RH Logo
Hubs
About
Live
Leaderboard

My Hubs
All

Trending Papers in Biochemistry

Trending
Today
Trending
Today

Sign in to discover all of the research papers you care about, live as they're published.

4
Date Added: May 3, 2021
Authors: Gabriele Colozza, Bon‐Kyoung Koo
Date Added: May 3, 2021
Authors: Gabriele Colozza, Bon‐Kyoung Koo
2
Date Added: Apr 14, 2021
Date Added: Apr 14, 2021
Son of Sevenless (SOS) is a guanine nucleotide exchange factor that activates the important cell signaling switch KRAS. SOS acts as a pacemaker for KRAS, the beating heart of cancer, by catalyzing the “beating” from the KRAS(off) to the KRAS(on) conformation. Activating mutations in SOS1 are common in Noonan syndrome and oncogenic alterations in KRAS drive 1 in seven human cancers. Promising clinical efficacy has been observed for selective KRASG12C inhibitors, but the vast majority of oncogenic KRAS alterations remain undrugged. The discovery of a druggable pocket on SOS1 has led to potent SOS1 inhibitors such as BI-3406. SOS1 inhibition leads to antiproliferative effects against all major KRAS mutants. The first SOS1 inhibitor has entered clinical trials for KRAS-mutated cancers. In this review, we provide an overview of SOS1 function, its association with cancer and RASopathies, known SOS1 activators and inhibitors, and a future perspective is provided.
Load More Papers