IndraLab

Statements

SOS1 activates KRAS. 10 / 17
4 | 7 5
sparser
"In the absence of REM-bound allosteric KRas4B, SOS1 barely activates the catalytic KRas4B at CDC25."
30097175
reach
"ERK2-mediated phosphorylation of SOS1 on various sites (Ser1137/1167/1178/1193/1197) disrupts the interaction between SOS1 and GRB2, rendering SOS1 non-functional and unable to promote K-RAS activation [4,5]."
35093302
signor
"Because the KRAS-GDP to KRAS-GTP transition catalyzed by the GEF, son of sevenless 1 (SOS1), represents the rate-limiting step for nucleotide exchange, disrupting the activating SOS1/KRAS protein interaction has also been the focus of drug development efforts"
25624485
reach
"Novel SOS1-directed inhibitors with a broader anticancer coverage such as BAY-293 and BI-3406 inhibit KRAS through the hindrance of SOS1-KRAS interactions."
34598083
signor
"Because the KRAS-GDP to KRAS-GTP transition catalyzed by the GEF, son of sevenless 1 (SOS1), represents the rate-limiting step for nucleotide exchange, disrupting the activating SOS1/KRAS protein interaction has also been the focus of drug development efforts"
25624485
sparser
"A parallel HTS screen of over 3 000 000 compounds using a fluorescent enzymatic assay identified a quinazoline series, such as 20 , which inhibited the activation of KRas by Sos1 with submicromolar affinity and was selective over other GEF/GTPase complexes and the interaction of KRas with its effector."
30869179
sparser
"Although both Sos1 and Ras-GRF1 activate the Ras proteins Ha-Ras, N-Ras, and Ki-Ras, only Ras-GRF1 also activates the functionally distinct R-Ras GTPase."
11560935
sparser
"By contrast, in the limited activation cycle, the allosteric KRas4B-GDP does not induce proper allosteric signals, impeding SOS1 activation of KRas4B. The binding free energies of the allosteric GDP- [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
30097175
signor
"Because the KRAS-GDP to KRAS-GTP transition catalyzed by the GEF, son of sevenless 1 (SOS1), represents the rate-limiting step for nucleotide exchange, disrupting the activating SOS1/KRAS protein interaction has also been the focus of drug development efforts"
25624485
reach
"As a GEF, SOS1 promotes K-RAS activation by enhancing GDP to GTP exchange, which occurs at the plasma membrane through recruitment by GRB2."
35093302