Germanin (suramin) / Optimum Therap - LARVOL DELTA

Exploratory transcriptomics and in vivo analyses of suramin in tongue squamous cell carcinoma. (PubMed, Biomed Rep) - "Effect size estimates were relatively large for both the group effect (partial η2=0.20) and the time x group interaction (partial η2=0.24), suggesting that the study may have been underpowered to detect this difference statistically. In conclusion, the present exploratory study suggests that suramin exerts a dual antitumor effect on tongue squamous cell carcinoma by suppressing proliferative transcriptional programs, and modulating extracellular and stress response pathways, providing a basis for future studies to further elucidate its therapeutic relevance."

Journal • Preclinical • Oncology • Oral Cancer • Squamous Cell Carcinoma • Tongue Carcinoma • AURKA • CCNB1 • CDC20 • FOXM1 • MYBL2 • TIMP3 • TNFSF10 • TXNIP

P2Y Receptors Mediate Inhibition of Acetylcholine Release at the Developing Efferent-Inner Hair Cell Synapse (ARO 2026) - "The quantal content (m) was estimated as the ratio between the mean amplitude of evoked synaptic currents and the mean amplitude of spontaneous synaptic currents...The general P2 antagonist, Suramin, abolished the effect of ATP... Our results suggest that both ATP and adenosine inhibit ACh release at the MOC-IHC synapse through the activation of P2Y and A1 receptors, respectively. These results suggest that ATP may have multiple roles in the developing cochlea."

Effects of N3SA Analogues on Cerebral and Peripheral Arteriolar Vasomotion in Spontaneously Hypertensive Rats. (PubMed, Int J Mol Sci) - "To further support the relation between stabilizers anchored to NAPE-PLD and their beneficial effects on hypertension, we selected compound analogues of N3SA with chemical modifications at the three target-interacting sulfonic groups, including the drug Suramin...Findings showed that the minor structural differences in compounds correlated with the contribution of the six different frequency components affecting the arterial tone, as well as their vasodilatory effects, in both cerebral and femoral muscle arterioles. These results provide evidence that the spectra analysis of the regulation mechanisms of vascular tone and arterial blood pressure can accurately reflect the structure-activity correlations of different analogues of an antihypertensive compound."

Journal • Preclinical • Cardiovascular • Hypertension

Rational design and synthesis of new acetamide-indole-benzo[d]imidazole-carboxylic acid hybrids as dual PTP1B/α-glucosidase inhibitors. (PubMed, RSC Adv) - "The remaining compounds showed reduced efficacy relative to suramin. In contrast, only two compounds (8j and 8k) displayed marginally superior α-glucosidase inhibition compared to acarbose, while all other derivatives were less potent than the standard...Kinetic analysis of the most potent compound, 8l, confirmed a competitive inhibition mechanism against PTP1B. Molecular docking studies of the most active compounds yielded binding modes consistent with the in vitro activity, and molecular dynamics simulations further verified the stable binding of compound 8l within the PTP1B active site, supporting its potential as a lead PTP1B inhibitor."

Journal • PTPN1

Spinal P2X3 receptors blockade reverses paclitaxel-induced allodynia in rats. (PubMed, Purinergic Signal) - "Pharmacological blockade of spinal P2X3 and P2X2/3 receptors with Ro-51, TNP-ATP, and systemic suramin reversed allodynia in paclitaxel-treated rats. In conclusion, spinal P2X2/3 and P2X3 receptors have a significant role in allodynia to mechanical stimulation in paclitaxel-treated rats, regardless of sex. Therefore, the blockade of these receptors could be an alternative pharmacological target for alleviating sensory symptoms of paclitaxel-induced peripheral neuropathy in patients with cancer."

Journal • Preclinical • Oncology • Pain

Towards treatments targeting the gut to improve behavioural outcomes in autism spectrum disorder. (PubMed, J Neural Transm (Vienna)) - "Repurposed medications such as pimavanserin (an atypical antipsychotic) and the antiparasitic suramin are being trialled for treating irritable behaviours and impaired social interaction, respectively, in autism. NTI164 is a medicinal cannabis-derived biopharmaceutical undergoing clinical safety and efficacy trials for improving social communication and similarly, ML-004 is an investigational drug being assessed for treating social communication deficits. Two other repurposed medications previously utilised for schizophrenia; brexpiprazole and lumateperone, as well as AB-2004, a microbial metabolite sequestering agent (with proposed actions on gut function), are undergoing clinical trials to assess impacts on irritability associated with autism. We also outline emerging findings from clinical studies on the use of gut-targeted small molecules and bacteriophage therapy, prebiotics, probiotic supplementation and faecal microbiota transplantation (FMT), and their potential..."

Journal • Review • Autism Spectrum Disorder • CNS Disorders • Developmental Disorders • Gastrointestinal Disorder • Genetic Disorders • Mental Retardation • Psychiatry • Schizophrenia • Transplantation

Biomarkers. (PubMed, Alzheimers Dement) - "This study demonstrates that SV2A levels decrease while tau accumulations increase in AD brains with [3H]UCB-J and [18F]MK-6420 respectively, and our data is consistent with in vivo human PET imaging studies of SV2A and tau. We also showed that P2Y12R is decreased in AD brains with [3H]PSB-0413. Positive correlation between regional binding of the three tracers was shown in AD patients."

Biomarker • Journal • Alzheimer's Disease • CNS Disorders • LPAR6

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."

Heterogeneity • Journal • Cervical Cancer • Gynecologic Cancers • Metabolic Disorders • Oncology • Solid Tumor • CD123 • IL3RA • PFKP • TPM3

Engineering Inhalable Carboxymethyl Chitosan-Swellable Microgels for Pulmonary Delivery of Charged Hydrophilic Molecules. (PubMed, Gels) - "Cell viability assays demonstrated >85% viability up to 100 µM suramin, suggesting that CMC-leucine microgels enable efficient pulmonary delivery of hydrophilic drugs by combining respirable dry-state properties with in situ swelling and reducing immunological clearance. Future in vivo studies will be needed to assess long-term stability, macrophage interaction, and the translational potential of this delivery system."

Journal

Mechanisms of ligand recognition and channel opening for P2X2 receptors in lipid nanodiscs. (PubMed, bioRxiv) - "Here we report cryo-EM structures of the human P2X2R in lipid nanodiscs in an apo closed state, with ATP 4- , Mg-ATP 2- and suramin bound...A continuous belt of partially resolved lipids in the outer leaflet stabilizes the closed state, and the presence of lipids prevents the severing of subunit interfaces as the channel opens. These findings establish key mechanistic principles of gating for P2X2R in a membrane-like environment, providing a framework for future mechanistic studies and therapeutic development."

Journal

GPER1 Activation Regulates Renal Purinergic P2Y2 Receptor Natriuretic Pathway. (PubMed, Am J Physiol Regul Integr Comp Physiol) - "Furthermore, P2 receptor blockade by suramin blocked GPER1-evoked natriuresis. These findings indicate that GPER1 upregulates the natriuretic Cx30/ATP/P2Y2 receptor signaling pathway in the kidney which may contribute to the blood pressure lowering response to GPER1 activation."

Journal • Cardiovascular • Hypertension • GJB6 • GPER1

Ionic agarose derivatives as polyelectrolytic additives for drug release. (PubMed, Carbohydr Polym) - "Incorporating ionic agarose derivatives into these materials proved to effectively reduce the burst release and sustain the release of adenosine triphosphate (ATP), suramin, methylene blue, and A740003 over a time of 14 days. The release curves were evaluated using established models as well as two novel Langmuir-like models. Especially the latter two offered additional insight into the release and yielded higher scores in Akaike's Information Criterion rankings than commonly used models."

Journal

Mechanism-informed identification of FDA-approved topoisomerase inhibitors disrupting SARS-CoV-2 nucleocapsid-RNA interactions. (PubMed, BMC Chem) - "Inspired by adenosine triphosphate (ATP)'s competitive inhibition of NP-RNA binding, we screened 121 FDA-approved ATP-competitive kinase inhibitors, identifying mitoxantrone (IC₅₀ = 1.22 µM) as a potent inhibitor. Considering its known topoisomerase inhibitory activity, we further screened 23 additional topoisomerase inhibitors, uncovering four active compounds-pixantrone (IC₅₀ = 5.67 µM), doxorubicin (IC₅₀ = 20.19 µM), epirubicin (IC₅₀ = 7.23 µM), and suramin (IC₅₀ = 0.44 µM)...Our findings demonstrate the feasibility of a mechanism-informed repurposing strategy and identify FDA-approved topoisomerase inhibitors and suramin as valuable chemical starting points. Although these compounds are not directly suitable as antivirals due to toxicity concerns, they provide promising scaffolds for further optimization aimed at selective disruption of SARS-CoV-2 NP-RNA interactions."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Suramin protects against chronic stress-induced neurobehavioral deficits via cGAS-STING/NF-κB suppression. (PubMed, Sci Rep) - "The level of corticosterone and neurotransmitters (dopamine and serotonin); various parameters of oxidative stress and neuroinflammation; acetylcholinesterase (AChE) activity and histological changes in hippocampus and cortex were also assessed. The results highlighted that administration of suramin (5, 10 and 20 mg/kg, i.p.) dose dependently improves neurobehavioral parameters, decreases corticosterone; elevates the level of neurotransmitters, and reduces the deleterious effects of CUS on oxidative stress and neuroinflammation; along with the histological improvement by inhibiting the cGAS-STING pathway and modulating NF-κB signaling as observed from decrease NF-κB levels in our study This study provides insights into suramin as a new treatment approach for mitigating the effects of chronic stress on restoring neurobehavioral changes."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Depression • Inflammation • Mood Disorders • Pain • Psychiatry • STING

Role of S1P- and Rho-kinase signalling in age-related myogenic tone deficiency in murine resistance arteries. (PubMed, Exp Physiol) - "The P2Y-receptor blocker suramin inhibited MT, whereas PPADS and apyrase did not...High-resolution microangiography confirmed that infusion of JTE-013 or KD025 (a Rho-kinase 2 inhibitor) preferentially dilated small (distal) CAs, and infusion of nifedipine (an L-type channel inhibitor) dilated all CAs in all mice, independent of age. SK and S1P2-R are crucially involved in pressure sensing in MT. RhoA/Rho-kinase signalling might be involved in age-related MT deficiency."

Journal • Preclinical • Alzheimer's Disease • Cardiovascular • CNS Disorders • RHOA

YopP modulates bacterial virulence and systemic dissemination in Peyer´s patches during murine Yersinia enterocolitica infection. (PubMed, Med Microbiol Immunol) - "Additionally, inhibition of cytotoxicity by suramin treatment in mice promoted wild-type Ye (Ye WT) dissemination to levels comparable to Ye ΔyopP...Blocking DC migration by FTY720 treatment in Ye ΔyopP-infected mice significantly reduced the MLN bacterial burden, indicating that YopP regulates Ye-transporting DCs from PP to MLN. Overall, our findings provide insights into how YopP participates in host-pathogen interactions, seemingly benefiting the host while simultaneously facilitating bacterial evasion from early immune clearance. These findings contribute to understanding the impact of YopP on the clinical outcome of Ye infection."

Journal • Preclinical • Gastroenterology • Gastrointestinal Disorder • Infectious Disease • Inflammation • IL10 • ITGAM

Epithelial cell signaling modulates responses of intrinsic primary afferent neurons of the mouse ileum to mechanical stimulation (Neuroscience 2025) - "To test the role of enterochromaffin cells, the same set of experiments were repeated with the addition of ondansetron (1 µM), GR 113808 (30nM), and suramin (500 µM)...Hex increased and Neo decreased immediate responses in submucosal neurons (Basal: Avil 19%/64%/17%, Hex: 29%/41%30%, Neo: 0%,25%,75%; p=0.006, Chi-square). Collectively, these results demonstrate mucosal mechanical receptive fields of IPANs that are modulated rather than mediated by neuroepithelial signaling of 5-HT, ATP, and acetylcholine."

Preclinical • CNS Disorders

Retraction: In vivo experiments demonstrate the potent antileishmanial efficacy of repurposed suramin in visceral leishmaniasis. (PubMed, PLoS Negl Trop Dis) - No abstract available

Journal • Preclinical • Infectious Disease

Extending Thioflavin T Fluorescence Probe to 2-Ethenyl-benzothiazole Derivatives: Drug-like Quadruplex Ligands with Potent Antitrypanosomatid Activity. (PubMed, ACS Infect Dis) - "In fact, compound 2b demonstrated superior efficacy and selectivity in comparison to the clinically used drugs suramin, fexinidazole, miltefosine, and amphotericin B. Biophysical studies revealed that all tested derivatives exhibited significant G4 stabilization, surpassing ThT. Location of compound 2b inside the nucleus and the kinetoplast, as well as partially in the mitochondria, opens up the possibility of 2b acting against the parasite through binding to G4."

Journal • Infectious Disease

Mechanism and therapeutic potential of purinergic receptor antagonism for treatment of cerebral malaria (ASTMH 2025) - "We have also found that suramin protects endothelial cells independently of calcium and cAMP, the canonical second messengers involved in purinergic receptor signaling, further pointing to alternative pathways of endothelial barrier enhancement. We will also perform RNA-sequencing to identify the cell signaling pathways that are modulated by suramin and further clarify how it protects brain endothelial cells from iRBC-mediated disruption."

CNS Disorders • Infectious Disease • Malaria • P2RY13

Rapamycin and Suramin Effects on TNF-⍺-Mediated Mast Cell and Brain Microvascular Endothelial Cell Dysfunction. (PubMed, Biotechnol Bioeng) - "However, suramin also increased intracellular BMEC levels of multiple pro-inflammatory cytokines. Neither rapamycin nor suramin improved the intracellular inflammatory profile of cocultured MCs, indicating that MC activation had not been resolved by either treatment."

Journal • Alzheimer's Disease • CNS Disorders • Inflammation • CCL2 • CCL3 • CSF2 • RPS6 • TNFA

Structural basis for suramin binding to the C-terminal domain of the SARS-CoV-2 nucleocapsid protein. (PubMed, Acta Biochim Biophys Sin (Shanghai)) - "Furthermore, ITC and EMSA experiments demonstrate that suramin can bind to the full-length N protein at multiple sites and dissociate RNA from the N protein. Taken together, these findings provide structural and biophysical insights into the mechanism of action of suramin and establish a rational basis for the development of targeted antiviral therapies against SARS-CoV-2."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Discovery of therapeutic AGC2 modulators by combining docking, binding, and vesicle-based transport assays. (PubMed, J Transl Med) - "This study establishes a reproducible, and scalable workflow that bridges high-throughput ligand identification with high-resolution kinetic characterization for targeting mitochondrial carriers."

Journal • Genetic Disorders • Oncology

Human African Trypanosomiasis (HAT): Epidemiology, Biological Diagnosis and Treatment: A Review. (PubMed, Acta Parasitol) - "All these difficulties raised raise questions about the need to develop new diagnostic tools that are more specific, more sensitive and better suited to field screening. They also call out the urgency of finding new drugs that are less toxic, easy to administer and more effective."

Journal • Review • Narcolepsy • Sleep Disorder

The immunoregulator β-glucan produces antidepressant effects through microglia-mobilized astrocytic P2Y1R-BDNF signaling in the dentate gyrus. (PubMed, Int Immunopharmacol) - "Degradation of endogenous ATP by apyrase, non-specific antagonism of purinergic receptors by suramin, specific antagonism of P2Y1Rs in the hippocampus or selective deletion of P2Y1R in astrocytes was able to abolish the antidepressant effect of β-glucan...Further analysis showed that antagonism of BDNF signaling in the hippocampus abolished the antidepressant effect of β-glucan. These results suggest that ATP-triggered astrocytic P2Y1R signaling may mediate the antidepressant effect of β-glucan by promoting BDNF production in the hippocampus."

Journal • CNS Disorders • Depression • Inflammation • Psychiatry