Preferred Label : SOS1 Inhibitor KQB198;
NCIt definition : An orally available inhibitor of the guanine nucleotide exchange factor (GEF) Son
of sevenless homolog 1 (SOS1), with potential antineoplastic activity. Upon oral administration,
SOS1 inhibitor KQB198 selectively targets and binds to SOS1, thereby preventing the
interaction of SOS1 with Kirsten rat sarcoma viral oncogene homolog (KRAS) in the
guanosine diphosphate (GDP)-bound 'off' state, which is the inactivated state of KRAS.
This abrogates the exchange of RAS-bound GDP for guanosine triphosphate (GTP) and
prevents the formation of GTP-loaded KRAS, which is the activated 'on' state of KRAS.
This prevents activation of downstream RAF/mitogen-activated protein kinase kinase
(MEK)/extracellular signal-regulated kinase (ERK) signaling pathway by GTP-loaded
KRAS. This inhibits mutant KRAS-dependent signaling and may inhibit growth and survival
of KRAS-expressing tumor cells. KRAS is a member of the RAS family of oncogenes that
is mutated in many cancer cell types. Mutations of KRAS may induce constitutive signal
transduction leading to tumor cell proliferation, survival, invasion, and metastasis.
SOS1 regulates the KRAS GDP-GTP cycle and promotes nucleotide exchange and formation
of 'active' KRAS-GTP.;
Molecule name : KQB 198; KQB-198;
Origin ID : C211867;
concept_is_in_subset
- has_target
