{"id":4844,"date":"2016-07-08T15:04:49","date_gmt":"2016-07-08T22:04:49","guid":{"rendered":"http:\/\/blogs.reed.edu\/chemistry_news\/?p=4844"},"modified":"2016-07-08T15:05:32","modified_gmt":"2016-07-08T22:05:32","slug":"kevan-shokat-86-finding-a-pathway-for-kras-inhibition","status":"publish","type":"post","link":"https:\/\/blogs.reed.edu\/chemistry_news\/2016\/07\/kevan-shokat-86-finding-a-pathway-for-kras-inhibition\/","title":{"rendered":"Kevan Shokat ’86 Finding a Pathway for KRas Inhibition"},"content":{"rendered":"

Wikipedia:<\/em><\/a> The protein product of the KRas gene performs an essential function in normal tissue signaling: it acts as a molecular on\/off switch. In the ‘on’ position, KRas recruits and activates proteins necessary for the propagation of growth factor and other signaling pathways, however, the mutation of a KRas gene also happens to be an essential step in the development of many cancers.<\/p>\n

C&EN (6 June 2016, cover story<\/a>):<\/em> “KRas, part of a family of proteins commonly mutated in cancer, is one of the most desirable drug targets in the pharmaceutical industry. It is also one of the most maddeningly difficult targets; after a long period of failures, many scientists simply stopped trying to develop drugs that block KRas.”<\/p>\n

The C&EN cover story also describes how the first real break in the KRas story came in December 2011, when Dr. Ulf Peters<\/strong>, a postdoc in the Shokat<\/a> lab at UC San Francisco, was able to determine an x-ray structure of a KRas-small molecule complex. Peters sent the coordinates to Shokat by email, but what he didn’t know was this: Shokat had been caught in an early winter Lake Tahoe snowstorm, and was stuck in his car at the bottom of a slick, steep hill. Finally, once this obstacle had been overcome, and Shokat had located a computer, he was able to download Peters’ 3-D structure, which struck him as, “just, like, unbelievable.” The structure revealed a previously unknown “shallow pocket” that functioned as an allosteric binding site, and it gave Shokat’s team the toehold it needed to design the first covalent inhibitor of the KRas protein.<\/p>\n","protected":false},"excerpt":{"rendered":"

Wikipedia: The protein product of the KRas gene performs an essential function in normal tissue signaling: it acts as a molecular on\/off switch. In the ‘on’ position, KRas recruits and activates proteins necessary for the propagation of growth factor and … finish reading Kevan Shokat ’86 Finding a Pathway for KRas Inhibition<\/a><\/p>\n","protected":false},"author":55,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[3],"tags":[],"class_list":["post-4844","post","type-post","status-publish","format-standard","hentry","category-alumni"],"_links":{"self":[{"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/posts\/4844","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/users\/55"}],"replies":[{"embeddable":true,"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/comments?post=4844"}],"version-history":[{"count":4,"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/posts\/4844\/revisions"}],"predecessor-version":[{"id":4848,"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/posts\/4844\/revisions\/4848"}],"wp:attachment":[{"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/media?parent=4844"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/categories?post=4844"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/blogs.reed.edu\/chemistry_news\/wp-json\/wp\/v2\/tags?post=4844"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}