Anti-tumor efficacy of a potent and selective non-covalent KRAS[superscript G12D] inhibitor
Explore the source record for details and available documents.
Hallin, Jill↗
Engineering topics
Sullivan, Francis
Publications and source records attributed to Sullivan, Francis.
Discovery of ( S )-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1 H -pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1 H )-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development
The extracellular signal-regulated kinases ERK1/2 represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that is commonly activated by oncogenic mutations in BRAF or RAS or by upstream oncogenic signaling. While targeting upstream nodes with RAF and MEK inhibitors has proven effective clinically, resistance frequently develops through reactivation of the pathway. Simultaneous targeting of multiple nodes in the pathway, such as MEK and ERK, offers the prospect of enhanced efficacy as well as reduced potential for acquired resistance. Here, described herein is the discovery and characterization of GDC-0994 (22), an orally bioavailable small molecule inhibitor selective for ERK kinase activity.
60 APPLIED LIFE SCIENCES↗
A fast MPP algorithm for Ising spin exchange simulations
A very efficient massively parallel processor (MPP) algorithm is described for performing one important class of Ising spin simulations. Results and physical significance of MPP calculations using the method described is discussed elsewhere. A few comments, however, are made on the problem under study and results so far are reported. Ted Einstein provided guidance in interpreting the initial results and in suggesting calculations to perform.
Sullivan, Francis↗