8uh0
From Proteopedia
(Difference between revisions)
| Line 12: | Line 12: | ||
== Function == | == Function == | ||
[https://www.uniprot.org/uniprot/SOS2_HUMAN SOS2_HUMAN] Promotes the exchange of Ras-bound GDP by GTP.[UniProtKB:Q62245] | [https://www.uniprot.org/uniprot/SOS2_HUMAN SOS2_HUMAN] Promotes the exchange of Ras-bound GDP by GTP.[UniProtKB:Q62245] | ||
| - | <div style="background-color:#fffaf0;"> | ||
| - | == Publication Abstract from PubMed == | ||
| - | SOS1 and SOS2 are guanine nucleotide exchange factors that mediate RTK-stimulated RAS activation. Selective SOS1:KRAS PPI inhibitors are currently under clinical investigation, whereas there are no reports to date of SOS2:KRAS PPI inhibitors. SOS2 activity is implicated in MAPK rebound when divergent SOS1 mutant cell lines are treated with the SOS1 inhibitor BI-3406; therefore, SOS2:KRAS inhibitors are of therapeutic interest. In this report, we detail a fragment-based screening strategy to identify X-ray cocrystal structures of five diverse fragment hits bound to SOS2. | ||
| - | |||
| - | Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.,Smith CR, Chen D, Christensen JG, Coulombe R, Fethiere J, Gunn RJ, Hollander J, Jones B, Ketcham JM, Khare S, Kuehler J, Lawson JD, Marx MA, Olson P, Pearson KE, Ren C, Tsagris D, Ulaganathan T, Van't Veer I, Wang X, Ivetac A J Med Chem. 2023 Dec 29. doi: 10.1021/acs.jmedchem.3c02140. PMID:38156904<ref>PMID:38156904</ref> | ||
| - | |||
| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 8uh0" style="background-color:#fffaf0;"></div> | ||
| - | == References == | ||
| - | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
Current revision
SOS2 co-crystal structure with fragment bound (compound 10)
| |||||||||||
