ArticleBioorganic & medicinal chemistry2014
Structural optimization of a retrograde trafficking inhibitor that protects cells from infections by human polyoma- and papillomaviruses.
Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 37 citations in OpenAlex.
- Retrograde trafficking inhibitors allosterically trap Get3 to block tail-anchored protein biogenesis.bioRxiv : the preprint server for biology · 2026Article
- Repurposing screens reveal a role for PKCη and NF1 in SARS-CoV-2 infection.PLoS pathogens · 2026Article
- In Vivo Sustained Release of the Retrograde Transport Inhibitor Retro-2.1 Formulated in a Thermosensitive Hydrogel.International journal of molecular sciences · 2022Article
- Thermoresponsive Copolymer Nanovectors Improve the Bioavailability of Retrograde Inhibitors in the Treatment ofFrontiers in cellular and infection microbiology · 2021Article
- Functional dissection of the retrograde Shiga toxin trafficking inhibitor Retro-2.Nature chemical biology · 2020Article
- Discovery of Retro-1 Analogs Exhibiting Enhanced Anti-vaccinia Virus Activity.Frontiers in microbiology · 2020Article
- Internalization and Intoxication of Human Macrophages by the Active Subunit of theFrontiers in immunology · 2020Article
- Article
- Inhibition of diverse opportunistic viruses by structurally optimized retrograde trafficking inhibitors.Bioorganic & medicinal chemistry · 2019Article
- 2,3-Dihydroquinazolin-4(1RSC advances · 2018Review
- Strategies for the enhanced intracellular delivery of nanomaterials.Drug discovery today · 2018Review
- ABMA, a small molecule that inhibits intracellular toxins and pathogens by interfering with late endosomal compartments.Scientific reports · 2017Article
- JC Polyomavirus Attachment and Entry: Potential Sites for PML Therapeutics.Current clinical microbiology reports · 2017Article
- Structurally optimized analogs of the retrograde trafficking inhibitor Retro-2cycl limit Leishmania infections.PLoS neglected tropical diseases · 2017Article
- Protection against Shiga Toxins.Toxins · 2017Review
- Potent Inhibition of Human Cytomegalovirus by Modulation of Cellular SNARE Syntaxin 5.Journal of virology · 2017Article
- Retrograde Transport from Early Endosomes to the trans-Golgi Network Enables Membrane Wrapping and Egress of Vaccinia Virus Virions.Journal of virology · 2016Article
- BK nephropathy in the native kidneys of patients with organ transplants: Clinical spectrum of BK infection.World journal of transplantation · 2016Review
- An animal model for progressive multifocal leukoencephalopathy.The Journal of clinical investigation · 2014Article
- Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
Human polyoma- and papillomaviruses are non-enveloped DNA viruses that cause severe pathologies and mortalities. Under circumstances of immunosuppression, JC polyomavirus causes a fatal demyelinating disease called progressive multifocal leukoencephalopathy (PML) and the BK polyomavirus is the etiological agent of polyomavirus-induced nephropathy and hemorrhagic cystitis. Human papillomavirus type 16, another non-enveloped DNA virus, is associated with the development of cancers in tissues like the uterine cervix and oropharynx. Currently, there are no approved drugs or vaccines to treat or prevent polyomavirus infections. We recently discovered that the small molecule Retro-2(cycl), an inhibitor of host retrograde trafficking, blocked infection by several human and monkey polyomaviruses. Here, we report diversity-oriented syntheses of Retro-2(cycl) and evaluation of the resulting analogs using an assay of human cell infections by JC polyomavirus. We defined structure-activity relationships and also discovered analogs with significantly improved potency as suppressors of human polyoma- and papillomavirus infection in vitro. Our findings represent an advance in the development of drug candidates that can broadly protect humans from non-enveloped DNA viruses and toxins that exploit retrograde trafficking as a means for cell entry.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.