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DRUG CLASS:

Protein tyrosine phosphatase inhibitor

26d
Trial completion
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BRAF (B-raf proto-oncogene)
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BRAF mutation • BRAF V600
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Libtayo (cemiplimab-rwlc) • BNT111
1m
Integrative analysis of single-cell and bulk transcriptomes reveals metabolic heterogeneity and identifies PFKP as a therapeutic target in cervical cancer. (PubMed, Biochim Biophys Acta Mol Basis Dis)
Moreover, we demonstrated that Suramin effectively suppressed CC tumor growth by inhibiting PFKP-mediated glycolysis. Our findings provide a robust prognostic model and disclose PFKP as a potential therapeutic target in CC, offering insightful guidance on cancer management of CC patients.
Journal
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CD123 (Interleukin 3 Receptor Subunit Alpha) • TPM3 (Tropomyosin 3) • IL3RA (Interleukin 3 Receptor Subunit Alpha) • PFKP (Phosphofructokinase, Platelet)
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Germanin (suramin)
4ms
A Phase I Safety Study of NVG-291 in Healthy Adults (ACTRN12621000303842)
P1, N=74, Completed, NervGen Pharma Corp. | Recruiting --> Completed
Trial completion
7ms
Screening of Protein Tyrosine Phosphatase 1B Inhibitors from Actinomycete Extracts Using Recombinant Saccharomyces cerevisiae. (PubMed, J Microbiol Biotechnol)
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.
Preclinical • Journal
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PTPN1 (Protein Tyrosine Phosphatase Non-Receptor Type 1) • LEP (Leptin)
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Germanin (suramin)
8ms
Trial completion date
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BRAF (B-raf proto-oncogene)
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BRAF mutation • BRAF V600
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Libtayo (cemiplimab-rwlc) • BNT111
8ms
Suramin Exerts an Ameliorative Effect on Acetic Acid-Induced Acute Colitis in Rats by Demonstrating Potent Antioxidant and Anti-Inflammatory Properties. (PubMed, Medicina (Kaunas))
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.
Preclinical • Journal
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TNFA (Tumor Necrosis Factor-Alpha)
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Germanin (suramin)
9ms
Possible Interaction of Suramin with Thalamic P2X Receptors and NLRP3 Inflammasome Activation Alleviates Reserpine-Induced Fibromyalgia-Like Symptoms. (PubMed, J Neuroimmune Pharmacol)
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.
Journal
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TNFA (Tumor Necrosis Factor-Alpha) • CD163 (CD163 Molecule) • IL10 (Interleukin 10) • NLRP3 (NLR Family Pyrin Domain Containing 3) • CD86 (CD86 Molecule)
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Germanin (suramin)
9ms
Enrollment open
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Germanin (suramin)
10ms
LDLR-targeted orlistat therapeutic nanoparticles: Peptide selection, assembly, characterization, and cell-uptake in breast cancer cell lines. (PubMed, Int J Pharm)
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.
Preclinical • Journal
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FASN (Fatty acid synthase) • LDLR (Low Density Lipoprotein Receptor)
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Germanin (suramin)
10ms
Centromere protein A knockdown inhibits rectal cancer through O6-methylguanine DNA methyltransferase/protein tyrosine phosphatase nonreceptor type 4 axis. (PubMed, World J Gastrointest Oncol)
CENPA knockdown inhibited rectal cancer cell growth and attenuated xenograft tumor growth through regulating the MGMT/PTPN4 axis.
Journal
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MGMT (6-O-methylguanine-DNA methyltransferase) • DNMT1 (DNA methyltransferase 1) • CENPA (Centromere protein A)
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MGMT promoter methylation
11ms
New P2 trial
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Germanin (suramin)
11ms
HMGA2 Overexpression in Papillary Thyroid Cancer Promotes Thyroid Cell Dedifferentiation and Invasion, and These Effects Are Counteracted by Suramin. (PubMed, Int J Mol Sci)
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.
Journal
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HMGA2 (High mobility group AT-hook 2)
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Germanin (suramin)