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- W2897527318 endingPage "511" @default.
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- W2897527318 abstract "RAS has long been viewed as undruggable due to its lack of deep pockets for binding of small molecule inhibitors. However, recent successes in the development of direct RAS inhibitors suggest that the goal of pharmacological inhibition of RAS in patients may soon be realized. This review will discuss the role of RAS in cancer, the approaches used to develop direct RAS inhibitors, and highlight recent successes in the development of novel RAS inhibitory compounds that target different aspects of RAS biochemistry. In particular, this review will discuss the different properties of RAS that have been targeted by various inhibitors including membrane localization, the different activation states of RAS, effector binding, and nucleotide exchange. In addition, this review will highlight the recent success with mutation-specific inhibitors that exploit the unique biochemistry of the RAS(G12C) mutant. Although this mutation in KRAS accounts for 11% of all KRAS mutations in cancer, it is the most prominent KRAS mutant in lung cancer suggesting that G12C-specific inhibitors may provide a new approach for treating the subset of lung cancer patients harboring this mutant allele. Finally, this review will discuss the involvement of dimerization in RAS function and highlight new approaches to inhibit RAS by specifically interfering with RAS:RAS interaction." @default.
- W2897527318 created "2018-10-26" @default.
- W2897527318 creator A5084266690 @default.
- W2897527318 date "2019-01-01" @default.
- W2897527318 modified "2023-09-30" @default.
- W2897527318 title "Pharmacological targeting of RAS: Recent success with direct inhibitors" @default.
- W2897527318 cites W1483388049 @default.
- W2897527318 cites W1492513673 @default.
- W2897527318 cites W1533781057 @default.
- W2897527318 cites W1549268831 @default.
- W2897527318 cites W1556741602 @default.
- W2897527318 cites W1558058709 @default.
- W2897527318 cites W1781950500 @default.
- W2897527318 cites W1914204293 @default.
- W2897527318 cites W1953264505 @default.
- W2897527318 cites W1958258471 @default.
- W2897527318 cites W1964551999 @default.
- W2897527318 cites W1967902354 @default.
- W2897527318 cites W1968401207 @default.
- W2897527318 cites W1970856032 @default.
- W2897527318 cites W1971102429 @default.
- W2897527318 cites W1975702431 @default.
- W2897527318 cites W1984857320 @default.
- W2897527318 cites W1985309852 @default.
- W2897527318 cites W1989510858 @default.
- W2897527318 cites W2001400574 @default.
- W2897527318 cites W2002036996 @default.
- W2897527318 cites W2002252224 @default.
- W2897527318 cites W2003625629 @default.
- W2897527318 cites W2004731962 @default.
- W2897527318 cites W2010207338 @default.
- W2897527318 cites W2010955929 @default.
- W2897527318 cites W2012479646 @default.
- W2897527318 cites W2016268789 @default.
- W2897527318 cites W2017960640 @default.
- W2897527318 cites W2024027456 @default.
- W2897527318 cites W2025499369 @default.
- W2897527318 cites W2033125632 @default.
- W2897527318 cites W2033204562 @default.
- W2897527318 cites W2034063805 @default.
- W2897527318 cites W2038027636 @default.
- W2897527318 cites W2043282329 @default.
- W2897527318 cites W2044210875 @default.
- W2897527318 cites W2047812331 @default.
- W2897527318 cites W2049662137 @default.
- W2897527318 cites W2051626784 @default.
- W2897527318 cites W2053737392 @default.
- W2897527318 cites W2058333572 @default.
- W2897527318 cites W2062983115 @default.
- W2897527318 cites W2066696278 @default.
- W2897527318 cites W2066784934 @default.
- W2897527318 cites W2068032848 @default.
- W2897527318 cites W2069269337 @default.
- W2897527318 cites W2069537707 @default.
- W2897527318 cites W2070023258 @default.
- W2897527318 cites W2070633164 @default.
- W2897527318 cites W2073460054 @default.
- W2897527318 cites W2073801668 @default.
- W2897527318 cites W2073967748 @default.
- W2897527318 cites W2075564766 @default.
- W2897527318 cites W2078936681 @default.
- W2897527318 cites W2080046842 @default.
- W2897527318 cites W2083506343 @default.
- W2897527318 cites W2083570813 @default.
- W2897527318 cites W2087523490 @default.
- W2897527318 cites W2088064651 @default.
- W2897527318 cites W2091169894 @default.
- W2897527318 cites W2092973995 @default.
- W2897527318 cites W2093323373 @default.
- W2897527318 cites W2093457556 @default.
- W2897527318 cites W2093965961 @default.
- W2897527318 cites W2098760239 @default.
- W2897527318 cites W2098806204 @default.
- W2897527318 cites W2105779105 @default.
- W2897527318 cites W2110719738 @default.
- W2897527318 cites W2111175126 @default.
- W2897527318 cites W2121393047 @default.
- W2897527318 cites W2121719392 @default.
- W2897527318 cites W2123551753 @default.
- W2897527318 cites W2128339707 @default.
- W2897527318 cites W2128392882 @default.
- W2897527318 cites W2130182381 @default.
- W2897527318 cites W2131037662 @default.
- W2897527318 cites W2135371328 @default.
- W2897527318 cites W2142454421 @default.
- W2897527318 cites W2143185290 @default.
- W2897527318 cites W2144265524 @default.
- W2897527318 cites W2146926552 @default.
- W2897527318 cites W2147687412 @default.
- W2897527318 cites W2148309992 @default.
- W2897527318 cites W2149344188 @default.
- W2897527318 cites W2151366572 @default.
- W2897527318 cites W2152561142 @default.
- W2897527318 cites W2162658068 @default.
- W2897527318 cites W2168770561 @default.
- W2897527318 cites W2171109371 @default.
- W2897527318 cites W2211890826 @default.
- W2897527318 cites W2233032895 @default.