• UWA-101 is the first selective DAT/SERT inhibitor described with comparable affinities for these two sites. (erowid.org)
  • WP1130 (Degrasyn) is a novel selective small molecular deubiquitinase inhibitor and a Bcr/Abl destruction pathway activator that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells. (adooq.com)
  • IU1 is a selective inhibitor of Usp14. (adooq.com)
  • P005091 is a selective inhibitor of ubiquitin-specific protease (USP) 7 (IC50 = 4.2 uM). (adooq.com)
  • ML323 is a selective and highly potent USP1-UAF1 inhibitor links deubiquitination to DNA damage responses. (adooq.com)
  • GNE-6640 is a novel selective USP7 inhibitor, inducing tumor cell death. (adooq.com)
  • GRL0617 is a potent, selective and competitive noncovalent inhibitor of SARS PLPro, with an IC50 of 0.6 μM, and with a Ki of 0.49 μM. (adooq.com)
  • F.E showed significant anti-tyrosinase, antibacterial, and cytotoxicity results, therefore it can be considered as an effective inhibitor only or in combination with other flower components. (columbiagypsy.net)
  • Synergistic anti-inflammatory agents, i.e. celecoxib as selective COX-2 inhibitor and montelukast as cysteinyl leukotriene receptor antagonist, were selected. (ac.ir)
  • In contrast, in vivo administration of the selective CYP3A inhibitor troleandomycin (TAO) reduced both potentiation of MMDX cytotoxicity and the rate of CYP3A-catalyzed N-demethylation of erythromycin by isolated liver microsomes (55.5 and 49% reduction, respectively). (unboundmedicine.com)
  • LLPS inhibitor enhanced cytotoxicity of cisplatin/paclitaxel in selective cancer cell lines. (bvsalud.org)
  • The cellular uptake and cytotoxicity of curcumin-encapsulated nanoliposomes on bladder carcinoma HTB9 cell line and normal fibroblast L929 cell line were studied. (current-pharmaceutical-design.com)
  • Of note, SPC and HSPC nanoliposome formulations significantly increased the cellular uptake and cytotoxicity of curcumin on bladder cancer HTB9 cells. (current-pharmaceutical-design.com)
  • Differences in surface coatings and charges were evaluated against cellular uptake, ROS generation, cytotoxicity, and mitochondrial targeting. (cdc.gov)
  • When in vitro experimental models are exposed to ATZ, they are faced with increased levels of reactive oxygen species (ROS), cytotoxicity and decreased growth rate at dosages that may vary with cell types. (frontiersin.org)
  • Desmosdumotin C, which shows significant and selective in vitro cytotoxicity ,was a novel compound with unique chalcone structure. (fip.org)
  • It showed significant and selective in vitro cytotoxicity. (fip.org)
  • It has no detectable in vitro cytotoxicity and is highly selective for CCR5, indicating the potential for an excellent clinical safety profile. (scialert.net)
  • 37.7 g/ml over the viability of HeLa cells using cytotoxicity MTT assay. (columbiagypsy.net)
  • 75:25) and partitioned with demonstrated that the as well as the isolated compounds from the ethanolic extract of fruits (tutin and hyenanchin) was assayed using the MTT cytotoxicity assay. (columbiagypsy.net)
  • Anitmalarial activity is measured by PfNDH2 assay, cytotoxicity, and animal test. (nih.gov)
  • Gamma-delta T cells may be involved in antibody-dependent cell mediated cytotoxicity (ADCC). (medscape.com)
  • Selective inhibitors of protein kinase CK2 with significant cytotoxicity on tumor cells based on a 2-aminothiazole scaffold were described recently. (rcsb.org)
  • We found that MMDX cytotoxicity for cultured M5076 tumor cells was potentiated 22-fold by preincubating the drug with NADPH-supplemented liver microsomes from untreated C57BL/6 female mice. (unboundmedicine.com)
  • In this investigation, the cytotoxicity of 23 α-methylene-γ-lactones towards normal breast epithelial MCF-10A cells as well as breast cancer JIMT-1 cells is compared. (lu.se)
  • Mechanistically, liposomal curcumin was found to exert a selective inhibitory effect on the viability of cancer cells by inducing apoptosis and DNA damage. (current-pharmaceutical-design.com)
  • In the present study, the anticancer activity of pleurocidin-like peptide WF3 isoform X2 (AMP-WF3), from the Poecilia Mexicana fish, against leukemic cell line Jurkat was evaluated, and the cytotoxicity compared with the effects on normal cells, including peripheral blood mononuclear cells (PBMCs) and human dermal fibroblast (HDF) cells. (celljournal.org)
  • Nevertheless, ex vivo activation with cytokines can restore cytolytic activity of NK cells against GB, indicating that NK cells have potential for adoptive immunotherapy of GB if potent cytotoxicity can be maintained in vivo . (frontiersin.org)
  • NK cells contribute to cancer immune surveillance not only by their direct natural cytotoxicity which is triggered rapidly upon stimulation through germline-encoded cell surface receptors, but also by modulating T-cell mediated antitumor immune responses through maintaining the quality of dendritic cells and enhancing the presentation of tumor antigens. (frontiersin.org)
  • In conjugated form, HPAPIs exhibit selective cytotoxicity which can spare non-target cells from toxic effects. (sigmaaldrich.com)
  • Genetically engineered CAR NK cells display selective cytotoxicity against FLT3-positive B-ALL and inhibit in vivo leukemia growth. (stembook.org)
  • The components were tested just at two concentrations, 20 and 200 g/ml, for his or her inhibitory influence on the monophenolase and diphenolase triggered types of tyrosinase (F.E) exhibited the best cytotoxicity aftereffect of Hela cells set alongside the additional components. (columbiagypsy.net)
  • PNC-27, a promising anticancer peptide, has gained attention due to its selective cytotoxicity against cancer cells without harming normal cells. (prospecbio.com)
  • PNC-27, a novel anticancer peptide, holds great promise in the treatment of cancer due to its unique mechanism of action and selective cytotoxicity towards cancer cells (Goldberg et al. (prospecbio.com)
  • Rhodium metalloinsertors are octahedral complexes that bind DNA mismatches with high affinity and specificity and exhibit unique cell-selective cytotoxicity, targeting mismatch repair (MMR)-deficient cells over MMR-proficient cells. (caltech.edu)
  • Moreover, the activities of the new metalloinsertors are coupled with high levels of selective cytotoxicity for MMR-deficient versus proficient colorectal cancer cells. (caltech.edu)
  • DESCRIPTION (provided by applicant): This proposal outlines a body of research to evaluate the cytotoxicity and therapeutic efficacy of radiolabeled alpha-melanocyte stimulating hormone (a-MSH) peptide analogs that target a-particle emitting radioisotopes to the nuclei of melanoma cells. (sbir.gov)
  • Using mice with selective deletion of STAT1 in T cells (STAT1 CD4-Cre ), we identified a potentially novel mechanism by which STAT1 regulates neuroinflammation independently of Foxp3 + Tregs. (jci.org)
  • In skin, there is selective infiltration and long-term persistence of varicella-zoster virus-specific T cells in the rash siterelative to the contralateral site. (cdc.gov)
  • 1994] . Patients with ZAP-70 deficiency have the selective absence of CD8+ T cells and abundant CD4+ T cells in peripheral blood. (lu.se)
  • Nepodin showed a potential selective inhibition (SI index: ratio of 50 % cytotoxic concentration to 50 % effective anti-plasmodial concentration) of 161.6 and 151.4 against P. falciparum 3D7 and P. falciparum S20. (nih.gov)
  • Autophagic cell death was excluded as the inhibition of autophagy did not attenuate the cytotoxicity. (spandidos-publications.com)
  • Maraviroc (MVC) is a selective CCR5 antagonist with potent activity and favourable pharmacological properties against human immunodeficiency virus type 1 (HIV-1). (scialert.net)
  • 4,4-difluoro-N-{(1S)-3-(exo-3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo(3.2.1)oct-8-yl)-1-phenylpropyl}cyclohexanecarboxamide) is a highly selective orally bioavailable chemokine receptor 5 (CCR5) antagonist with potent activity and favourable pharmacological properties against human immunodeficiency virus type 1 (HIV-1) (Dorr et al . (scialert.net)
  • Antimicrobial peptides with selective antitumor mechanisms: prospect for anticancer applications. (celljournal.org)
  • Starch binding domain-containing protein 1 (Stbd1) is a carbohydrate-binding protein that has been proposed to be a selective autophagy receptor for glycogen. (imperial.ac.uk)
  • Notably, this enhanced cytotoxicity is not mediated by the induction of apoptosis, but is accompanied by the pronounced induction of autophagy. (spandidos-publications.com)
  • GNE-6640 enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors. (adooq.com)
  • Cytotoxicity, antiproliferative and apoptosis-inducing capacity of ACNVs against hepatoma carcinoma cell were assessed. (dovepress.com)
  • Results show that the negative charged QDs coated with GSH exhibit excellent water solubility, high quantum yield and low cytotoxicity. (cdc.gov)
  • 1998]. XLP patients exhibit immune defects such as abnormal natural killer and T cell mediated cytotoxicity. (lu.se)
  • Compound 3a, which was active and selective against the three parasites and displayed adequate metabolic stability, is a fine candidate for in vivo studies. (bvsalud.org)
  • Furthermore, sequence homology between mammalian and fungal genes in the GPI pathway show modest conservation raising the chances of finding fungal-selective molecules with good therapeutic index 8 . (nature.com)
  • The formulation displayed impressive oral bioavailability, sustained release, negligible cytotoxicity against THLE-2 normal human hepatocytes, low toxicity (high LD 50 ) and wide therapeutic window. (ac.ir)
  • The Eshmuno ® CMX resin has been designed for highly selective mixed mode chromatography. (sigmaaldrich.com)
  • Acrolein is chemically reactive, highly water soluble, and and diesel engine exhausts, partially combusted animal fats and produces cytotoxicity at the site of initial contact. (cdc.gov)
  • The addition of essential amino acids, but not non-essential amino acids to the cell culture medium resulted in the cancellation of this pronounced cytotoxicity. (spandidos-publications.com)
  • The loss of ZAP-70 function leads to selective inability to produce CD8+ T lymphocytes and abolishes T cell receptor stimulation in mature CD4+ T lymphocytes [Arpaia, et al. (lu.se)
  • Tirapazamine (3-amino-1,2,4-benzotriazine-1,4-dioxide) is a promising hypoxia-selective cytotoxin that has shown significant activity in advanced clinical trials in combination with radiotherapy and cisplatin. (aacrjournals.org)
  • The anti-inflammatory nanoparticles manifested tumor specific release potential exhibiting selective cytotoxicity at cancerous milieu with slightly acidic environment and activated inflammatory pathways. (ac.ir)
  • Macrocyclic scaffolds are particularly attractive for designing selective G-quadruplex ligands essentially because, on one hand, they show a poor affinity for the "standard" B-DNA conformation and, on the other hand, they fit nicely with the external G-quartets of quadruplexes. (hindawi.com)
  • Furthermore, cytotoxicity assays and determination of selectivity index (SI) revealed that ZnCl 2 ( H3 ) 2 (CC 50 = 5 μΜ, SI = 156) is more selective than H3 (CC 50 = 10 μΜ, SI = 20). (nih.gov)
  • toxigenic culture on selective media (typically cycloserine cefoxitin fructose agar [CCFA]) followed by CCNA. (mlo-online.com)
  • Ligand composition is more important in ROS generation than surface charge whereas surface charge is an important driver of cytotoxicity. (cdc.gov)