Triapine (3-AP) / Vion, Northwestern University 
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 194 Diseases   7 Trials   7 Trials   234 News 


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  • ||||||||||  Lutathera (lutetium Lu 177 dotatate) / Novartis
    Enhancing [177Lu]Lu-DOTA-TATE therapeutic efficacy in vitro by combining it with chemotherapy (Hall Y4-Y9) -  Sep 27, 2024 - Abstract #EANM2024EANM_490;    
    Hydroxyurea, gemcitabine and triapine all increased cell size, SSTR2A expression, and [177Lu]Lu-DOTA-TATE uptake, whilst further reducing cell metabolic viability in U2OS+SSTR2A cells when compared to [177Lu]Lu-DOTA-TATE monotherapy. Further investigations could transform patient care and positively increase outcomes for patients treated with [177Lu] Lu-DOTA-TATE.
  • ||||||||||  Lutathera (lutetium Lu 177 dotatate) / Novartis
    Preclinical, Journal:  Enhancing [177Lu]Lu-DOTA-TATE therapeutic efficacy in vitro by combining it with metronomic chemotherapeutics. (Pubmed Central) -  Aug 13, 2024   
    Hydroxyurea, gemcitabine and triapine all increased cell size, SSTR2A expression, and [177Lu]Lu-DOTA-TATE uptake, whilst reducing cell metabolic viability in U2OS?+?SSTR2A cells when compared to [177Lu]Lu-DOTA-TATE monotherapy. Further investigations could transform patient care and positively increase outcomes for patients treated with [177Lu]Lu-DOTA-TATE.
  • ||||||||||  Triapine (3-AP) / Vion
    FDA event, Journal:  Identification of several African swine fever virus replication inhibitors by screening of a library of FDA-approved drugs. (Pubmed Central) -  Mar 13, 2024   
    Furthermore, molecular docking studies showed that triapine might interact with the active center Fe2+ in the small subunit of ASFV ribonucleotide reductase while cytarabine hydrochloride metabolite might interact with three residues (Arg589, Lys593, and Lys631) of ASFV DNA polymerase to block new DNA chain extension. Taken together, our results suggest that triapine and cytarabine hydrochloride displayed significant antiviral activity against ASFV in vitro.
  • ||||||||||  Triapine (3-AP) / Vion
    Covalent conjugation of the deferasirox and triapine iron chelators to exploit dual chelation in anticancer therapy (In-person; Room 212 (Ernest N. Morial Convention Center)) -  Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_12002;    
    As seen in Jurkat cell viability experiments, the cytotoxicity of DefNEtTrp is superior to that of unconjugated Def and Trp ligands in single-drug and combination drug treatments, and is assessed in the context of intracellular labile Fe binding. Preliminary studies will also be presented for the Ti(IV)(DefNEtTrp) 2 complex, which appears to retain the cancer selectivity and promising potency of the free ligand.
  • ||||||||||  Triapine (3-AP) / Vion
    Dual chelator conjugates express enhanced eelectivity than non-conjugated chelators | Poster Board #437 (In-person; Poster Board #437; Hall C (Ernest N. Morial Convention Center)) -  Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_1246;    
    The use of two iron binding compounds, deferasirox (def) and triapine (trp), are known to coordinate with intracellular iron (Fe) to inhibit the development cells, which depend on Fe to proliferate and is known to fuel cancer...MRC-5 treated cells present GI 50 /IC 50 and TGI values significantly greater than MDA-MB-468, indicating how DefNEtTrp is much more selective towards cancer cells. This development will increase the availability of a novel design of chemotherapeutics for widespread patient access and to overcome the limitations of present TNBC and NSCLC therapies.
  • ||||||||||  Triapine (3-AP) / Vion
    Journal:  RRM2 as a novel prognostic and therapeutic target of NF1-associated MPNST. (Pubmed Central) -  Nov 3, 2023   
    RRM2 acts as an integral part in the promotion of NF1-associated MPNST cell proliferation via the AKT-mTOR signaling pathway. Inhibition of RRM2 may be a promising therapeutic strategy for NF1-associated MPNST.
  • ||||||||||  Triapine (3-AP) / Vion, rabusertib (LY 2603618) / Eli Lilly
    Journal, Combination therapy, Synthetic lethality:  Inhibition of RRM2 radiosensitizes glioblastoma and uncovers synthetic lethality in combination with targeting CHK1. (Pubmed Central) -  Aug 14, 2023   
    Collectively, our results suggest RRM2 is a promising therapeutic target for GBM, and targeting RRM2 with triapine sensitizes GBM cells to radiation and independently induces synthetic lethality of GBM cells with CHK1 inhibition. Our findings suggest combining triapine with radiation or rabusertib may improve therapeutic outcomes in GBM.
  • ||||||||||  Triapine (3-AP) / Vion
    Journal:  Human serum albumin as a copper source for anticancer thiosemicarbazones. (Pubmed Central) -  Jul 28, 2023   
    Noteworthy, Fe-chelation from transferrin was not overserved, even not for Triapine. In summary, the labile Cu pool of HSA is a potential source for Cu-TSC complex formation and, consequently, distinctly influences the anticancer activity and pharmacological behavior of TSCs.
  • ||||||||||  Triapine (3-AP) / Vion, VE-821 / EMD Serono, Vertex, didox (NSC-324360) / Molecules for Health
    Journal:  Synergistic anticancer activity of combined ATR and ribonucleotide reductase inhibition in Ewing's sarcoma cells. (Pubmed Central) -  Apr 25, 2023   
    Clinical trial information: NCT02466971. Our study reveals that combined targeting of ATR and RNR was effective against Ewing's sarcoma in vitro and thus rationalises an in vivo exploration into the potential of combining ATR and RNR inhibitors as a new strategy for the treatment of this challenging disease.
  • ||||||||||  Triapine (3-AP) / Vion
    Journal:  Co-delivery of gemcitabine and Triapine by calcium carbonate nanoparticles against chemoresistant pancreatic cancer. (Pubmed Central) -  Apr 4, 2023   
    CaCO-GEM-Triapine NPs nano-formulations enhanced the therapeutic effect of GEM-based chemotherapy by inhibiting cancer cell proliferation, migration, and resistance to GEM using both 2D PANC-1/GEM cells and 3D tumor spheroids. The study indicated that CaCO NPs loaded with GEM and Triapine could provide an effective treatment option to overcome drug resistance in pancreatic cancer.
  • ||||||||||  Triapine (3-AP) / Vion, COTI-2 / Cotinga Pharma
    The role of protein disulfide isomerase and copper in the paraptotic cell death of clinically investigated anticancer thiosemicarbazones (Section 14; Poster Board #12) -  Mar 14, 2023 - Abstract #AACR2023AACR_7245;    
    To further improve the anticancer activity of TSCs, novel derivatives (such as DpC and COTI-2) have been developed and clinically investigated for their activity against solid tumors...The formation of the complex results in the interaction with thiol-containing proteins and subsequently in the disruption of the thiol-redox homeostasis, which leads to paraptotic cell death. Overall this work shed light on the paraptotic cell death and will be of interest for future clinical development of anticancer TSCs, as paraptosis is hypothesized to overcome apoptosis-resistance of cancer cells.
  • ||||||||||  Triapine (3-AP) / Vion, rabusertib (LY 2603618) / Eli Lilly
    Targeting ribonucleotide reductase subunit 2 (RRM2) to radio-sensitize glioblastoma (Section 3; Poster Board #7) -  Mar 14, 2023 - Abstract #AACR2023AACR_5387;    
    Moreover, RRM2 inhibition with triapine effectively sensitizes GBM tumors to radiation in vitro and in vivo. Our findings suggest that triapine warrants clinical testing with radiation.
  • ||||||||||  Triapine (3-AP) / Vion
    Pharmacokinetics, bioavailability, and pharmacodynamics of oral triapine (Section 18; Poster Board #23) -  Mar 14, 2023 - Abstract #AACR2023AACR_5026;    
    Correlation of methemoglobin with exposure highlights the importance of optimizing triapine exposure. Additional data may support the exploration of a dose specific to current smokers.