Development of son of sevenless homologue 1 (SOS1) modulators to treat cancers by regulating RAS signaling

G Luo, B Wang, Q Hou, X Wu - Journal of Medicinal Chemistry, 2023 - ACS Publications
Son of sevenless homologue 1 (SOS1) protein is universally expressed in cells and plays an
important role in the RAS signaling pathway. Specifically, this protein interacts with RAS in …

Targeting the RAS upstream and downstream signaling pathway for cancer treatment

MA Hossain - European Journal of Pharmacology, 2024 - Elsevier
Cancer often involves the overactivation of RAS/RAF/MEK/ERK (MAPK) and PI3K-Akt-mTOR
pathways due to mutations in genes like RAS, RAF, PTEN, and PIK3CA. Various strategies …

Critical requirement of SOS1 for tumor development and microenvironment modulation in KRASG12D-driven lung adenocarcinoma

FC Baltanás, R García-Navas… - Nature …, 2023 - nature.com
The impact of genetic ablation of SOS1 or SOS2 is evaluated in a murine model of
KRASG12D-driven lung adenocarcinoma (LUAD). SOS2 ablation shows some protection …

Inhibition of son of sevenless homologue 1 (SOS1): promising therapeutic treatment for KRAS-mutant cancers

T Chen, X Tang, Z Wang, F Feng, C Xu, Q Zhao… - European Journal of …, 2023 - Elsevier
Kristen rat sarcoma (KRAS) is one of the most common oncogenes in human cancers. As a
guanine nucleotide exchange factor, Son of Sevenless Homologue 1 (SOS1) represents a …

Current advances and development strategies of targeting son of sevenless 1 (SOS1) in drug discovery

J Wu, X Li, C Wu, Y Wang, J Zhang - European Journal of Medicinal …, 2024 - Elsevier
Abstract The Son of Sevenless 1 (SOS1) guanine nucleotide exchange factor, prevalent
across eukaryotic species, plays a pivotal role in facilitating the attachment of RAS protein to …

An overview of recent advancements in small molecules suppression of oncogenic signaling of K-RAS: an updated review

A Sabt, HO Tawfik, EF Khaleel, RM Badi… - Molecular Diversity, 2024 - Springer
RAS (rat sarcoma) oncoproteins are crucial for the growth of some human cancers, including
lung, colorectal, and pancreatic adenocarcinomas. The RAS family contains three known …

Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido [2, 3-d] pyrimidin-7-one-based SOS1 inhibitor

K Wang, Z Zhou, X Ma, J Xu, W Xu, G Zhou… - Bioorganic & Medicinal …, 2024 - Elsevier
Oncogenic KRAS mutations drive an approximately 25% of all human cancers. Son of
Sevenless 1 (SOS1), a critical guanine nucleotide exchange factor, catalyzes the activation …

DNMT1/miR-152-3p/SOS1 signaling axis promotes self-renewal and tumor growth of cancer stem-like cells derived from non-small cell lung cancer

Q Yuan, R Wang, X Li, F Sun, J Lin, Z Fu, J Zhang - Clinical Epigenetics, 2024 - Springer
Abstract Background CSLCs (Cancer stem cell-like cells), which are central to
tumorigenesis, are intrinsically influenced by epigenetic modifications. This study aimed to …

An updated patent review of SOS1 inhibitors (2022–present)

G Zhou, C Zhou, X Ma, J Xu, Z Zhou, T Xu… - Expert Opinion on …, 2024 - Taylor & Francis
Introduction SOS1 is a crucial guanine nucleotide exchange factor for KRAS. It facilitates the
transition of KRAS from inactive GDP-bound state to active GTP-bound state. The activation …

Lead Identification of Novel Naphthyridine Derivatives as Potent SOS1 Inhibitors

D Li, Q **e, M Yang, Y Cai, K Sun, S Jiang… - ACS Medicinal …, 2024 - ACS Publications
SOS1, a guanine nucleotide exchange factor (GEF), plays a critical role in catalyzing the
conversion of KRAS from its GDP-to GTP-bound form, regardless of KRAS mutation status …