{"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

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

Read our article Open Access<\/a><\/p>\n\n\n\n

\n
\"Crystal
Crystal structure of VH298 bound to VHL<\/figcaption><\/figure>\n\n\n\n
\"Table
Table of content graphics<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 1. Initial optimization strategy<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 2. Biophysical characterization of inhibitor 10 binding to VBC.<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 3. Co-crystal structures of first-series inhibitors<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 4. Cellular activity and toxicity of 10<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 5. Second series optimization strategy.<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 6. Inhibitor 15 is not cytotoxic.<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 7. Co-crystal structures of second-series inhibitors<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 8. Correlations between cellular activity and physicochemical parameters in vitro<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 9. Activity in cells vs half-life dissociation from VBC protein complex.<\/figcaption><\/figure>\n\n\n\n
\"Scheme
Scheme 1<\/figcaption><\/figure>\n\n\n\n
\"Scheme
Scheme 2<\/figcaption><\/figure>\n\n\n\n
\"Scheme
Scheme 3<\/figcaption><\/figure>\n<\/figure>\n\n\n\n


<\/p>\n\n\n\n

<\/p>\n","protected":false},"excerpt":{"rendered":"

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}]}}