{"id":3866,"date":"2017-01-20T14:06:00","date_gmt":"2017-01-20T14:06:00","guid":{"rendered":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/?p=3866"},"modified":"2026-01-28T09:34:46","modified_gmt":"2026-01-28T09:34:46","slug":"relationships-leading-to-the-potent-vhl-inhibitor-vh298","status":"publish","type":"post","link":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/2017\/01\/20\/relationships-leading-to-the-potent-vhl-inhibitor-vh298\/","title":{"rendered":"Relationships leading to the potent VHL inhibitor VH298"},"content":{"rendered":"\n<p class=\"wp-block-paragraph\">The article will be part of the journal Special Issue on \u201cInducing Protein Degradation as a New Therapeutic Strategy\u201d, edited by Prof. Craig Crews and Prof. Shameng Wang.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><a href=\"https:\/\/pubs.acs.org\/doi\/full\/10.1021\/acs.jmedchem.7b00675\">Read our article Open Access<\/a><\/p>\n\n\n\n<figure class=\"wp-block-gallery has-nested-images columns-4 is-cropped brgr gallery wp-block-gallery-1 is-layout-flex wp-block-gallery-is-layout-flex\">\n<figure class=\"wp-block-image size-full\"><img loading=\"lazy\" decoding=\"async\" width=\"600\" height=\"450\" data-id=\"3878\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/vh298-blue.png\" alt=\"Crystal structure of VH298 bound to VHL\" class=\"wp-image-3878\"\/><figcaption class=\"wp-element-caption\">Crystal structure of VH298 bound to VHL<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img decoding=\"async\" data-id=\"3879\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/ToC-graphics-01-1024x447.jpg\" alt=\"Table of content graphics\" class=\"wp-image-3879\"\/><figcaption class=\"wp-element-caption\">Table of content graphics<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-full\"><img loading=\"lazy\" decoding=\"async\" width=\"943\" height=\"884\" data-id=\"3877\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0001.jpeg\" alt=\"Figure 1. Initial optimization strategy\" class=\"wp-image-3877\"\/><figcaption class=\"wp-element-caption\">Figure 1. Initial optimization strategy<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-full\"><img decoding=\"async\" data-id=\"3876\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0002.jpeg\" alt=\"Figure 2. Biophysical characterization of inhibitor 10 binding to VBC.\" class=\"wp-image-3876\"\/><figcaption class=\"wp-element-caption\">Figure 2. Biophysical characterization of inhibitor 10 binding to VBC.<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img decoding=\"async\" data-id=\"3875\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0003-1024x816.jpeg\" alt=\"Figure 3. Co-crystal structures of first-series inhibitors\" class=\"wp-image-3875\"\/><figcaption class=\"wp-element-caption\">Figure 3. Co-crystal structures of first-series inhibitors<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img decoding=\"async\" data-id=\"3874\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0004-1024x989.jpeg\" alt=\"Figure 4. Cellular activity and toxicity of 10\" class=\"wp-image-3874\"\/><figcaption class=\"wp-element-caption\">Figure 4. Cellular activity and toxicity of 10<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img loading=\"lazy\" decoding=\"async\" width=\"989\" height=\"955\" data-id=\"3873\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0005.jpeg\" alt=\"Figure 5. Second series optimization strategy.\" class=\"wp-image-3873\"\/><figcaption class=\"wp-element-caption\">Figure 5. Second series optimization strategy.<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img decoding=\"async\" data-id=\"3872\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0006-1024x576.jpeg\" alt=\"Figure 6. Inhibitor 15 is not cytotoxic.\" class=\"wp-image-3872\"\/><figcaption class=\"wp-element-caption\">Figure 6. Inhibitor 15 is not cytotoxic.<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img decoding=\"async\" data-id=\"3871\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0007-1024x786.jpeg\" alt=\"Figure 7. Co-crystal structures of second-series inhibitors\" class=\"wp-image-3871\"\/><figcaption class=\"wp-element-caption\">Figure 7. Co-crystal structures of second-series inhibitors<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img decoding=\"async\" data-id=\"3870\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0008-571x1024.jpeg\" alt=\"Figure 8. Correlations between cellular activity and physicochemical parameters in vitro\" class=\"wp-image-3870\"\/><figcaption class=\"wp-element-caption\">Figure 8. Correlations between cellular activity and physicochemical parameters in vitro<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img loading=\"lazy\" decoding=\"async\" width=\"975\" height=\"642\" data-id=\"3880\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0009.jpeg\" alt=\"Figure 9. Activity in cells vs half-life dissociation from VBC protein complex.\" class=\"wp-image-3880\"\/><figcaption class=\"wp-element-caption\">Figure 9. Activity in cells vs half-life dissociation from VBC protein complex.<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img decoding=\"async\" data-id=\"3869\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0010-1024x979.jpeg\" alt=\"Scheme 1\" class=\"wp-image-3869\"\/><figcaption class=\"wp-element-caption\">Scheme 1<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img decoding=\"async\" data-id=\"3868\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0011-1024x496.jpeg\" alt=\"Scheme 2\" class=\"wp-image-3868\"\/><figcaption class=\"wp-element-caption\">Scheme 2<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-large\"><img decoding=\"async\" data-id=\"3867\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2025\/01\/jm-2017-00675x_0012-1024x204.jpeg\" alt=\"Scheme 3\" class=\"wp-image-3867\"\/><figcaption class=\"wp-element-caption\">Scheme 3<\/figcaption><\/figure>\n<\/figure>\n\n\n\n<p class=\"wp-block-paragraph\"><br><\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><\/p>\n","protected":false},"excerpt":{"rendered":"<p>The article will be part of the journal Special Issue on \u201cInducing Protein Degradation as a New Therapeutic Strategy\u201d, edited by Prof. Craig Crews and Prof. Shameng Wang. Read our article Open Access<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[19],"tags":[],"class_list":["post-3866","post","type-post","status-publish","format-standard","hentry","category-19"],"blocksy_meta":[],"_links":{"self":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/3866","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/comments?post=3866"}],"version-history":[{"count":1,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/3866\/revisions"}],"predecessor-version":[{"id":4948,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/3866\/revisions\/4948"}],"wp:attachment":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/media?parent=3866"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/categories?post=3866"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/tags?post=3866"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}