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  • inhibitor
  • Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. (umassmed.edu)
  • Because PAD levels are elevated in mouse and human colitis, we hypothesized that a novel small-molecule inhibitor of the PADs, i.e., chloramidine (Cl-amidine), could suppress colitis in a dextran sulfate sodium mouse model. (umassmed.edu)
  • and Hofseth, Lorne J., "Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. (umassmed.edu)
  • The efficacy of the PADI inhibitor, Cl-amidine, was tested in vitro using MCF10DCIS cells grown in 2D-monolayers and 3D-spheroids, and in vivo using MCF10DCIS tumor xenografts. (biomedcentral.com)
  • Lastly, we performed cell cycle array analysis of Cl-amidine treated and control MCF10DCIS cells, and found that the PADI inhibitor strongly affects the expression of several cell cycle genes implicated in tumor progression, including p21 , GADD45α , and Ki67 . (biomedcentral.com)
  • Interestingly, treatment of several PADI4-expressing cancer cell lines with the PADI inhibitor, Cl-amidine, elicited strong cytotoxic effects while having no observable effect on non-cancerous lines [ 11 ], suggesting that PADIs may represent targets for new cancer therapies. (biomedcentral.com)
  • vitro
  • In vitro studies indicated that Cl-amidine may act as a tumor suppressor by upregulating miR-16, a putative tumor suppressor miRNA with cell cycle targets, and causing G1 cell cycle arrest. (sc.edu)
  • aromatic
  • announced today that the United States Patent and Trademark Office (patent 6635668) and Australian patent office, IP Australia (patent 766814), have issued patents on a class of dicationic compounds known as aromatic amidine compounds that target Imidazoline receptors in the brain and other organs in the body. (thefreedictionary.com)
  • Immtech's licensed library of aromatic amidine compounds shows high selectivity and affinity for Imidazoline receptors, which are generating substantial interest as targets for new drug development. (thefreedictionary.com)
  • Novel
  • We have previously reported that non-symmetrical furan amidines are potent inhibitors of NQO2 and here novel analogues are evaluated. (aston.ac.uk)
  • Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine" by Alexander A. Chumanevich, Corey P. Causey et al. (umassmed.edu)
  • efficacy
  • Next, we tested the efficacy of Cl-amidine in the HCT116 colon cancer cell line and the Azoxymethane (AOM)/Dextran Sulfate Sodium (DSS) murine model of UC. (sc.edu)
  • mice
  • We then carried out preclinical studies in nude (nu/nu) mice and found that Cl-amidine also suppressed the growth of xenografted MCF10DCIS tumors by more than 3-fold. (biomedcentral.com)
  • toxic
  • Moreover, he says that the new amidines may be toxic to aquatic organisms. (thefreedictionary.com)
  • Results are consistent with this hypothesis, as demonstrated by the finding that Cl-amidine treatment, both prophylactic and after the onset of disease, reduced the clinical signs and symptoms of colitis, without any indication of toxic side effects. (umassmed.edu)
  • hypothesis
  • Our results showed that in the AOM/DSS murine model of UC-associated CRC, Cl-amidine significantly inhibited tumorigenesis, further supporting our hypothesis. (sc.edu)
  • PADs
  • In total, these data help validate the PADs as therapeutic targets for the treatment of IBD and further suggest Cl-amidine as a candidate therapy for this disease. (umassmed.edu)
  • molecular
  • The observed structure-activity relationship for the furan-amidine series with NQO2 was rationalized by preliminary molecular docking and binding mode analysis. (aston.ac.uk)
  • activity
  • The furan ring has been changed to other heterocycles (imidazole, N-methylimidazole, oxazole, thiophene) and the amidine group has been replaced with imidate, reversed amidine, N-arylamide and amidoxime to probe NQO2 activity, improve solubility and decrease basicity of the lead furan amidine. (aston.ac.uk)
  • The analogues were evaluated for inhibition of NQO2, which showed lower activity than the lead furan amidine. (aston.ac.uk)
  • Studies
  • Our initial studies have determined that Cl-amidine is generally nontoxic in cell and animal models. (sc.edu)
  • candidate
  • Together, these results suggest that PADI2 may function as an important new biomarker for HER2/ERBB2+ tumors and that Cl-amidine represents a new candidate for breast cancer therapy. (biomedcentral.com)
  • growth
  • In addition, the oxazole-amidine analogue inhibited the growth of Plasmodium falciparum with an IC50 value of 0.3 μM. (aston.ac.uk)