Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State.

By M. Patricelli, M. R. Janes, Lian-Sheng Li, R. Hansen, U. Peters, L. Kessler, YuChing Chen, Jeff M. Kucharski, Jun Feng, T. Ely and 5 more. Cancer Discovery, 2016

613 citations recorded by the source corpus.

Subfields: Molecular Biology

View Paper: https://www.semanticscholar.org/paper/6127bb309880e730b075fa27ca457400b82d5817

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In Molecular Biology

1. Stefano Forli
2. Bruno E. Correia
3. Stephen W. Fesik
4. Roderick E. Hubbard
5. Arthur J. Olson
6. B. Cravatt
7. K. Yu
8. Abdo A. Elfiky

Citations in the corpus

• Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor. (2018, methodology): “Consistent with other S-IIP KRAS inhibitors mode of action (Ostrem et al., 2013; Patricelli et al., 2016), ARS-1620 preferentially engages the GDP nucleotide-bound state of KRAS and lacks detectable reactivity on any residue of wild-type (WT)-KRAS protein (Figure 2E).”
• Proteome-wide covalent ligand discovery in native biological systems (2016, background): “One fragment (11) marked in red showed notably lower reactivity in situ versus in vitro.”
• Twenty years on: the impact of fragments on drug discovery (2016, background): “5) , and some of these have been optimized to cell-active molecules 102 .”