ubenimex (DFP-14323) / Delta-Fly Pharma 
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  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal, Cytokine storm:  The triple combination DBDx alleviates cytokine storm and related lung injury. (Pubmed Central) -  Oct 26, 2024   
    All of these results demonstrate that DBDx, a triple combination of clinical orally-administered drugs, can alleviate cytokine storm and related lung injury. DBDx is beneficial for treating cytokine storm disorders.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Review, Journal:  State of the Art in the Development of Human Serum Carnosinase Inhibitors. (Pubmed Central) -  Jun 19, 2024   
    Bestatin is the only inhibitor reported other than carnostatine, although its activity is not selective towards serum carnosinase. Herein, we present a review of the most critical findings on human serum carnosinase, including enzyme expression, localization and substrate selectivity, along with factors affecting the hydrolytic activity, its implication in human diseases and the properties of known inhibitors of the enzyme.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  Bestatin attenuates breast cancer stemness by targeting puromycin-sensitive aminopeptidase. (Pubmed Central) -  May 30, 2024   
    Puromycin-sensitive aminopeptidase is implicated in the process through the regulation of cell cycle, resulting in heightened cell apoptosis and diminished cell proliferation of BCSCs. Our study suggest that targeting cancer stem cell may offer a promising approach in breast cancer treatment, presenting noval therapeutic strategies for patients with breast cancer.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal, IO biomarker:  Targeting the GPI transamidase subunit GPAA1 abrogates the CD24 immune checkpoint in ovarian cancer. (Pubmed Central) -  Apr 4, 2024   
    Consequently, we show that bestatin, a clinically advanced aminopeptidase inhibitor, binds to GPAA1 and blocks GPI attachment, resulting in reduced CD24 cell surface expression, increased macrophage-mediated phagocytosis, and suppressed growth of ovarian tumors. Our study highlights the potential of targeting GPAA1 as an immunotherapeutic approach for CD24+ ovarian cancers.
  • ||||||||||  Natacyn (natamycin) / Novartis, ubenimex (DFP-14323) - Delta / Fly Pharma, SAL-003 (evolocumab biosimilar) / Shenzhen Salubris, Ligand
    Journal:  Targeting Allosteric Site of PCSK9 Enzyme for the Identification of Small Molecule Inhibitors: An In Silico Drug Repurposing Study. (Pubmed Central) -  Feb 24, 2024   
    Moreover, the MM-GBSA calculations revealed binding free energy values ranging from -84.22 to -76.39 kcal/mol, which were found comparable to those obtained for the co-crystallized ligand structure. In conclusion, these identified drug molecules have the potential to serve as inhibitors PCSK9 enzyme and these finding could pave the way for the development of new PCSK9 inhibitory drugs in future in vitro research.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  Ubenimex suppresses glycolysis mediated by CD13/Hedgehog signaling to enhance the effect of cisplatin in liver cancer. (Pubmed Central) -  Nov 16, 2023   
    The glycolysis inhibitor 2-deoxy-D-glucose enhanced the antiproliferative effect of ubenimex and CDDP...Moreover, ubenimex inhibited the production of lactic acid and adenosine triphosphate (ATP), as well as the expression of key proteins involved in glycolysis, which was similar to the effects caused by the Hh inhibitor cyclopamine...Ubenimex inhibits glycolysis by targeting the CD13/Hh pathway, thus playing an anti-tumor role together with CDDP. This study demonstrated the adjuvant effect of ubenimex from the perspective of Hh signal-dependent glycolysis regulation.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  Statins markedly potentiate aminopeptidase inhibitor activity against (drug-resistant) human acute myeloid leukemia cells. (Pubmed Central) -  Oct 16, 2023   
    Consistently, statin potentiation of CHR2863 activity was abrogated by co-administration of mevalonate and/or farnesyl pyrophosphate, suggesting the involvement of protein prenylation; this was experimentally confirmed by impaired Rheb prenylation by simvastatin. These novel findings suggest that the combined inhibitory effect of impaired Rheb prenylation and CHR2863-dependent mTOR inhibition instigates a potent synergistic inhibition of statins and APis on human AML cells.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  A promising new target to control fasciolosis: Fasciola hepatica leucine aminopeptidase 2. (Pubmed Central) -  Jul 31, 2023   
    The activity was inhibited by bestatin, 1,10-phenanthroline, and EDTA, specific inhibitors of aminopeptidase and/or metalloproteases...The immunized group elicited total specific IgG and subclasses IgG1 and IgG2 antibody responses. This study highlights the potential of a new candidate vaccine formulation with potential applications in natural ruminant hosts, especially those targeting the juvenile stage.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  Antiplasmodial Activity Evaluation of a Bestatin-Related Aminopeptidase Inhibitor, Phebestin. (Pubmed Central) -  Jul 17, 2023   
    This study highlights the potential of a new candidate vaccine formulation with potential applications in natural ruminant hosts, especially those targeting the juvenile stage. Phebestin inhibited the in vitro multiplication of the P. falciparum 3D7 (chloroquine-sensitive) and K1 (chloroquine-resistant) strains at IC values of 157.90?
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  Bestatin as a treatment modality in experimental periodontitis. (Pubmed Central) -  Apr 6, 2023   
    We show that in a murine model of CP bestatin not only shifted the biofilm species composition from pathogenic to a commensal one, but also promoted bacteria clearance by immune cells and alleviated inflammation. Taken together, these results suggest that bestatin is a promising drug choice for the treatment and/or prevention of periodontitis and clinical trials are required to fully evaluate its potency.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  Development of Hydroxamate Derivatives Containing a Pyrazoline Moiety as APN Inhibitors to Overcome Angiogenesis. (Pubmed Central) -  Dec 12, 2022   
    2,6-Dichloro substituted compound 14o with R = CH, showed the best capacity for inhibiting APN with an IC value of 0.0062 ± 0.0004 μM, which was three orders of magnitude better than that of the positive control bestatin...The hydroxamate moiety chelated the zinc ion and formed four hydrogen bonds with His, Glu and His. Meanwhile, the terminal phenyl group and another phenyl group of 14o interacted with S' and S pockets via hydrophobic effects, respectively.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal, PARP Biomarker:  FASN inhibitors enhance bestatin-related tumor cell apoptosis through upregulating PEPT1. (Pubmed Central) -  Nov 23, 2022   
    Meanwhile, the terminal phenyl group and another phenyl group of 14o interacted with S' and S pockets via hydrophobic effects, respectively. FASN inhibitors facilitate tumor cells susceptible to bestatin-induced apoptosis involving the up-regulation of PEPT1 at the mRNA translation level and the transport of bestatin by PEPT1, emerging as a promising strategy for tumor targeted therapy.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  Therapeutic effect on Alveolar echinococcosis by targeting EM-Leucine aminopeptidase. (Pubmed Central) -  Nov 1, 2022   
    In this study, the therapeutic effect of recombinant EM-LAP (rEM-LAP) on AE was evaluated and verified using Ubenimex, a broad-spectrum inhibitor of LAP...The indirect ELISA shows that rEM-LAP could induce specific immunity response and produce high levels of IgG, IgG1, IgG2a, IgM, and IgA, and the serum levels of IFN-γ and IL-4 are significantly increased compared to the control groups, indicating that treatment with rEM-LAP leads to a Th1 and Th2 mixed-type immune response. This study suggests that EM-LAP could be a potential therapeutic target of E. multilocularis infection.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Preclinical, Journal:  Exploring ex vivo peptideolysis of thymopentin and lipid-based nanocarriers towards oral formulations. (Pubmed Central) -  Sep 14, 2022   
    Inhibition of TP5 enzymatic peptidolysis was screened in the presence or absence of EDTA, trypsin and chymotrypsin inhibitors from soybean (SBTCI), and bestatin...TP5 and SBTCI were loaded into three lipid-based delivery systems, displaying superior protection under ex vivo intestinal luminal contents and mucosal homogenates for 6 hours compared with the pure drug solution. These findings suggest that using select inhibitors and lipid-based nanocarriers can decrease peptide degradation and may improve oral bioavailability of TP5 following oral administration.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma, tosedostat (CHR-2797) / CTI BioPharma
    Review, Journal:  Review: Aminopeptidases in Cancer, Biology and Prospects for Pharmacological Intervention. (Pubmed Central) -  Jun 25, 2022   
    While there are agents that directly target aminopeptidases which demonstrate potential as cancer therapies, such as bestatin and tosedostat, more selective and more targeted therapeutic approaches are needed. This article specifically looks at the biological role of aminopeptidases in both normal and cancer processes, and their potential as a biological target for future therapeutic strategies.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Preclinical, Journal:  Bradykinin induces peripheral antinociception in PGE-induced hyperalgesia in mice. (Pubmed Central) -  Apr 26, 2022   
    We are planning a phase III study to evaluate this combination therapy as compared with other EGFR-TKIs. The present study is the first to demonstrate BK-induced antinociception in peripheral tissues against PGE-induced nociception in mice and the involvement of κ-opioid and CB cannabinoid receptors in this effect.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  Curcumin induces peripheral antinociception by opioidergic and cannabinoidergic mechanism: Pharmacological evidence. (Pubmed Central) -  Feb 22, 2022   
    The present study is the first to demonstrate BK-induced antinociception in peripheral tissues against PGE-induced nociception in mice and the involvement of κ-opioid and CB cannabinoid receptors in this effect. These results suggest that curcumin possibly peripheral antinociception induced by opioid and cannabinoid systems activation and possibly for endocannabinoids and opioids release.
  • ||||||||||  Nexavar (sorafenib) / Bayer, Amgen
    Biomarker, Review, Journal:  New frontiers against sorafenib resistance in renal cell carcinoma: From molecular mechanisms to predictive biomarkers. (Pubmed Central) -  Feb 10, 2022   
    Herein, we comprehensively summarize the underlying mechanisms of sorafenib resistance and molecular biomarkers for predicting sorafenib responsiveness. Moreover, we outline strategies suitable for overcoming sorafenib resistance and prospect potential approaches for identifying biomarkers associated with sorafenib resistance in RCC, which contributes to guide individualized and precision drug therapy.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma, capivasertib (AZD5363) / Otsuka, AstraZeneca
    Journal:  Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors. (Pubmed Central) -  Dec 20, 2021   
    HUVEC tube formation assays confirmed the superior APN inhibitory activities of 5f and 5h relative to bestatin at the cellular level. Western blot analysis demonstrated that 5h could effectively inhibit the phosphorylation of GSK3β, the intracellular substrate of AKT.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Preclinical, Journal:  Bestatin cream impairs solar simulated light-driven skin inflammation and skin carcinogenesis in mice. (Pubmed Central) -  Dec 16, 2021   
    Mechanistic studies showed bestatin inhibited skin carcinogenesis by suppressing cell proliferation and inducing cell apoptosis through LTA4H-BLT1-AKT-NF-κB P65 pathway. Overall, our results suggest that topical application of novel cream containing bestatin might open a helpful avenue for SSL induced skin carcinogenesis.
  • ||||||||||  ubenimex (DFP-14323) - Delta / Fly Pharma
    Journal:  Overexpression of Plasmodium falciparum M1 Aminopeptidase Promotes an Increase in Intracellular Proteolysis and Modifies the Asexual Erythrocytic Cycle Development. (Pubmed Central) -  Nov 29, 2021   
    Inhibition studies showed that overPfA-M1 presented a lower sensitivity against the metalloaminopeptidase inhibitor bestatin and to other recombinant PfA-M1 inhibitors, in comparison with the wild-type strain, indicating that PfA-M1 is a target for the in vitro antimalarial activity of these compounds...We also investigated the potential role of calmodulin and cysteine proteases in PfA-M1 activity. Taken together, our data show that the overexpression of PfA-M1 in the parasite cytosol can be a suitable tool for the screening of antimalarials in specific high-throughput assays and may be used for the identification of intracellular molecular partners that modulate their activity in P. falciparum.
  • ||||||||||  dexamethasone / Generic mfg., gefitinib / Generic mfg.
    Clinical, Journal:  Enhancing the Therapeutic Efficacy of Gefitinib in Human Non-Small-Cell Lung Cancer through Drug Combination. (Pubmed Central) -  Nov 4, 2021   
    In vivo, compared with DBDx alone, the combination treatment distinctly inhibited tumor growth in mouse xenograft models of human NSCLC. Overall, our results indicate that the combination of DBDx and gefitinib in the treatment of human NSCLC is very promising, which warrants further translational studies.