The inhibitory properties of acidic functionalised calix[4]arenes on human papillomavirus pentamer formation
© 2020 Informa UK Limited, trading as Taylor & Francis Group. Human Papillomavirus (HPV) is the leading cause of cervical cancer, with only some HPV types prevented with vaccines and no treatments for the viral infection itself. One way to target viral infection is by inhibiting the assemb...
| Main Authors: | , , , , , , , |
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| Format: | Journal Article |
| Language: | English |
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TAYLOR & FRANCIS LTD
2020
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| Subjects: | |
| Online Access: | http://hdl.handle.net/20.500.11937/80239 |
| _version_ | 1848764186021068800 |
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| author | Goh, Ching Yong Fu, D.Y. Duncan, Caitlin Tinker, Adam Li, F. Mocerino, Mauro Ogden, Mark Wu, Y. |
| author_facet | Goh, Ching Yong Fu, D.Y. Duncan, Caitlin Tinker, Adam Li, F. Mocerino, Mauro Ogden, Mark Wu, Y. |
| author_sort | Goh, Ching Yong |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | © 2020 Informa UK Limited, trading as Taylor & Francis Group.
Human Papillomavirus (HPV) is the leading cause of cervical cancer, with only some HPV types prevented with vaccines and no treatments for the viral infection itself. One way to target viral infection is by inhibiting the assembly of the L1 monomer into a pentamer, which forms the viral capsid. Four calix[4]arene compounds functionalised with D- and L-aspartic and glutamic acid and an iminodiacetic functionalised calix[4]arene were synthesised and tested for L1 pentamer formation inhibition. The amino acid functionalised calix[4]arene derivatives showed millimolar inhibition (IC50 = 0.72 to 2.67 mM) of pentamer formation, with little difference between the stereoisomers. The iminodiacetic acid calix[4]arene derivative showed no inhibitory properties, despite sharing structural similarities with the four other calix[4]arenes. Confirmation of binding the negatively charged compounds to the positive residues of the L1 protein was achieved by trypsin digestion. This study is helpful in the development of cost-effective inhibitors to prevent HPV assembly. |
| first_indexed | 2025-11-14T11:15:21Z |
| format | Journal Article |
| id | curtin-20.500.11937-80239 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-14T11:15:21Z |
| publishDate | 2020 |
| publisher | TAYLOR & FRANCIS LTD |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-802392021-07-16T00:30:07Z The inhibitory properties of acidic functionalised calix[4]arenes on human papillomavirus pentamer formation Goh, Ching Yong Fu, D.Y. Duncan, Caitlin Tinker, Adam Li, F. Mocerino, Mauro Ogden, Mark Wu, Y. Science & Technology Physical Sciences Chemistry, Multidisciplinary Chemistry Calixarene human papillomavirus assembly inhibitor L1 pentamer amino acid CAPSID PROTEIN CALIXARENE AGENTS © 2020 Informa UK Limited, trading as Taylor & Francis Group. Human Papillomavirus (HPV) is the leading cause of cervical cancer, with only some HPV types prevented with vaccines and no treatments for the viral infection itself. One way to target viral infection is by inhibiting the assembly of the L1 monomer into a pentamer, which forms the viral capsid. Four calix[4]arene compounds functionalised with D- and L-aspartic and glutamic acid and an iminodiacetic functionalised calix[4]arene were synthesised and tested for L1 pentamer formation inhibition. The amino acid functionalised calix[4]arene derivatives showed millimolar inhibition (IC50 = 0.72 to 2.67 mM) of pentamer formation, with little difference between the stereoisomers. The iminodiacetic acid calix[4]arene derivative showed no inhibitory properties, despite sharing structural similarities with the four other calix[4]arenes. Confirmation of binding the negatively charged compounds to the positive residues of the L1 protein was achieved by trypsin digestion. This study is helpful in the development of cost-effective inhibitors to prevent HPV assembly. 2020 Journal Article http://hdl.handle.net/20.500.11937/80239 10.1080/10610278.2020.1779930 English TAYLOR & FRANCIS LTD fulltext |
| spellingShingle | Science & Technology Physical Sciences Chemistry, Multidisciplinary Chemistry Calixarene human papillomavirus assembly inhibitor L1 pentamer amino acid CAPSID PROTEIN CALIXARENE AGENTS Goh, Ching Yong Fu, D.Y. Duncan, Caitlin Tinker, Adam Li, F. Mocerino, Mauro Ogden, Mark Wu, Y. The inhibitory properties of acidic functionalised calix[4]arenes on human papillomavirus pentamer formation |
| title | The inhibitory properties of acidic functionalised calix[4]arenes on human papillomavirus pentamer formation |
| title_full | The inhibitory properties of acidic functionalised calix[4]arenes on human papillomavirus pentamer formation |
| title_fullStr | The inhibitory properties of acidic functionalised calix[4]arenes on human papillomavirus pentamer formation |
| title_full_unstemmed | The inhibitory properties of acidic functionalised calix[4]arenes on human papillomavirus pentamer formation |
| title_short | The inhibitory properties of acidic functionalised calix[4]arenes on human papillomavirus pentamer formation |
| title_sort | inhibitory properties of acidic functionalised calix[4]arenes on human papillomavirus pentamer formation |
| topic | Science & Technology Physical Sciences Chemistry, Multidisciplinary Chemistry Calixarene human papillomavirus assembly inhibitor L1 pentamer amino acid CAPSID PROTEIN CALIXARENE AGENTS |
| url | http://hdl.handle.net/20.500.11937/80239 |