Fluorinated nucleoside analogues are a major class of cancer chemotherapy agents, and include the drugs 5-fluorouracil (5FU) and 5-fluoro-2'-deoxyuridine (FdUrd). The aim of this study was to examine the cellular toxicity of two novel fluorinated pyrimidine L-nucleosides that are enantiomers of D-nucleosides and may be able to increase selectivity for cancer cells as a result of their unnatural L-configuration. Two fluorinated pyrimidine L-nucleosides were examined in this study, L110 ([β-L, β-D]-5-fluoro-2'-deoxyuridine) and L117 (β-L-deoxyuridine:β-D-5'-fluoro-2'-deoxyuridine). The cytotoxicity of these L-nucleoside was determined in primary mouse fibroblasts and was compared with 5FU and FdUrd. In addition, the influence of p53 status on cytotoxicity was investigated. These cytotoxicity assays were performed on a matched set of primary mouse fibroblasts that were either wild type or null for the p53 tumour suppressor gene. It was found that cells lacking functional p53 were over 7500 times more sensitive to the drugs L110, L117 and FdUrd than cells containing wild type p53.

1992-12-01·Biochemistry international

Stimulation of Nb2 mitogenesis by an analogue of human growth hormone (110-127).

Article

作者: Kornberg, L J ; Liberti, J P

Two 18-mer peptides were synthesized. Peptide E117 had the same amino acid sequence as that in the region 110-127 of human growth hormone [hGH (110-127)]. In the second peptide (L117), E117 was replaced with leucine. Biological activity of the peptides was assessed in cultured Nb2 lymphoma cells. L117 stimulated cell division and DNA synthesis in a concentration-dependent manner. Maximum stimulation was equivalent to that noted with native hGH although L117 was much less potent (L117; EC50 approximately 1 microM vs. hGH; EC50 approximately 20 pM). No demonstrable activity was found with peptide E117. These results suggest that the amphipathic helical structure of hGH (110-127) is crucial for biological activity.

1992-03-01·The Journal of Biochemistry4区 · 生物学

Carbohydrate Binding Specificity of Monoclonal Antibodies Raised against Lactose-Protein Maillard Adducts

4区 · 生物学

Article

作者: Iwao Ohkubo ; Ryo Nakamura ; Tsukasa Matsuda ; Hiroshi Ishiguro ; Makoto Sasaki

Three hybridoma antibodies (L101, L104, and L117) specific for lactose-protein amino carbonyl products (Maillard adducts) were obtained by immunizing mice with the lactose-ovalbumin Maillard adduct and by screening with the lactose-bovine serum albumin (BSA) adduct. They reacted with the Maillard adducts of lactose with several different proteins, but not with the adducts of several other reducing sugars. L101 reacted well with the lactose-BSA adducts formed by 2- to 16-day incubation, whereas L104 and L117 reacted with the advanced stage reaction products but not with the adducts of 2-day incubation. The competitive inhibition of the antibody binding by several mono- and disaccharides showed that lactulose (4-O-beta-D-galactopylanosyl-D-fructose) was the best inhibitor for all three antibodies, and that L104 and L117 were inhibited by methyl-beta-D-galactoside more effectively than L101. These results suggested that different components produced during the progress of the Maillard reaction could be antigenic determinants, and that the carbohydrate moiety including the terminal galactosyl residue played an important role in the antibody binding to the lactose-protein Maillard adducts.

项与 OVI-117 相关的新闻（医药）

2012-07-10

·BioSpace

FDA Approves OncoVista Innovative Therapies, Inc.'s Phase I Clinical Trial of New Drug Candidate (OVI-117) for Solid Tumors

SAN ANTONIO, TX--(Marketwire - July 10, 2012) - OncoVista Innovative Therapies, Inc. (OTCBB: OVIT), a biopharmaceutical company engaged in the development and commercialization of targeted cancer therapies, announced today that the US Food and Drug Administration (FDA) granted approval for the Company's investigational new drug (IND) application for its L-nucleoside conjugate (OVI-117) drug candidate. "The FDA's swift approval of our IND provides validation of OncoVista's mission to be a leader in the development of more efficacious and less toxic targeted cancer therapies," said Alexander Weis, PhD., Chairman, President and CEO of OncoVista. This will allow the Company to build and enhance our drug portfolio to the benefit of shareholders and more importantly, patients. The founding mission of OncoVista is to develop more effective and less toxic drugs for cancer. This is an important milestone towards that mission. About OVI-117 OVI-117, a derivative of FdUMP/5-FU, is a Thymidylate Synthase (TS) inhibitor with enhanced pharmacological properties resulting in the retention of efficacy and the reduction of toxicity. It has particular promise for colon, breast, gastric and prostate tumors. About OncoVista Innovative Therapies Texas-based OncoVista Innovative Therapies, Inc. (OTCBB: OVIT), founded in 2004, is a biopharmaceutical company engaged in the development and commercialization of targeted cancer therapies which are more efficacious and less toxic. For additional information, please visit OncoVista's corporate website at Forward-Looking Statements: A number of statements contained in this press release are forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995 that involve risks and uncertainties that could cause actual results to differ materially from those expressed or implied in the applicable statements. These risks and uncertainties that could cause actual results to differ materially from those expressed or implied in the applicable statements. COMPANY CONTACT: Michael Moloney Chief Operating Officer (210) 677-6000

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适应症	最高研发状态	国家/地区	公司	日期
结直肠癌	临床1期	美国	OncoVista, Inc.	-
结直肠癌	临床1期	-	DuPont Pharma, Inc.	-
结直肠癌	临床1期	-	Lipitek International, Inc.	-
结直肠癌	临床1期	-	OncoVista Innovative Therapies, Inc.	-