6EPN

Ras guanine exchange factor SOS1 (Rem-cdc25) in complex with KRAS(G12C) and fragment screening hit F2

Summary for 6EPN

• Entry DOI: 10.2210/pdb6epn/pdb
• Related: 6EPL 6EPM 6EPO 6EPP
• Descriptor: GTPase KRas, Son of sevenless homolog 1, GLYCEROL, ... (6 entities in total)
• Functional Keywords: guanine nucleotide exchange factor, gef, fragment screen, gtpase, signaling protein
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 76851.59

Authors

Hillig, R.C.,Moosmayer, D.,Hilpmann, A.,Bader, B.,Schroeder, J.,Wortmann, L.,Sautier, B.,Kahmann, J.,Wegener, D.,Briem, H.,Petersen, K.,Badock, V. (deposition date: 2017-10-12, release date: 2019-02-06, Last modification date: 2024-01-17)

• Primary citation: Hillig, R.C.,Sautier, B.,Schroeder, J.,Moosmayer, D.,Hilpmann, A.,Stegmann, C.M.,Werbeck, N.D.,Briem, H.,Boemer, U.,Weiske, J.,Badock, V.,Mastouri, J.,Petersen, K.,Siemeister, G.,Kahmann, J.D.,Wegener, D.,Bohnke, N.,Eis, K.,Graham, K.,Wortmann, L.,von Nussbaum, F.,Bader, B.; Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.; Proc. Natl. Acad. Sci. U.S.A., 116:2551-2560, 2019; PubMed: 30683722; DOI: 10.1073/pnas.1812963116

Experimental method

X-RAY DIFFRACTION (2.5 Å)