{"id":184672,"date":"2024-03-09T02:45:55","date_gmt":"2024-03-09T08:45:55","guid":{"rendered":"https:\/\/lifeboat.com\/blog\/2024\/03\/pancreatic-cancer-drug-candidate-targets-elusive-but-common-k-ras-variant"},"modified":"2024-03-09T02:45:55","modified_gmt":"2024-03-09T08:45:55","slug":"pancreatic-cancer-drug-candidate-targets-elusive-but-common-k-ras-variant","status":"publish","type":"post","link":"https:\/\/lifeboat.com\/blog\/2024\/03\/pancreatic-cancer-drug-candidate-targets-elusive-but-common-k-ras-variant","title":{"rendered":"Pancreatic Cancer Drug Candidate Targets Elusive, but Common, K-Ras Variant"},"content":{"rendered":"

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

K-Ras mutations are all too familiar as drivers of cancer. And until recently, they were considered all but undruggable. But ever since the arrival of sotorasib and adagrasib\u2014two FDA-approved K-Ras-G12C inhibitors\u2014K-Ras mutations have had the distinction of being somewhat<\/em> druggable. Even better, K-Ras mutations may soon become yet more druggable. Scientists at the University of California, San Francisco, have found a way to target K-Ras-G12D mutations, which are especially prevalent in pancreatic ductal adenocarcinoma.<\/p>\n

The scientists were led by Kevan Shokat, PhD, a professor in the department of cellular and molecular pharmacology. Back in 2013, Shokat and colleagues developed the first K-Ras-G12C inhibitors. And today, in Nature Chemical Biology<\/em>, they present a paper (\u201cStrain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D<\/a>\u201d) describing how they designed a candidate drug that could help make pancreatic cancer, which is almost always fatal, a treatable and perhaps even curable condition.<\/p>\n

\u201c[Covalent] inhibition of G12D, the most frequent K-Ras mutation particularly prevalent in pancreatic ductal adenocarcinoma, has remained elusive due to the lack of aspartate-targeting chemistry,\u201d the article\u2019s authors wrote. \u201cHere we present a set of malolactone-based electrophiles that exploit ring strain to crosslink K-Ras-G12D at the mutant aspartate to form stable covalent complexes.\u201d<\/p>\n","protected":false},"excerpt":{"rendered":"

K-Ras mutations are all too familiar as drivers of cancer. And until recently, they were considered all but undruggable. But ever since the arrival of sotorasib and adagrasib\u2014two FDA-approved K-Ras-G12C inhibitors\u2014K-Ras mutations have had the distinction of being somewhat druggable. Even better, K-Ras mutations may soon become yet more druggable. Scientists at the University of [\u2026]<\/p>\n","protected":false},"author":662,"featured_media":0,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[11,19],"tags":[],"class_list":["post-184672","post","type-post","status-publish","format-standard","hentry","category-biotech-medical","category-chemistry"],"_links":{"self":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/posts\/184672","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/users\/662"}],"replies":[{"embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/comments?post=184672"}],"version-history":[{"count":0,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/posts\/184672\/revisions"}],"wp:attachment":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/media?parent=184672"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/categories?post=184672"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/tags?post=184672"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}