Search Results - "Firestone, Raymond A"
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Cathepsin B-Labile Dipeptide Linkers for Lysosomal Release of Doxorubicin from Internalizing Immunoconjugates: Model Studies of Enzymatic Drug Release and Antigen-Specific In Vitro Anticancer Activity
Published in Bioconjugate chemistry (01-07-2002)“…The anticancer drug doxorubicin (DOX) has been linked to chimeric BR96, an internalizing monoclonal antibody that binds to a Lewisy-related, tumor-associated…”
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The Low Energy of Concert in Many Symmetry-Allowed Cycloadditions Supports a Stepwise-Diradical Mechanism
Published in International journal of chemical kinetics (01-07-2013)“…ABSTRACT The thesis of this paper is that orbital symmetry allowedness does not guarantee concert. The activation energy (Ea) for concerted Diels–Alder and…”
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Low-Density Lipoprotein as a Vehicle for Targeting Antitumor Compounds to Cancer Cells
Published in Bioconjugate chemistry (01-03-1994)Get full text
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Lessons from 54 years of pharmaceutical research
Published in Nature reviews. Drug discovery (01-12-2011)Get full text
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Synergistic Anticancer Action of Lysosomal Membrane Permeabilization and Glycolysis Inhibition
Published in The Journal of biological chemistry (28-10-2016)“…We investigated the in vitro and in vivo anticancer effect of combining lysosomal membrane permeabilization (LMP)-inducing agent N-dodecylimidazole (NDI) with…”
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Synthesis of an immunoconjugate of camptothecin
Published in Bioorganic & medicinal chemistry letters (21-01-2002)“…The first immunoconjugate of camptothecin has been synthesized wherein the drug is attached to the tumor-recognizing antibody BR96 via a Cathepsin B cleavable…”
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Cathepsin B Cleavable Novel Prodrug Ac-Phe-Lys-PABC-ADM Enhances Efficacy at Reduced Toxicity in Treating Gastric Cancer Peritoneal Carcinomatosis: An Experimental Study
Published in Cancer (01-06-2012)“…Doxorubicin (Adriamycin) is effective in gastric cancer treatment, but with severe dose-dependent toxicities. A novel prodrug of doxorubicin…”
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(6-Maleimidocaproyl)hydrazone of doxorubicin. A new derivative for the preparation of immunoconjugates of doxorubicin
Published in Bioconjugate chemistry (01-11-1993)“…The (6-maleimidocaproyl)hydrazone of doxorubicin was synthesized and conjugated to several mAbs, including chimeric BR96, via a Michael addition reaction to…”
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Targeting therapy of hepatocellular carcinoma with doxorubicin prodrug PDOX increases anti-metastatic effect and reduces toxicity: a preclinical study
Published in Journal of translational medicine (21-08-2013)“…This study was to investigate the effects and safety of cathepsin B-cleavable doxorubicin (DOX)-prodrug (PDOX) for targeting therapy of metastatic human…”
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Experimental evidence of good efficacy and reduced toxicity with peptide-doxorubicin to treat gastric cancer
Published in Oncotarget (05-01-2018)“…To compare the efficacy and toxicity of peptide-doxorubicin (PDOX) and doxorubicin (DOX) on nude mice models of human gastric cancer. Both PDOX and DOX could…”
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11
Studies with vitamin E and β-carotene as single agents do not prove lack of benefit
Published in British journal of nutrition (01-11-2007)Get full text
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Lipid‐lowering agents may fight cancer by denying it LDL
Published in International journal of cancer (15-11-2006)Get full text
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Anticancer effects of Ac-Phe-Lys-PABC-doxorubicin via mitochondria-centered apoptosis involving reactive oxidative stress and the ERK1/2 signaling pathway in MGC-803 cells
Published in Oncology reports (01-10-2013)“…Ac-Phe-Lys-PABC-DOX (PDOX) is a smart doxorubicin (DOX) prodrug designed to decrease toxicities while maintaining the potent anticancer effects of DOX. The…”
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Synthesis, identification and in vivo studies of tumor-targeting agent peptide doxorubicin (PDOX) to treat peritoneal carcinomatosis of gastric cancer with similar efficacy but reduced toxicity
Published in Molecular cancer (03-03-2014)“…This work aimed to synthesize a cathepsin B (CTSB)-cleavable tumor-targeting prodrug peptide doxorubicin (PDOX) and study the in vivo efficacy and toxicities…”
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Induction of cell death by the lysosomotropic detergent MSDH
Published in FEBS letters (17-03-2000)“…Controlled lysosomal rupture was initiated in lysosome-rich, macrophage-like cells by the synthetic lysosomotropic detergent, O-methyl-serine dodecylamide…”
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Monoclonal Antibody Conjugates of Doxorubicin Prepared with Branched Peptide Linkers: Inhibition of Aggregation by Methoxytriethyleneglycol Chains
Published in Journal of medicinal chemistry (12-09-2002)“…High mole ratio BR96 immunoconjugates were synthesized using branched peptide−doxorubicin linkers designed to liberate doxorubicin following antigen-specific…”
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Drug giants hamstrung by timid middle management
Published in Nature (18-05-2006)“…A letter to the editor regarding hierarchical organizational structures in pharmaceutical companies is presented…”
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Cathepsin B-sensitive dipeptide prodrugs. 1. A model study of structural requirements for efficient release of doxorubicin
Published in Bioorganic & medicinal chemistry letters (01-12-1998)“…A series of lysosomal protease-sensitive peptides attached to doxorubicin (DOX) was prepared as model substrates for internalizing anticancer immunoconjugates…”
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Anti-Cancer Effects of Novel Doxorubicin Prodrug PDOX in MCF-7 Breast Cancer Cells
Published in Journal of Huazhong University of Science and Technology. Medical sciences (01-08-2014)“…Ac-Phe-Lys-PABC-DOX(PDOX) is a smart doxorubicin(DOX) prodrug designed to decrease toxicities while maintaining the potent anticancer effects of DOX. This…”
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Reply to “Comment on ‘Phantom Activation Volumes'”
Published in The journal of physical chemistry. A, Molecules, spectroscopy, kinetics, environment, & general theory (26-08-2004)Get full text
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