Tag: KRAS

LJI308 is a Pan-Ribosomal S6 Kinase (RSK) Inhibitor

The cold shock protein Y-box binding protein-1 (YB-1) is a multifunctional protein. It shows relations in cell proliferation, survival, and stress response. Through translation and transcription of key proteins and regulation of DNA repair, YB-1 performs its functions in different cancers. YB-1 displays overexpression in many tumor entities, especially...

SMAP-2 (DT-1154) is an Orally Bioavailable PP2A Activator

Protein Phosphatase 2A (PP2A) is a serine/threonine phosphatase. It regulates multiple signaling cascades implicated in cancer progression, including downstream effectors of KRAS. Inhibition of PP2A contributes to oncogenesis in multiple tumor types, highlighting the importance of this protein in maintaining normal kinase activity. Pancreatic ductal adenocarcinoma (PDA) cells have...

DT-061 is an Orally Active PP2A Activator

Protein phosphatase 2A (PP2A) comprises a family of serine/threonine phosphatases, minimally containing a well-conserved catalytic subunit. PP2A plays a prominent role in the regulation of specific signal transduction cascades. Additionally, PP2A interacts with a substantial number of other cellular and viral proteins. DT-061 is an orally bioavailable small-molecule activator...

BI-3406 is an Orally Active and Selective KRAS and SOS1 Interaction Inhibitor

KRAS functions as a molecular switch, cycling between inactive (GDP-bound) and active (GTP-bound) states to transduce extracellular signals via cell-surface receptors. KRAS signaling occurs through engagement with effector proteins that orchestrate intracellular signaling cascades regulating tumor cell survival and proliferation. Mutations in the KRAS gene occur in approximately one of seven...

Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor

ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription. MEK1/2 catalyze the phosphorylation of human...

LY3214996 an Orally Active ERK1/2 Inhibitor with Potential Antineoplastic Activity

The Ras/Raf/MEK/ERK signaling cascade integrates extracellular clues from cell surface receptors to gene expression and regulation of multiple cellular proteins. Extracellular-signal-regulated kinases (ERKs) serve as key central nodes within this pathway. Simultaneous targeting of multiple effectors such as RAF, MEK, and ERK offers the potential for enhanced efficacy while...

BI-2852 is the First Highly Potent KRAS Inhibitor for the SI/II Pocket

The three human RAS genes [KRAS, NRAS and HRAS] encode four RAS proteins, with two KRAS isoforms. The two KRAS isoforms arise from alternative RNA splicing KRAS4A and KRAS4B. The 3 human RAS genes belong to the protein family of small GTPases. GTPases function as binary molecular switches involved...