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SIPA1 inhibitor
- Development stage
- Preclinical
- Lead developer
- Kyoto University
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Aerosol, Parenteral, Subcutaneous, Intravenous, Intramuscular, Intraarterial, Intrathecal, Intraperitoneal, Rectal
01
Overview
SIPA1 (Signal-induced proliferation-associated gene 1) inhibitors are a class of therapeutic agents designed to target the Rap1 GTPase-activating protein SIPA1. SIPA1 is a critical regulator of the tumor microenvironment (TME), specifically controlling the differentiation of mesenchymal stromal cells (MSCs) into cancer-associated fibroblasts (CAFs). Inhibition or deficiency of SIPA1 reprograms MSCs from a myofibroblastic phenotype (myCAF) toward an inflammatory, immunostimulatory phenotype (iCAF) that produces CXCL9 and enhances T-cell recruitment. Furthermore, SIPA1 negatively regulates the IFNγ-STAT1 signaling axis by directly interacting with STAT1 and suppressing its activation. By blocking SIPA1, these inhibitors aim to enhance anti-tumor immunity and improve the efficacy of cancer immunotherapies in various malignancies, including epithelial cancers and leukemia.
- Other names
- Sipa1 inhibitorSipa-1 inhibitorSipa 1 inhibitor
02
Targets
SIPA1 (Signal-induced proliferation-associated gene 1)
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