{"id":10619,"date":"2003-02-01T09:46:53","date_gmt":"2003-02-01T09:46:53","guid":{"rendered":"http:\/\/i-base.info\/htb\/?p=10619"},"modified":"2014-05-28T16:52:07","modified_gmt":"2014-05-28T16:52:07","slug":"t-20-a-model-for-novel-anti-hiv-drugs-in-development","status":"publish","type":"post","link":"https:\/\/i-base.info\/htb\/10619","title":{"rendered":"T-20: a model for novel anti-HIV drugs in development"},"content":{"rendered":"<p><strong>Jeffrey Laurence<br \/>\n<\/strong>from The AIDS Reader<\/p>\n<p><strong>In September of 1993, Drs Wild, Greenwell, and Matthews of Duke University published a letter in an AIDS research journal describing a synthetic peptide directed against the gp41 transmembrane portion of the HIV envelope, which appeared to have remarkable antiviral activity in vitro.<\/strong><\/p>\n<p>This 36-amino acid peptide, corresponding to residues 643 to 678 of the HIV-1LAI isolate, was originally designated DP-178. It later became known as T-20. Renamed enfuvirtide (Fuzeon) by its clinical developers at Trimeris and Roche, it belongs to a new family of antiretroviral drugs that inhibit HIV entry.<\/p>\n<p>As noted in the original publication, the 50% inhibitory concentration of T-20 for HIV-1-mediated cell fusion, assessed by syncytia formation, was 0.4 nmol\/L (1.7 ng\/mL). This is very low, and unprecedented for a peptide. The area of gp41 against which it was directed shows limited genetic variability, and this variance did not appear to affect function. Specificity was illustrated by the fact that three-fold higher log concentrations of T-20 were required to block HIV-2 entry into target cells.<\/p>\n<p>The conclusion of that original brief study was that T-20 \u201ccould serve as a lead compound in the discovery of both peptide- and nonpeptide-based drug candidates.\u201d That turned out to be an understatement.<\/p>\n<p>Full text at: <a href=\"http:\/\/www.medscape.com\/viewarticle\/444890\"><br \/>\nhttp:\/\/www.medscape.com\/viewarticle\/444890<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>Jeffrey Laurence from The AIDS Reader In September of 1993, Drs Wild, Greenwell, and Matthews of Duke University published a letter in an AIDS research journal describing a synthetic peptide directed against the gp41 transmembrane portion of the HIV envelope, &hellip;<\/p>\n","protected":false},"author":4,"featured_media":0,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[30],"tags":[],"class_list":["post-10619","post","type-post","status-publish","format-standard","hentry","category-on-the-web"],"_links":{"self":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts\/10619","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/users\/4"}],"replies":[{"embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/comments?post=10619"}],"version-history":[{"count":0,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts\/10619\/revisions"}],"wp:attachment":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/media?parent=10619"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/categories?post=10619"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/tags?post=10619"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}