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Articles by Simon Messing
Structural mechanisms underlying resistance to Switch-II pocket inhibitors in KRAS
Abstract Direct targeting of KRAS through the Switch-II pocket is an effective therapeutic strategy, but acquired resistance limits clinical benefit. We examine clinically observed resistance mutations (R68S, H95Q, Y96C, Y96D and Q99L) arising during KRAS G12C inhibitor therapy using biochemical, structural, computational and cellular approaches. Covalent and noncovalent binding measurements reveal mutation- and inhibitor-specific reductions in drug engagement across inhibitor classes.
Disulfide tethering reveals cryptic pockets in oncogenic KRAS
Abstract Disulfide tethering is a site-directed method of drug discovery used to identify hits for challenging targets. We applied tethering to target oncogenic KRAS, a small GTPase once considered undruggable due to its high nucleotide affinity and a perceived absence of binding sites. We prepared a library of 2160 disulfide-containing fragments.
Structural insights into isoform-specific RAS-PI3Kα interactions and the role of RAS in PI3Kα activation - Nature Communications
Abstract Mutations in RAS and PI3Kα are major drivers of human cancer. Their interaction plays a crucial role in activating PI3Kα and amplifying the PI3K-AKT-mTOR pathway. Disrupting RAS-PI3Kα interaction enhances survival in lung and skin cancer models and reduces tumor growth and angiogenesis, although the structural details of this interaction remain unclear.
Abstract A10: Quantitative biophysical analysis defining key components modulating KRAS recruitment to the plasma membrane
Poster Presentations - Proffered Abstracts Bindu Lakshman, Simon Messing, Eva M. Schmid, Jeffrey D. Clogston, William K. Gillette, Dominic Esposito, Bailey Kessing, Daniel A. Fletcher, Dwight V. Nissley, Frank McCormick, Andrew G. Stephen and Frantz L.
Quantitative biophysical analysis defines key components modulating recruitment of the GTPase KRAS to the plasma membrane
Bindu Lakshman‡, Simon Messing‡, Eva M. Schmid§, Jeffrey D. Clogston¶, William K. Gillette‡, Dominic Esposito‡, Bailey Kessing‡, Daniel A. Fletcher§,‖,**, Dwight V. Nissley‡, Frank McCormick‡,‡‡, Andrew G. Stephen‡ and Frantz L.
Quantitative biophysical analysis defines key components modulating recruitment of the GTPase KRAS to the plasma membrane
Author contributions: B.L., S.M., E.M.S., J.D.C., W.K.G., D.E., D.A.F., F.M., and F.L.J.-F. conceptualization; B.L., S.M., E.M.S., J.D.C., W.K.G., and F.L.J.-F. data curation; B.L., E.M.S., J.D.C., and F.L.J.-F. formal analysis; B.L., S.M., E.M.S., and J.D.C. investigation; B.L. and F.L.J.-F. methodology; E.M.S., J.D.C., W.K.G., D.E., D.V.N., F.M., A.G.S., and F.L.J.-F. writing-review and editing; W.K.G., D.E., D.A.F., D.V.N., F.M., A.G.S., and F.L.J.-F.
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