Germanin (suramin) / Optimum Therap - LARVOL DELTA

Interaction between purinergic signalling and purinergic modulators with skin wound repair effectors: a systematic review of preclinical in vivo models. (PubMed, Purinergic Signal) - "Topical or oral administration of CGS-21680 (4-[{N-ethyl-5'-carbamoyladenos-2-yl}aminoethyl] phenylpropionic acid), UTP (Uridine-5'-triphosphate), NECA (5'-N-ethylcarboxamidoadenosine), ATP (adenosine triphosphate), PDRN (polydeoxyribonucleotide), ADP (Adenosine-5'-diphosphate) and TMPS (Thymidine 5'-O-monophosphorothioate) agonists stimulated wound contraction, fibroblast and keratinocyte proliferation, angiogenesis, and collagen biosynthesis...Conversely, the purinergic antagonists DMPX (3,7-dimethyl-1-propargylxanthine), CSC (8-(3-chlorostyryl) caffeine), SUR (Suramin), ENP (enprofylline), caffeine, CLOP (clopidogrel), MRS 2179 (2'-deoxy-N6-methyladenosine-3',5'-bisphosphate), and MRS 2395 (2-Chloro-3',5'-O-(benzoyl-β,γ-methylene) adenosine 5'-triphosphate), as well as genetic knockout for purinergic receptors delayed wound closure by inhibiting these pathways, impairing angiogenesis, collagenogenesis, and aggravating..."

Journal • Preclinical • Review • Inflammation • EGF • IL10 • IL13 • TGFB1

Cryo-EM structures of CCHFV polymerase reveal a stepwise initiation stabilization pathway and a dual-site inhibition mechanism. (PubMed, Cell Rep) - "Suramin competitively occludes the 5' vRNA-binding pocket through electrostatic mimicry of the RNA backbone and concurrently traps a distal linker-fingers interface, restricting the conformational dynamics required for catalysis. Collectively, these findings provide structural insights into CCHFV polymerase regulation and inhibition."

Journal • Hematological Disorders

Evaluation of lysine modified peptides and their cell penetrating peptide conjugates with sirtuin activity inhibition properties and intracellular delivery. (PubMed, Methods Enzymol) - "We present data of three peptides from this family Tat KP 1, Tat KP 2 and Tat KP 3 that show promising yeast sirtuin and mammalian SIRT1 inhibition potential (IC50 6-12 µM) comparable to known sirtuin inhibitors suramin and splitomicin and also showed cytotoxicity against HeLa and BE(2)-C cells...This study documents the one of the initial reports of Tat conjugation modification to enhance the sirtuin inhibition potential. Collectively, this chapter provides comprehensive protocols and practical guidance for the characterization and biological evaluation of sirtuin inhibitors which could be used to identify and characterize novel peptides inhibitors of sirtuins with cell penetrating properties."

Journal

Design, synthesis, and antitrypanosomal activity of novel analogs of the hit benzofuranone for the protozoan parasitic disease Human African trypanosomiasis | Poster Board #1757 (ACS-Fall 2026) - "Currently available treatments, including fexinidazole, pentamidine, suramin, melarsoprol, nifurtimox, and eflornithine are limited by drug resistance, toxicity, poor CNS penetration, and the need for parenteral administration. Further derivatization of the hit/analogs was also carried out for biological evaluation. The design, synthesis, and antitrypanosomal activity of the analogs will be presented."

CNS Disorders • Infectious Disease • Narcolepsy • Sleep Disorder

Design, synthesis, and antitrypanosomal activity of novel analogs of the hit benzofuranone for the protozoan parasitic disease Human African trypanosomiasis | Poster Board #1173 (ACS-Fall 2026) - "Currently available treatments, including fexinidazole, pentamidine, suramin, melarsoprol, nifurtimox, and eflornithine are limited by drug resistance, toxicity, poor CNS penetration, and the need for parenteral administration. Further derivatization of the hit/analogs was also carried out for biological evaluation. The design, synthesis, and antitrypanosomal activity of the analogs will be presented."

CNS Disorders • Infectious Disease • Narcolepsy • Sleep Disorder

Kinetic Compatibility as a Predictor of PTP1B Inhibitor Combination Outcomes: An Integrated Experimental and Computational Study. (PubMed, ChemMedChem) - "Although chlorogenic acid, suramin, ursolic acid, and the glycyrrhetinic acid derivative FC122 are individually known PTP1B inhibitors, no study has systematically characterized how mechanistic diversity determines the pharmacological outcome of their combinations. For the first time, the MD-AMBER-Umbrella-COM protocol was applied to generate a comparative membrane permeability profile for mechanistically diverse PTP1B inhibitors, proposing a permeability order (SUR > FC122 > CGA ≈ UA). These results suggest that kinetic compatibility is a more reliable predictor of promising inhibitor combinations than binding-site geography alone, and they offer a rational framework for designing multisite PTP1B inhibition strategies in type 2 diabetes mellitus."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus • PTPN1

Machine learning of sunitinib resistance genes reveals that SP5 regulates angiogenesis and sunitinib resistance in RCC via the VEGFA/AKT axis. (PubMed, Neoplasia) - "Our findings establish SP5 as a critical driver of sunitinib resistance and identify suramin as a promising therapeutic strategy."

Journal • Genito-urinary Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor

Blocking the m6Am methyltransferase PCIF1 releases STAT1-mediated Th1 immunity to potentiate cancer immunotherapy. (PubMed, Nat Commun) - "Crucially, we identify Suramin as a pharmacological PCIF1 inhibitor that disrupts m6Am modification, boosts Th1 responses, and suppresses tumor growth. Our findings establish the PCIF1-m6Am-STAT1 axis as a translational checkpoint governing T cell differentiation and suggest that targeting PCIF1 represents a potential strategy for tumor immunotherapy."

Journal • Oncology • CD4 • PCIF1 • STAT1

Recent advances in antiviral drugs for Chikungunya virus (CHIKV): Targets, mechanisms, and development strategies. (PubMed, Acta Pharm Sin B) - "We analyze the current research status of various anti-CHIKV compounds, including suramin, baicalin, halofuginone, betulinic acid, andrographolide, and itraconazole. Additionally, we summarize host-directed antiviral strategies targeting pathways such as host cell oxidative folding, Na+/K+-ATPase, and MAPK signaling. This review aims to establish a theoretical foundation and outline potential research directions for the development of CHIKV-related therapeutics, thereby facilitating the discovery of effective treatment strategies against this pathogen."

Journal • Review • Chikungunya • Immunology • Infectious Disease • Musculoskeletal Diseases • Musculoskeletal Pain • Orthopedics • Pain • Rheumatology

Structural mechanism of Borna disease virus 1 RNA polymerase autoinhibition and suramin-mediated inhibition. (PubMed, Cell Rep) - "We identify an N-terminal autoinhibitory element (AIE) that is positioned to physically block the template entry tunnel, suggesting an autoinhibition mechanism reminiscent of a "molecular plug." Furthermore, we demonstrate that the inhibitor suramin binds in a specific triple-molecule mode, potentially achieving inhibition by sterically occluding RNA access and allosterically restricting the catalytic core. These findings elucidate the architecture and regulation of the BoDV-1 polymerase, providing a structural framework for rational antiviral design."

Journal • CNS Disorders

Mechanisms of ligand recognition and channel opening for P2X2 receptors in lipid nanodiscs. (PubMed, Sci Adv) - "Here we report cryo-electron microscopy structures of the human P2X2R in lipid nanodiscs in an apo closed state, with ATP4-, Mg-ATP2-, 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

Kv1.3 Channel Blockade by Dalfampridine Attenuates NLRP3 Inflammasome-Driven Demyelination via the NEK7/Ripk1/FADD Pathway, Matching the Efficacy of Broad P2X7 Antagonism by Suramin in EAE. (PubMed, Drug Dev Res) - "These findings suggest that Kv1.3 may serve as a contributory node where downstream channel modulation can deliver neuroprotection equivalent to the upstream pathway intervention. By modulating this potential checkpoint, Kv1.3-targeted therapy may reduce collateral effects associated with pan-purinergic blockade, offering a potential streamlined therapeutic corridor for demyelinating neuroinflammation with enhanced specificity and reduced systemic burden."

Journal • CNS Disorders • Immunology • Inflammation • Multiple Sclerosis • Solid Tumor • FADD • NLRP3 • RIPK1

Involvement of cystathionine β-synthase in ATP-induced hydrogen sulfide production in cochlear outer hair cells. (PubMed, J Otol) - "This ATP-induced H2S production was inhibited by suramin, an antagonist of the P2 receptor...These findings imply generation of H2S by CBS in response to exposure to ATP in OHCs. Regulatory cross-talk among ATP, H2S, and NO may also exist in the cellular signaling pathways in OHCs."

Journal

Structural basis for RNA synthesis and inhibition of the orthobunyavirus polymerase. (PubMed, Nat Commun) - "Here, we establish robust in vitro enzymatic activity assays for the Ebinur Lake virus (EBIV) polymerase and identify suramin, a century-old drug, as an inhibitor of EBIV polymerase...The other site directly blocks RNA template strand binding, thereby inhibiting polymerase activity. These findings advance our understanding of orthobunyavirus RNA synthesis mechanisms and offer a structural framework for the rational design and optimization of antiviral drugs."

Journal

Suramin Interactions Across Biological Systems: From Molecular Targets to Therapeutic Implications. (PubMed, Biomolecules) - "At the same time, its largeness and high negative charge limit oral bioavailability and brain penetration, prompting efforts to develop simplified analogues. This review brings together chemical, biological, and structural perspectives on suramin, highlighting opportunities for drug repurposing, transporter-focused drug design, and a better understanding of mitochondrial toxicity."

Journal • Review

Targeting P2X purinergic receptors with suramin alleviates rotenone-induced parkinson's-like pathology via modulation of mitophagy and NLRP3-pyroptosis: Comparison with metformin. (PubMed, Life Sci) - "They also suppressed NLRP3 inflammasome activation and pyroptosis, with suramin showing more potent anti-inflammatory effects. Altogether, suramin's neuroprotective effects could be mediated via suppressing P2X7/P2X4 receptors, enhancing mitophagy and counteracting NLRP3-driven pyroptosis in the striatum, with its relatively stronger profile attributable to more robust P2X7/P2X4 signaling inhibition, underscoring its potential as a therapeutic candidate for PD."

Journal • CNS Disorders • Inflammation • Movement Disorders • Parkinson's Disease • NLRP3

Development of HTS enzymatic assays for WRN helicase and exonuclease functions (AACR 2024) - "There are no published inhibitors for the WRN exonuclease, but suramin inhibited with an IC50 of approximately 100 nM. These assays allow sensitive, robust, quantitative detection of WRN ATPase and exonuclease activities using an extensively validated HTS platform; they should be valuable tools for screening and optimizing small molecules targeting specific WRN functions."

Microsatellite Instability • Oncology • MSI • WRN

Purinergic P2Y6 receptor antagonists as potential anti tumor agents (AACR 2024) - "We found that suramin-injected tumors had a substantial reduction in tumor volume when compared to saline-injected ones. Intra-tumoral injections of P2 receptor antagonists such as MRS-2578 also resulted in similar outcomes as suramin. In tumors treated with P2 receptor antagonists, the expression of COX-2, cell cycle proteins and epithelial-to-mesenchymal (EMT) markers, which aid in metastasis, were significantly downregulated, indicating a suppressive effect."

Hematological Malignancies • Lymphoma • Oncology • PTGS2

The HIV protease inhibitor nelfinavir increases the sensitivity of epithelial ovarian cancer cells to cisplatin (AACR 2025) - "Cytosolic dsDNA is an activation signal for the AIM2 inflammasome; to confirm its involvement, EOC cells were incubated with CDDP and NFV in the presence or absence of the AIM2 inhibitor suramin. Resistance to apoptosis is a major mechanism by which EOC cells become Pt-resistant. Therefore, NFV and CDDP together, may be a feasible therapeutic option for these patients through the induction of pyroptosis."

Epithelial Ovarian Cancer • Oncology • Ovarian Cancer • Solid Tumor • ANXA5 • GSDME • IL1B

Suramin directly targets PI3K to alleviate experimental colitis by restoring intestinal barrier and activating autophagy. (PubMed, Biochem Biophys Res Commun) - "Taken together, our results indicate that suramin protects against experimental colitis mainly by directly engaging PI3K p85α, thereby restraining the PI3K/AKT/mTOR axis to stimulate autophagy and reinforce intestinal epithelial barrier integrity. This research identifies suramin as a potential drug repurposing candidate for treating UC."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Mucositis • Ulcerative Colitis • CLDN1 • OCLN • TJP1

Multi-omics and causal inference reveal lactylation-based osteoblast regulatory networks and drug candidates. (PubMed, iScience) - "Molecular dynamics simulations revealed lactylation-driven functional remodeling of these proteins, and network pharmacology suggested FDA-approved compounds (e.g., Suramin sodium and Paritaprevir) as potential osteogenic agents. This study advances mechanistic understanding of osteogenesis and provides a framework for discovering small molecules that mimic lactylation-induced conformational changes for drug repurposing in clinical applications."

Journal • Osteoporosis

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