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Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 1333 | 2p22.1 | SOS1 | SOS Ras/Rac guanine nucleotide exchange factor 1 | |
Mouse | - | 1319 | 17 50.67 cM | Sos1 | SOS Ras/Rac guanine nucleotide exchange factor 1 | |
Rat | - | 1319 | 6q11 | Sos1 | SOS Ras/Rac guanine nucleotide exchange factor 1 |
Previous and Unofficial Names ![]() |
GF1 | gingival fibromatosis, hereditary, 1 (GINGF) | HGF | son of sevenless homolog 1 (Drosophila) | SOS-1 |
Database Links ![]() |
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ChEMBL Target | CHEMBL2079846 (Hs) |
Ensembl Gene | ENSG00000115904 (Hs), ENSMUSG00000024241 (Mm), ENSRNOG00000007106 (Rn) |
Entrez Gene | 6654 (Hs), 20662 (Mm), 313845 (Rn) |
Human Protein Atlas | ENSG00000115904 (Hs) |
KEGG Gene | hsa:6654 (Hs), mmu:20662 (Mm), rno:313845 (Rn) |
OMIM | 182530 (Hs) |
Pharos | Q07889 (Hs) |
RefSeq Nucleotide | NM_005633 (Hs), NM_009231 (Mm), NM_001100716 (Rn) |
RefSeq Protein | NP_005624 (Hs), NP_033257 (Mm), NP_001094186 (Rn) |
UniProtKB | Q07889 (Hs), Q62245 (Mm) |
Wikipedia | SOS1 (Hs) |
Selected 3D Structures ![]() |
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Other Binding Ligands | |||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||
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Immuno Process Associations | |||||||||||||||
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General Comments |
SOS1 is a guanine nucleotide exchange factor that regulates the activation state of RAS GTPases. When the RAS/SOS1 complex forms RAS can reload with GTP and is activated. Inhibition of RAS/SOS1 formation prevents reloading with GTP and blocks RAS pathway activation. Blocking the RAS/SOS1 interaction using small-molecules is being explored as a novel antiproliferative mechanism [1,3-4]. Of particular interest in cancer would be the ability to inhibit SOS1 interaction with the KRASG12C oncogenic mutant which drives proliferation in many human cancers [2]. |
1. Burns MC, Howes JE, Sun Q, Little AJ, Camper DV, Abbott JR, Phan J, Lee T, Waterson AG, Rossanese OW et al.. (2018) High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling. Anal. Biochem., 548: 44-52. [PMID:29444450]
2. Hillig RC, Sautier B, Schroeder J, Moosmayer D, Hilpmann A, Stegmann CM, Werbeck ND, Briem H, Boemer U, Weiske J et al.. (2019) Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction. Proc. Natl. Acad. Sci. U.S.A., 116 (7): 2551-2560. [PMID:30683722]
3. Lu S, Jang H, Zhang J, Nussinov R. (2016) Inhibitors of Ras-SOS Interactions. ChemMedChem, 11 (8): 814-21. [PMID:26630662]
4. Winter JJ, Anderson M, Blades K, Brassington C, Breeze AL, Chresta C, Embrey K, Fairley G, Faulder P, Finlay MR et al.. (2015) Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation. J. Med. Chem., 58 (5): 2265-74. [PMID:25695162]
Rho GEFs: SOS Ras/Rac guanine nucleotide exchange factor 1. Last modified on 09/09/2019. Accessed on 01/03/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3096.