Antiviral Chemistry and Chemotherapy最新文献

筛选
英文 中文
Retinazone inhibits certain blood-borne human viruses including Ebola virus Zaire. 维甲酸酮抑制某些血液传播的人类病毒,包括扎伊尔埃博拉病毒。
Antiviral Chemistry and Chemotherapy Pub Date : 2014-04-11 DOI: 10.3851/IMP2568
Andreas J Kesel, Zhuhui Huang, Michael G Murray, Mark N Prichard, Laura Caboni, Daniel K Nevin, Darren Fayne, David G Lloyd, Mervi A Detorio, Raymond F Schinazi
{"title":"Retinazone inhibits certain blood-borne human viruses including Ebola virus Zaire.","authors":"Andreas J Kesel, Zhuhui Huang, Michael G Murray, Mark N Prichard, Laura Caboni, Daniel K Nevin, Darren Fayne, David G Lloyd, Mervi A Detorio, Raymond F Schinazi","doi":"10.3851/IMP2568","DOIUrl":"https://doi.org/10.3851/IMP2568","url":null,"abstract":"Background: Human HBV and HIV integrate their retro-transcribed DNA proviruses into the human host genome. Existing antiretroviral drug regimens fail to directly target these intrachromosomal xenogenomes, leading to persistence of viral genetic information. Retinazone (RTZ) constitutes a novel vitamin A-derived (retinoid) thiosemicarbazone derivative with broad-spectrum antiviral activity versus HIV, HCV, varicella-zoster virus and cytomegalovirus. Methods: The in vitro inhibitory action of RTZ on HIV-1 strain LAI, human HBV strain ayw, HCV-1b strain Con1, enhanced green fluorescent protein-expressing Ebola virus Zaire 1976 strain Mayinga, wild-type Ebola virus Zaire 1976 strain Mayinga, human herpesvirus 6B and Kaposi's sarcoma-associated herpesvirus replication was investigated. The binding of RTZ to human glucocorticoid receptor was determined. Results: RTZ inhibits blood-borne human HBV multiplication in vitro by covalent inactivation of intragenic and intraexonic viral glucocorticoid response elements, and, in close analogy, RTZ suppresses HIV-1 multiplication in vitro. RTZ disrupts the multiplication of blood-borne human HCV and Ebola Zaire virus at nanomolar concentrations in vitro. RTZ has the capacity to bind to human glucocorticoid receptor, to selectively and covalently bind to intraexonic viral glucocorticoid response elements, and thereby to inactivate human genome-integrated proviral DNA of human HBV and HIV. Conclusions: RTZ represents the first reported antiviral agent capable of eradicating HIV and HBV proviruses from their human host. Furthermore, RTZ represents a potent and efficacious small-molecule in vitro inhibitor of Ebola virus Zaire 1976 strain Mayinga replication.","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"23 5","pages":"197-215"},"PeriodicalIF":0.0,"publicationDate":"2014-04-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2568","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31401777","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 14
Small molecule inhibitors of West Nile virus. 西尼罗河病毒的小分子抑制剂。
Antiviral Chemistry and Chemotherapy Pub Date : 2014-04-11 DOI: 10.3851/IMP2581
Samia A Elseginy, Alberto Massarotti, Galal Am Nawwar, Kamilia M Amin, Andrea Brancale
{"title":"Small molecule inhibitors of West Nile virus.","authors":"Samia A Elseginy,&nbsp;Alberto Massarotti,&nbsp;Galal Am Nawwar,&nbsp;Kamilia M Amin,&nbsp;Andrea Brancale","doi":"10.3851/IMP2581","DOIUrl":"https://doi.org/10.3851/IMP2581","url":null,"abstract":"<p><p>West Nile virus (WNV) is a human pathogen which is rapidly expanding worldwide. It is a member of the Flavivirus genus and it is transmitted by mosquitos between its avian hosts and occasionally in mammalian hosts. In humans the infection is often asymptomatic, however, the most severe cases result in encephalitis or meningitis. Approximately 10% of cases of neuroinvasive disease are fatal. To date there is no effective human vaccine or effective antiviral therapy available to treat WNV infections. For this reason, research in this field is rapidly growing. In this article we will review the latest efforts in the design and development of novel WNV inhibitors from a medicinal chemistry point of view, highlighting challenges and opportunities for the researchers working in this field. </p>","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"23 5","pages":"179-87"},"PeriodicalIF":0.0,"publicationDate":"2014-04-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2581","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31492630","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
Topical SMIP-7.7, a toll-like receptor 7 agonist, protects against genital herpes simplex virus type-2 disease in the guinea pig model of genital herpes. 外用SMIP-7.7,一种toll样受体7激动剂,在生殖器疱疹的豚鼠模型中对生殖器单纯疱疹病毒2型疾病有保护作用。
Antiviral Chemistry and Chemotherapy Pub Date : 2014-04-11 DOI: 10.3851/IMP2499
David I Bernstein, Rhonda D Cardin, Fernando J Bravo, Julie Earwood, Jennifer R Clark, Yongkai Li, Pranab Mishra, Chun Li, Bishnu P Nayak, Andrew T Miller, Tom Y-H Wu, Michael P Cooke, Nicholas M Valiante
{"title":"Topical SMIP-7.7, a toll-like receptor 7 agonist, protects against genital herpes simplex virus type-2 disease in the guinea pig model of genital herpes.","authors":"David I Bernstein,&nbsp;Rhonda D Cardin,&nbsp;Fernando J Bravo,&nbsp;Julie Earwood,&nbsp;Jennifer R Clark,&nbsp;Yongkai Li,&nbsp;Pranab Mishra,&nbsp;Chun Li,&nbsp;Bishnu P Nayak,&nbsp;Andrew T Miller,&nbsp;Tom Y-H Wu,&nbsp;Michael P Cooke,&nbsp;Nicholas M Valiante","doi":"10.3851/IMP2499","DOIUrl":"https://doi.org/10.3851/IMP2499","url":null,"abstract":"<p><strong>Background: </strong>Development of more effective therapies for genital herpes simplex virus type-2 (HSV-2) infections remains a priority. The toll-like receptors (TLR) are attractive targets for the immunomodulation of primary and recurrent genital herpes infection. The guinea pig model of genital HSV-2 disease was therefore used to evaluate the efficacy of a new TLR-7 agonist, SMIP-7.7.</p><p><strong>Methods: </strong>The effects of SMIP-7.7 at concentrations between 0.90% and 0.09% were compared to the vehicle control or Aldara(®) (3M Health Care Limited, Northridge, CA, USA) as treatment for genital HSV-2 infections. Following intravaginal inoculation of Hartley guinea pigs with 10(6) pfu HSV-2 (MS strain), animals were treated intravaginally beginning at 36 h post-infection. Animals were evaluated for acute disease, acute virus replication, recurrent disease and shedding, as well as infection of the dorsal root ganglia.</p><p><strong>Results: </strong>Treatment with SMIP-7.7 significantly decreased mean total lesion scores during primary infection (all doses, P<0.01 compared with vehicle control, and similar to Aldara(®)). Vaginal virus titres were reduced in treated animals compared with vehicle control (P<0.001 for each treatment versus vehicle control on day 4). Treatment with SMIP-7.7 also significantly decreased the number of recurrent lesion days, the number of days with recurrent virus shedding and the infection of the dorsal root ganglia compared to the vehicle control, and was similar to Aldara(®). As opposed to Aldara(®), SMIP-7.7 did not induce fever or weight loss during treatment.</p><p><strong>Conclusions: </strong>SMIP-7.7 improves the outcome of primary and recurrent HSV-2 disease comparable to Aldara(®) but without some of the side effects associated with Aldara(®).</p>","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"23 5","pages":"189-96"},"PeriodicalIF":0.0,"publicationDate":"2014-04-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2499","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31116208","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 12
The application of prophylactic antibodies for rhinovirus infections. 鼻病毒感染预防性抗体的应用。
Antiviral Chemistry and Chemotherapy Pub Date : 2014-04-11 DOI: 10.3851/IMP2578
Riccardo Privolizzi, Roberto Solari, Sebastian L Johnston, Gary R McLean
{"title":"The application of prophylactic antibodies for rhinovirus infections.","authors":"Riccardo Privolizzi,&nbsp;Roberto Solari,&nbsp;Sebastian L Johnston,&nbsp;Gary R McLean","doi":"10.3851/IMP2578","DOIUrl":"https://doi.org/10.3851/IMP2578","url":null,"abstract":"<p><p>Rhinoviruses are extremely common pathogens of the upper respiratory tract with adults experiencing on average 2-5 infections per year and children up to 12 infections. Although infections are not life threatening, except in cases of chronic lung disease where rhinoviruses are the major precipitant of acute exacerbations of disease, there is a high associated economic cost resulting from lost productivity due to absence from work or school. Treatment of infections focuses on symptom relief with anti-pyretics/analgesics as there are no antiviral therapies available and vaccine strategies face difficulties because of the large number of viral serotypes. Here, we assess the potential for prophylactic antibody intervention for these ubiquitous human pathogens. </p>","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"23 5","pages":"173-7"},"PeriodicalIF":0.0,"publicationDate":"2014-04-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2578","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31460932","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 10
Activity of a phenolic dibenzylsulfide against New World arenavirus infections. 酚类二苄基硫化物抗新世界沙粒病毒感染的活性。
Antiviral Chemistry and Chemotherapy Pub Date : 2014-01-29 DOI: 10.3851/IMP2532
Brian B Gowen, Kie-Hoon Jung, Eric J Sefing, Min-Hui Wong, Jonna B Westover, Donald F Smee
{"title":"Activity of a phenolic dibenzylsulfide against New World arenavirus infections.","authors":"Brian B Gowen,&nbsp;Kie-Hoon Jung,&nbsp;Eric J Sefing,&nbsp;Min-Hui Wong,&nbsp;Jonna B Westover,&nbsp;Donald F Smee","doi":"10.3851/IMP2532","DOIUrl":"https://doi.org/10.3851/IMP2532","url":null,"abstract":"<p><strong>Background: </strong>Junín virus (JUNV) and several other clade B New World arenaviruses cause human disease ranging from mild febrile illness to severe viral haemorrhagic fever. These viruses pose a significant threat to national security and safe and effective therapies are limited except in Argentina, where immune plasma is the standard of care for treating JUNV infection in cases of Argentine haemorrhagic fever.</p><p><strong>Methods: </strong>An in vitro screen of the Chemtura library identified several compounds with activity against Tacaribe virus (TCRV), a clade B arenavirus closely related to JUNV. Of these compounds, D746, a phenolic dibenzylsulfide, was further pursued for additional in vitro studies and evaluated in the AG129 mouse TCRV infection model.</p><p><strong>Results: </strong>D746 was found to act during an early to intermediate stage of the TCRV replication cycle and μM range activity was confirmed by virus yield reduction assays with both TCRV and JUNV. Although intraperitoneal twice daily treatment regimens were found to be highly effective when started 2 h prior to TCRV challenge in AG129 mice, post-exposure treatment initiated 3 days after infection was not efficacious. Interestingly, despite the pre-exposure treatment success, D746 did not reduce serum or tissue virus titres during the acute infection. Moreover, D746 elicited ascites fluid accumulation in mice during, as well as independent of, infection.</p><p><strong>Conclusions: </strong>Our findings suggest that D746 may be altering the host response to TCRV infection in AG129 mice in a way that limits pathogenesis and thereby protects mice from otherwise lethal infection in the absence of measurable reductions in viral burden.</p>","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"23 4","pages":"151-9"},"PeriodicalIF":0.0,"publicationDate":"2014-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2532","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31177471","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Antivirally active ribavirin analogues--4,5-disubstituted 1,2,3-triazole nucleosides: biological evaluation against certain respiratory viruses and computational modelling. 抗病毒活性利巴韦林类似物——4,5-二取代1,2,3-三唑核苷:对某些呼吸道病毒的生物学评价和计算模型。
Antiviral Chemistry and Chemotherapy Pub Date : 2014-01-29 DOI: 10.3851/IMP2564
Anna Krajczyk, Katarzyna Kulinska, Tadeusz Kulinski, Brett L Hurst, Craig W Day, Donald F Smee, Tomasz Ostrowski, Piotr Januszczyk, Joanna Zeidler
{"title":"Antivirally active ribavirin analogues--4,5-disubstituted 1,2,3-triazole nucleosides: biological evaluation against certain respiratory viruses and computational modelling.","authors":"Anna Krajczyk,&nbsp;Katarzyna Kulinska,&nbsp;Tadeusz Kulinski,&nbsp;Brett L Hurst,&nbsp;Craig W Day,&nbsp;Donald F Smee,&nbsp;Tomasz Ostrowski,&nbsp;Piotr Januszczyk,&nbsp;Joanna Zeidler","doi":"10.3851/IMP2564","DOIUrl":"https://doi.org/10.3851/IMP2564","url":null,"abstract":"<p><strong>Background: </strong>Ribavirin is a broad-spectrum antiviral agent that derives some of its activity from inhibition of cellular inosine monophosphate dehydrogenase (IMPDH), resulting in lower guanosine triphosphate (GTP) levels. Here we report the biological activities of three ribavirin analogues.</p><p><strong>Methods: </strong>Antiviral activities of test compounds were performed by in vitro cytopathic effect inhibition assays against influenza A (H1N1, H3N2 and H5N1), influenza B, measles, parainfluenza type 3 (PIV-3) and respiratory syncytial viruses. Compounds were modelled into the ribavirin 5'-monophosphate binding site of the crystallographic structure of the human type II IMPDH (hIMPDH2) ternary complex. Effects of compounds on intracellular GTP levels were performed by strong anion exchange HPLC analysis.</p><p><strong>Results: </strong>Of the three compounds evaluated, the 5-ethynyl nucleoside (ETCAR) exhibited virus-inhibitory activities (at 1.2-20 μM, depending upon the virus) against most of the viruses, except for weak activity against PIV-3 (62 μM). Antiviral activity of ETCAR was similar to ribavirin; however, cytotoxicity of ETCAR was greater than ribavirin. Replacing the 5-ethynyl group with a 5-propynyl or bromo substituent (BrCAR) considerably reduced antiviral activity. Computational studies of ternary complexes of hIMPDH2 enzyme with 5'-monophosphates of the compounds helped rationalize the observed differences in biological activity. All compounds suppressed GTP levels in cells; additionally, BrCAR suppressed adenosine triphosphate and elevated uridine triphosphate levels.</p><p><strong>Conclusions: </strong>Three compounds related to ribavirin inhibited IMPDH and had weak to moderate antiviral activity. Cytotoxicity adversely affected the antiviral selectivity of ETCAR. As with ribavirin, reduction in intracellular GTP may play a role in virus inhibition.</p>","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":" ","pages":"161-71"},"PeriodicalIF":0.0,"publicationDate":"2014-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2564","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40234024","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 38
Therapy for latent HIV-1 infection: the role of histone deacetylase inhibitors. 治疗潜伏HIV-1感染:组蛋白去乙酰化酶抑制剂的作用。
Antiviral Chemistry and Chemotherapy Pub Date : 2014-01-29 DOI: 10.3851/IMP2551
Mary E Manson McManamy, Shweta Hakre, Eric M Verdin, David M Margolis
{"title":"Therapy for latent HIV-1 infection: the role of histone deacetylase inhibitors.","authors":"Mary E Manson McManamy,&nbsp;Shweta Hakre,&nbsp;Eric M Verdin,&nbsp;David M Margolis","doi":"10.3851/IMP2551","DOIUrl":"https://doi.org/10.3851/IMP2551","url":null,"abstract":"<p><p>Persistence of HIV-1 in latently infected CD4(+) T-cells prevents eradication in HIV-infected treated patients. Latency is characterized by a reversible silencing of transcription of integrated HIV-1. Several molecular mechanisms have been described which contribute to latency, including the establishment and maintenance of repressive chromatin on the HIV-1 promoter. Histone deacetylation is a landmark modification associated with transcriptional repression of the HIV-1 promoter and inhibition of histone deacetylase enzymes (HDACs) reactivates latent HIV-1. Here, we review the different HDAC inhibitors that have been studied in HIV-1 latency and their therapeutic potential in reactivating latent HIV-1. </p>","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"23 4","pages":"145-9"},"PeriodicalIF":0.0,"publicationDate":"2014-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2551","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31939489","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 46
Past and future. Current drugs targeting HIV-1 integrase and reverse transcriptase-associated ribonuclease H activity: single and dual active site inhibitors. 过去和未来。目前针对HIV-1整合酶和逆转录相关核糖核酸酶H活性的药物:单活性位点和双活性位点抑制剂。
Antiviral Chemistry and Chemotherapy Pub Date : 2014-01-29 DOI: 10.3851/IMP2690
Francesca Esposito, Enzo Tramontano
{"title":"Past and future. Current drugs targeting HIV-1 integrase and reverse transcriptase-associated ribonuclease H activity: single and dual active site inhibitors.","authors":"Francesca Esposito,&nbsp;Enzo Tramontano","doi":"10.3851/IMP2690","DOIUrl":"https://doi.org/10.3851/IMP2690","url":null,"abstract":"<p><p>Catalytic HIV type-1 (HIV-1) integrase (IN) and ribonuclease H (RNase H) domains belong to the polynucleotidyl transferase superfamily and are characterized by highly conserved motifs that coordinate two divalent Mg(2+) cations and are attractive targets for new antiviral agents. Several structural features of both domains are now available. Drugs targeting the HIV-1 IN are currently approved for anti-HIV therapy, while no drug targeting the HIV-1 RNase H function is yet available. This review describes HIV-1 IN and the RNase H function and structures, compounds targeting their active sites and dual inhibition as a new approach for drug development. </p>","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":" ","pages":"129-44"},"PeriodicalIF":0.0,"publicationDate":"2014-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2690","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40259515","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 57
Novel thiosialosides tethered to metal nanoparticles as potent influenza A virus haemagglutinin blockers. 新型硫代硫苷系在金属纳米颗粒上作为甲型流感病毒血凝素阻滞剂。
Antiviral Chemistry and Chemotherapy Pub Date : 2013-05-16 DOI: 10.3851/IMP2553
Fei Feng, Yoshihiro Sakoda, Tatsuya Ohyanagi, Noriko Nagahori, Hitomi Shibuya, Masatoshi Okamastu, Nobuaki Miura, Hiroshi Kida, Shin-Ichiro Nishimura
{"title":"Novel thiosialosides tethered to metal nanoparticles as potent influenza A virus haemagglutinin blockers.","authors":"Fei Feng,&nbsp;Yoshihiro Sakoda,&nbsp;Tatsuya Ohyanagi,&nbsp;Noriko Nagahori,&nbsp;Hitomi Shibuya,&nbsp;Masatoshi Okamastu,&nbsp;Nobuaki Miura,&nbsp;Hiroshi Kida,&nbsp;Shin-Ichiro Nishimura","doi":"10.3851/IMP2553","DOIUrl":"https://doi.org/10.3851/IMP2553","url":null,"abstract":"<p><strong>Background: </strong>The purpose of this study was to develop a new class of influenza A virus haemagglutinin (HA) blockers by tethering thiosialoside molecules to metal nanoparticles and producing glycoclusters that enhance the affinity of HA binding by N-acetylneuraminic acid.</p><p><strong>Methods: </strong>Oxygen of the glycoside bond of sialoside was replaced with sulfur to prevent hydrolytic digestion of the N-acetylneuraminic acid residue by viral neuraminidase. Two novel thiosialosides, α-2-S-[p-(N-levulinyl)aminophenyl]-5-N-acetylneuraminic acid (Neu5Ac-S-Lev) and α-2-S-[m-(N-levulinyl)aminobenzyl]-5-N-acetylneuraminic acid (Neu5Ac-S-CH2-Lev), were tethered onto the surface of metal nanoparticles via an aminooxy functionalized thiol linker in a glycoblotting reaction. Gold (Au) and silver (Ag) nanoparticles were coated simultaneously with 11-mercaptoundecyl phosphorylcholine to reduce non-specific adsorption of proteins. Phosphorylcholine self-assembled monolayer-coated metals displaying clustered Neu5Ac (Neu5Ac-PCSAM-Au and Neu5Ac-PCSAM-Ag) were subjected to haemagglutination inhibition (HI) assays using the influenza A virus strain A/PR/8/1934 (H1N1).</p><p><strong>Results: </strong>Glyconanoparticles with thiosialosides had potent HI activities. In particular, Neu5Ac-PCSAM-Au with a diameter of 20 nm corresponding to 9.8 μM monosaccharide Neu5Ac was the most potent HA inhibitor. The versatility of this strategy was demonstrated by similar submicromolar HI activities of Neu5Ac-PCSAM-Ag with diameters of 50 nm and 150 nm.</p><p><strong>Conclusions: </strong>Glycosylated metal nanoparticles were designed and synthesized as potent influenza A virus HA blockers. This study may contribute to the acceleration of the discovery of a new class of nanoparticle anti-influenza drugs.</p>","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"23 2","pages":"59-65"},"PeriodicalIF":0.0,"publicationDate":"2013-05-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2553","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31344634","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 13
Antiviral drug development--success and failure: a personal perspective with a Japanese connection. 抗病毒药物开发——成功与失败:与日本相关的个人观点。
Antiviral Chemistry and Chemotherapy Pub Date : 2013-05-16 DOI: 10.3851/IMP2396
Erik De Clercq
{"title":"Antiviral drug development--success and failure: a personal perspective with a Japanese connection.","authors":"Erik De Clercq","doi":"10.3851/IMP2396","DOIUrl":"https://doi.org/10.3851/IMP2396","url":null,"abstract":"<p><p>At the 25th International Conference on Antiviral Research, I received a special recognition for my contribution to the International Society of Antiviral Research over a period of 25 years (from 1987 until 2012). This review follows the theme of my presentation at that event, which comprised 10 reminiscences, all with a Japanese connection concerning the success, or otherwise, in the clinical development of: double- and single-stranded polynucleotides; suramin, a polysulfonate; dextran sulfate, a polysulfate; brivudin; BVaraU; 2',3'-dideoxynucleoside analogues; HEPT; adefovir and tenofovir; CXCR4 antagonists; and elvitegravir.</p>","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"23 2","pages":"45-55"},"PeriodicalIF":0.0,"publicationDate":"2013-05-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3851/IMP2396","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30917671","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信