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Article ; Online: Old Drugs for a New Virus: Repurposed Approaches for Combating COVID-19.

Saul, Sirle / Einav, Shirit

ACS infectious diseases

2020 Volume 6, Issue 9, Page(s) 2304–2318

Abstract: There is a large global unmet need for effective countermeasures to combat severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the causative agent of coronavirus disease 2019 (COVID-19). The development of novel antiviral drugs is expensive and ...

Abstract	There is a large global unmet need for effective countermeasures to combat severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the causative agent of coronavirus disease 2019 (COVID-19). The development of novel antiviral drugs is expensive and too slow to meet the immediate need. The repurposing of drugs that are approved or are under advanced clinical investigation provides a cost- and time-effective therapeutic solution. This review summarizes the major repurposed approaches that have been proposed or are already being studied in clinical trials for COVID-19. Among these approaches are drugs that aim to reduce SARS-CoV-2 replication by targeting either viral enzymatic functions or cellular factors required for the viral life cycle. Drugs that modulate the host immune response to SARS-CoV-2 infection by boosting it to enhance viral clearance or by suppressing it to prevent excessive inflammation and tissue injury represent another category. Lastly, we discuss means to discover repurposed drugs and the ongoing challenges associated with the off-label use of existing drugs in the context of the COVID-19 outbreak.
MeSH term(s)	Animals ; Anti-Inflammatory Agents/therapeutic use ; Antiviral Agents/therapeutic use ; Betacoronavirus/drug effects ; Betacoronavirus/isolation & purification ; COVID-19 ; Coronavirus Infections/drug therapy ; Coronavirus Infections/immunology ; Coronavirus Infections/virology ; Drug Repositioning ; Humans ; Inflammation/immunology ; Inflammation/prevention & control ; Inflammation/virology ; Pandemics ; Pneumonia, Viral/drug therapy ; Pneumonia, Viral/immunology ; Pneumonia, Viral/virology ; SARS-CoV-2 ; Virus Replication/drug effects
Chemical Substances	Anti-Inflammatory Agents ; Antiviral Agents
Keywords	covid19
Language	English
Publishing date	2020-08-10
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ISSN	2373-8227
ISSN (online)	2373-8227
DOI	10.1021/acsinfecdis.0c00343
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Old Drugs for a New Virus

Saul, Sirle / Einav, Shirit

ACS Infectious Diseases

Repurposed Approaches for Combating COVID-19

2020 Volume 6, Issue 9, Page(s) 2304–2318

Keywords	covid19
Language	English
Publisher	American Chemical Society (ACS)
Publishing country	us
Document type	Article ; Online
ISSN	2373-8227
DOI	10.1021/acsinfecdis.0c00343
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Optimization of 4-Anilinoquinolines as Dengue Virus Inhibitors.

Huang, Pei-Tzu / Saul, Sirle / Einav, Shirit / Asquith, Christopher R M

Molecules (Basel, Switzerland)

2021 Volume 26, Issue 23

Abstract: Emerging viral infections, including those caused by dengue virus (DENV) and Venezuelan Equine Encephalitis virus (VEEV), pose a significant global health challenge. Here, we report the preparation and screening of a series of 4-anilinoquinoline ... ...

Abstract	Emerging viral infections, including those caused by dengue virus (DENV) and Venezuelan Equine Encephalitis virus (VEEV), pose a significant global health challenge. Here, we report the preparation and screening of a series of 4-anilinoquinoline libraries targeting DENV and VEEV. This effort generated a series of lead compounds, each occupying a distinct chemical space, including 3-((6-bromoquinolin-4-yl)amino)phenol (
MeSH term(s)	Animals ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Cell Line ; Dengue/drug therapy ; Dengue Virus/drug effects ; Encephalitis Virus, Venezuelan Equine/drug effects ; Encephalomyelitis, Venezuelan Equine/drug therapy ; Humans ; Quinolines/chemistry ; Quinolines/pharmacology ; Virus Replication/drug effects
Chemical Substances	2-anilinoquinoline ; Antiviral Agents ; Quinolines
Language	English
Publishing date	2021-12-03
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules26237338
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Article ; Online: Identification and evaluation of 4-anilinoquin(az)olines as potent inhibitors of both dengue virus (DENV) and Venezuelan equine encephalitis virus (VEEV).

Saul, Sirle / Huang, Pei-Tzu / Einav, Shirit / Asquith, Christopher R M

Bioorganic & medicinal chemistry letters

2021 Volume 52, Page(s) 128407

Abstract: There is an urgent need for novel strategies for the treatment of emerging arthropod-borne viral infections, including those caused by dengue virus (DENV) and Venezuelan equine encephalitis virus (VEEV). We prepared and screened focused libraries of 4- ... ...

Abstract	There is an urgent need for novel strategies for the treatment of emerging arthropod-borne viral infections, including those caused by dengue virus (DENV) and Venezuelan equine encephalitis virus (VEEV). We prepared and screened focused libraries of 4-anilinoquinolines and 4-anilinoquinazolines for antiviral activity and identified three potent compounds. N-(2,5-dimethoxyphenyl)-6-(trifluoromethyl)quinolin-4-amine (10) inhibited DENV infection with an EC
MeSH term(s)	Aniline Compounds/chemical synthesis ; Aniline Compounds/chemistry ; Aniline Compounds/pharmacology ; Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Dengue Virus/drug effects ; Dose-Response Relationship, Drug ; Encephalitis Virus, Venezuelan Equine/drug effects ; Microbial Sensitivity Tests ; Molecular Structure ; Quinazolines/chemical synthesis ; Quinazolines/chemistry ; Quinazolines/pharmacology ; Structure-Activity Relationship
Chemical Substances	Aniline Compounds ; Antiviral Agents ; Quinazolines ; anilinoquinazoline
Language	English
Publishing date	2021-10-05
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2021.128407
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Old Drugs for a New Virus: Repurposed Approaches for Combating COVID-19

Saul, Sirle / Einav, Shirit

ACS Infect Dis

Abstract	There is a large global unmet need for effective countermeasures to combat severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the causative agent of coronavirus disease 2019 (COVID-19). The development of novel antiviral drugs is expensive and too slow to meet the immediate need. The repurposing of drugs that are approved or are under advanced clinical investigation provides a cost- and time-effective therapeutic solution. This review summarizes the major repurposed approaches that have been proposed or are already being studied in clinical trials for COVID-19. Among these approaches are drugs that aim to reduce SARS-CoV-2 replication by targeting either viral enzymatic functions or cellular factors required for the viral life cycle. Drugs that modulate the host immune response to SARS-CoV-2 infection by boosting it to enhance viral clearance or by suppressing it to prevent excessive inflammation and tissue injury represent another category. Lastly, we discuss means to discover repurposed drugs and the ongoing challenges associated with the off-label use of existing drugs in the context of the COVID-19 outbreak.
Keywords	covid19
Publisher	WHO
Document type	Article
Note	WHO #Covidence: #656961
Database	COVID19

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Article ; Online: Optimization of 4-Anilinoquinolines as Dengue Virus Inhibitors

Pei-Tzu Huang / Sirle Saul / Shirit Einav / Christopher R. M. Asquith

Molecules, Vol 26, Iss 7338, p

2021 Volume 7338

Abstract	Emerging viral infections, including those caused by dengue virus (DENV) and Venezuelan Equine Encephalitis virus (VEEV), pose a significant global health challenge. Here, we report the preparation and screening of a series of 4-anilinoquinoline libraries targeting DENV and VEEV. This effort generated a series of lead compounds, each occupying a distinct chemical space, including 3-((6-bromoquinolin-4-yl)amino)phenol ( 12 ), 6-bromo- N -(5-fluoro-1H-indazol-6-yl)quinolin-4-amine ( 50 ) and 6-((6-bromoquinolin-4-yl)amino)isoindolin-1-one ( 52 ), with EC 50 values of 0.63–0.69 µM for DENV infection. These compound libraries demonstrated very limited toxicity with CC 50 values greater than 10 µM in almost all cases. Additionally, the lead compounds were screened for activity against VEEV and demonstrated activity in the low single-digit micromolar range, with 50 and 52 demonstrating EC 50 s of 2.3 µM and 3.6 µM, respectively. The promising results presented here highlight the potential to further refine this series in order to develop a clinical compound against DENV, VEEV, and potentially other emerging viral threats.
Keywords	dengue virus (DENV) ; 4-anilinoquinoline ; flavivirus ; alphavirus ; VEEV ; antivirals ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2021-12-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines.

Saul, Sirle / Pu, Szu-Yuan / Zuercher, William J / Einav, Shirit / Asquith, Christopher R M

Bioorganic & medicinal chemistry letters

2020 Volume 30, Issue 16, Page(s) 127284

Abstract: Screening a series of 4-anilinoquinolines and 4-anilinoquinazolines enabled identification of potent novel inhibitors of dengue virus (DENV). Preparation of focused 4-anilinoquinoline/quinazoline scaffold arrays led to the identification of a series of ... ...

Abstract	Screening a series of 4-anilinoquinolines and 4-anilinoquinazolines enabled identification of potent novel inhibitors of dengue virus (DENV). Preparation of focused 4-anilinoquinoline/quinazoline scaffold arrays led to the identification of a series of high potency 6-substituted bromine and iodine derivatives. The most potent compound 6-iodo-4-((3,4,5-trimethoxyphenyl)amino)quinoline-3-carbonitrile (47) inhibited DENV infection with an EC
MeSH term(s)	Aniline Compounds/chemical synthesis ; Aniline Compounds/chemistry ; Aniline Compounds/pharmacology ; Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Dengue Virus/drug effects ; Dose-Response Relationship, Drug ; Microbial Sensitivity Tests ; Molecular Structure ; Quinazolines/chemical synthesis ; Quinazolines/chemistry ; Quinazolines/pharmacology ; Structure-Activity Relationship
Chemical Substances	Aniline Compounds ; Antiviral Agents ; Quinazolines
Language	English
Publishing date	2020-05-27
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S.
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2020.127284
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 3203: Show issues

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Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

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Article: Synthesis and evaluation of 3-alkynyl-5-aryl-7-aza-indoles as broad-spectrum antiviral agents.

Martinez-Gualda, Belén / Graus, Mirthe / Camps, Anita / Vanhulle, Emiel / Saul, Sirle / Azari, Siavash / Nhu Tran, Do Hoang / Vangeel, Laura / Chiu, Winston / Neyts, Johan / Schols, Dominique / Einav, Shirit / Vermeire, Kurt / De Jonghe, Steven

Frontiers in chemistry

2022 Volume 10, Page(s) 1058229

Abstract: RNA viral infections, including those caused by respiratory syncytial virus (RSV), severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and Venezuelan Equine encephalitis virus (VEEV), pose a major global health challenge. Here, we report the ... ...

Abstract	RNA viral infections, including those caused by respiratory syncytial virus (RSV), severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and Venezuelan Equine encephalitis virus (VEEV), pose a major global health challenge. Here, we report the synthesis and screening of a series of pyrrolo[2,3-
Language	English
Publishing date	2022-10-26
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2711776-5
ISSN	2296-2646
ISSN	2296-2646
DOI	10.3389/fchem.2022.1058229
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Discovery of 3-phenyl- and 3-N-piperidinyl-isothiazolo[4,3-b]pyridines as highly potent inhibitors of cyclin G-associated kinase.

Martinez-Gualda, Belén / Saul, Sirle / Froeyen, Mathy / Schols, Dominique / Herdewijn, Piet / Einav, Shirit / De Jonghe, Steven

European journal of medicinal chemistry

2021 Volume 213, Page(s) 113158

Abstract: Structural modifications at position 3 of the isothiazolo[4,3-b]pyridine scaffold afforded a new series of cyclin G-associated kinase (GAK) inhibitors. It was shown that the insertion of a carboxamide residue at position 3 of a phenyl or piperidinyl ... ...

Abstract	Structural modifications at position 3 of the isothiazolo[4,3-b]pyridine scaffold afforded a new series of cyclin G-associated kinase (GAK) inhibitors. It was shown that the insertion of a carboxamide residue at position 3 of a phenyl or piperidinyl moiety generated potent GAK inhibitors with IC
MeSH term(s)	Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Cell Line, Tumor ; Cell Survival/drug effects ; Dengue Virus/drug effects ; Dose-Response Relationship, Drug ; Drug Discovery ; Humans ; Intracellular Signaling Peptides and Proteins/antagonists & inhibitors ; Intracellular Signaling Peptides and Proteins/metabolism ; Microbial Sensitivity Tests ; Molecular Structure ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Protein-Serine-Threonine Kinases/antagonists & inhibitors ; Protein-Serine-Threonine Kinases/metabolism ; Structure-Activity Relationship
Chemical Substances	Antiviral Agents ; Intracellular Signaling Peptides and Proteins ; Protein Kinase Inhibitors ; GAK protein, human (EC 2.7.11.1) ; Protein-Serine-Threonine Kinases (EC 2.7.11.1)
Language	English
Publishing date	2021-01-12
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2021.113158
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.B 784: Show issues

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Article: PIP4K2C inhibition reverses autophagic flux impairment induced by SARS-CoV-2.

Karim, Marwah / Mishra, Manjari / Lo, Chieh-Wen / Saul, Sirle / Cagirici, Halise Busra / Tran, Do Hoang Nhu / Agrawal, Aditi / Ghita, Luca / Ojha, Amrita / East, Michael P / Gammeltoft, Karen Anbro / Sahoo, Malaya Kumar / Johnson, Gary L / Das, Soumita / Jochmans, Dirk / Cohen, Courtney A / Gottwein, Judith / Dye, John / Neff, Norma /

Pinsky, Benjamin A / Laitinen, Tuomo / Pantsar, Tatu / Poso, Antti / Zanini, Fabio / Jonghe, Steven De / Asquith, Christopher R M / Einav, Shirit

bioRxiv : the preprint server for biology

2024

Abstract: In search for broad-spectrum antivirals, we discovered a small molecule inhibitor, RMC-113, that potently suppresses the replication of multiple RNA viruses including SARS-CoV-2 in human lung organoids. We demonstrated selective dual inhibition of the ... ...

Abstract	In search for broad-spectrum antivirals, we discovered a small molecule inhibitor, RMC-113, that potently suppresses the replication of multiple RNA viruses including SARS-CoV-2 in human lung organoids. We demonstrated selective dual inhibition of the lipid kinases PIP4K2C and PIKfyve by RMC-113 and target engagement by its clickable analog. Advanced lipidomics revealed alteration of SARS-CoV-2-induced phosphoinositide signature by RMC-113 and linked its antiviral effect with functional PIP4K2C and PIKfyve inhibition. We discovered PIP4K2C's roles in SARS-CoV-2 entry, RNA replication, and assembly/egress, validating it as a druggable antiviral target. Integrating proteomics, single-cell transcriptomics, and functional assays revealed that PIP4K2C binds SARS-CoV-2 nonstructural protein 6 and regulates virus-induced impairment of autophagic flux. Reversing this autophagic flux impairment is a mechanism of antiviral action of RMC-113. These findings reveal virus-induced autophagy regulation via PIP4K2C, an understudied kinase, and propose dual inhibition of PIP4K2C and PIKfyve as a candidate strategy to combat emerging viruses.
Language	English
Publishing date	2024-04-17
Publishing country	United States
Document type	Preprint
DOI	10.1101/2024.04.15.589676
Database	MEDical Literature Analysis and Retrieval System OnLINE

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