Germanin (suramin)

In a protein-chip assay, actinomycete extract 4585DW showed PTP1B inhibitory activity comparable to the positive controls, suramin and vanadate. The extract was non-cytotoxic in mammalian and yeast cells and inhibited PTP1B with Km and Vmax values of 10.91 ± 0.50 mM and 0.02 ± 0.00 μmol/min, respectively. In conclusion, 4585DW is a promising candidate for further investigation as a PTP1B inhibitor.

Our findings demonstrate that suramin significantly attenuates inflammatory and oxidative damage in an experimental model of acute colitis. These results suggest that suramin may possess therapeutic potential in intestinal inflammation; however, this effect requires further support through advanced experimental and clinical studies.

This improvement in the somatosensory experience was reflected in alleviating depressive-like behavior in the forced swimming test. These findings highlight the therapeutic potential of blocking thalamic P2X receptors in alleviating fibromyalgia symptoms.

P2, N=45, Recruiting, Children's Hospital of Orange County | Not yet recruiting --> Recruiting

LDLR-OTNs demonstrated receptor-mediated uptake and potent cytotoxicity in LDLR- and FAS- overexpressing breast cancer cells. These findings support LDLR-targeted nanoparticles as a promising approach for delivering FAS inhibitors to LDLR-rich tumours, meriting further investigation in targeted cancer therapy development.

P2, N=45, Not yet recruiting, Children's Hospital of Orange County

The negative correlations between HMGA2 and thyroid-specific gene expressions were confirmed in a transgenic mouse model of PTC and in human PTC. Finally, we showed that HMGA2 inhibition by suramin reduced cell invasion and induced differentiation expression in vitro, indicating a new therapeutic strategy for treating thyroid cancer.

The broad-spectrum P2 receptor antagonist, suramin, P2X7 receptor-specific antagonist, oATP, P2Y6 receptor-specific antagonist, MRS 2578, and P2Y12 receptor-specific antagonist, AR-C 69931, all showed significant arrest in tumor growth...Disaggregated cells from AR-C 69931-treated tumors, when injected intravenously in naïve mice, did not exhibit metastasis in various tissues which was observed in mice injected with cells from saline-treated tumors. Our results show that blocking of P2 receptors is a therapeutic alternative to inhibit COX-2 expression, and thereby, arrest tumor progression and metastasis.

Suramin dramatically inhibited NIH ligation in the left common carotid artery (LCCA) vivo. Therefore, our results indicate that suramin protects against the development of pathological vascular remodelling by attenuating VSMCs proliferation, migration, and phenotypic transformation and may be used as a potential medicine for the treatment of NIH.

P=N/A, N=20, Not yet recruiting, The First Affiliated Hospital of Zhejiang University School of Medicine; The First Affiliated Hospital, Zhejiang University School of Medicine | Phase classification: P1 --> P=N/A

Suramin could inhibit NLRP3/caspase-1/GSDMD canonical pyroptosis pathway in LPS-induced MH-S alveolar macrophages.

Finally, we suggested the top-ranked six drug molecules (Suramin, Rifaximin, Telmisartan, Tukysa Tucatinib, Lynparza Olaparib, and TG.02) for the treatment of BC by molecular docking analysis with the proposed HubGs-mediated receptors. Molecular docking analysis results also showed that these drug molecules may inhibit cancer-related post-translational modification (PTM) sites (Succinylation, phosphorylation, and ubiquitination) of hub proteins. This study's findings might be valuable resources for diagnosis, prognosis, and therapies at an earlier stage of BC.