dellamora; Pinheiro, Anderson S.; Manoel, Evelin Andrade

doi:10.1002/med.21919

Cited by 8 publications

(1 citation statement)

References 231 publications

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“…M protease (Mpro) and PL protease (PLpro), respectively known as nsp5 and nsp3, are essential enzymes in the virus replication cycle, representing a therapeutic target to prevent the success of the infection. They process the virus polyproteins into active proteins and differ from human proteases, promoting the lower toxicity of protease inhibitors [ 40 ]. Notably, nirmatrelvir (NM) is an oral protease inhibitor that is active by cleaving the 2 viral polyproteins; it is available in association with ritonavir ® , a strong cytochrome P450-3A4 inhibitor, that increases nirmatrelvir concentrations reducing the dose regimen and the side effects of the antiviral.…”

Section: Therapeutic Agents Approved In Covid-19 Therapymentioning

confidence: 99%

Overview of Antiviral Drug Therapy for COVID-19: Where Do We Stand?

et al. 2022

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The vaccine weapon has resulted in being essential in fighting the COVID-19 outbreak, but it is not fully preventing infection due to an alarming spreading of several identified variants of concern. In fact, the recent emergence of variants has pointed out how the SARS-CoV-2 pandemic still represents a global health threat. Moreover, oral antivirals also develop resistance, supporting the need to find new targets as therapeutic tools. However, cocktail therapy is useful to reduce drug resistance and maximize vaccination efficacy. Natural products and metal-drug-based treatments have also shown interesting antiviral activity, representing a valid contribution to counter COVID-19 outbreak. This report summarizes the available evidence which supports the use of approved drugs and further focuses on significant clinical trials that have investigated the safety and efficacy of repurposing drugs and new molecules in different COVID-19 phenotypes. To date, there are many individuals vulnerable to COVID-19 exhibiting severe symptoms, thus characterizing valid therapeutic strategies for better management of the disease is still a challenge.

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Section: Therapeutic Agents Approved In Covid-19 Therapymentioning

confidence: 99%

Overview of Antiviral Drug Therapy for COVID-19: Where Do We Stand?

et al. 2022

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Enzymes in the time of COVID‐19: An overview about the effects in the human body, enzyme market, and perspectives for new drugs

Fé

Cipolatti

Pinto

et al. 2022

Medicinal Research Reviews

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The rising pandemic caused by a coronavirus, resulted in a scientific quest to discover some effective treatments against its etiologic agent, the severe acute respiratory syndrome‐coronavirus 2 (SARS‐CoV‐2). This research represented a significant scientific landmark and resulted in many medical advances. However, efforts to understand the viral mechanism of action and how the human body machinery is subverted during the infection are still ongoing. Herein, we contributed to this field with this compilation of the roles of both viral and human enzymes in the context of SARS‐CoV‐2 infection. In this sense, this overview reports that proteases are vital for the infection to take place: from SARS‐CoV‐2 perspective, the main protease (M pro ) and papain‐like protease (PL pro ) are highlighted; from the human body, angiotensin‐converting enzyme‐2, transmembrane serine protease‐2, and cathepsins (CatB/L) are pointed out. In addition, the influence of the virus on other enzymes is reported as the JAK/STAT pathway and the levels of lipase, enzymes from the cholesterol metabolism pathway, amylase, aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase, and glyceraldehyde 3‐phosphate dehydrogenase are also be disturbed in SARS‐CoV‐2 infection. Finally, this paper discusses the importance of detailed enzymatic studies for future treatments against SARS‐CoV‐2, and how some issues related to the syndrome treatment can create opportunities in the biotechnological market of enzymes and the development of new drugs.

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1,2,3‐Triazole‐Based New Aurones as Anticancer Agents with the Capability to Target Extracellular Digestive Enzymes

Kumar,

Saroha,

Kumar

et al. 2024

ChemistrySelect

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This study involves the synthesis of a series of dimethyl substituted novel aurones, featuring 1,2,3‐triazole as an integral structure. All the newly synthesized compounds were thoroughly characterized using various spectroscopic tools and also subjected to computational analysis utilizing the DFT/B3LYP methodology, which involved the determination of frontier molecular orbital energy values and the computation of various quantum chemical parameters. Further their impact on cell viability and cytotoxic activity on the adenocarcinoma gastric cell line (AGS) was investigated using cell‐based MTT assay. Compounds 6d, 6o and 6p displayed significant cytotoxic activity, reducing cell viability to a greater extent with IC50 values of 9.74, 20.09, and 5.92 µM, respectively and even better than the standard chemotherapeutic drug leucovorin (IC50 = 30.8 µM). In addition, all the compounds were also screened for their extracellular enzymatic assay and through in vitro results compound 6n emerged as the efficient inhibitor of amylase (% inhibition = 51.92) and trypsin (% inhibition = 68.36), whereas an activation is observed for lipase (% activation = 269.48). In silico molecular docking was also conducted to assess the interactions between proteins and ligands, revealing the binding patterns of the synthesized compounds and the standard drug with receptor proteins.

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Enzymes in the time of COVID‐19: An overview about the effects in the human body, enzyme market, and perspectives for new drugs

Cited by 8 publications

References 231 publications

Overview of Antiviral Drug Therapy for COVID-19: Where Do We Stand?

Overview of Antiviral Drug Therapy for COVID-19: Where Do We Stand?

Enzymes in the time of COVID‐19: An overview about the effects in the human body, enzyme market, and perspectives for new drugs

1,2,3‐Triazole‐Based New Aurones as Anticancer Agents with the Capability to Target Extracellular Digestive Enzymes

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