Retro Hydrazino-azapeptoids as Peptidomimetics of Proteasome Inhibitors
Several groups of proteasome inhibitors are widely used to study the role of the ubiquin proteasome pathway in various cellular processes or as anticancer drugs. Peptidomimetics have been developed to circumvent problems inherent in peptides such as poor bioavailability and protease-mediated degrada...
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Published in | Journal of medicinal chemistry Vol. 48; no. 1; pp. 330 - 334 |
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Main Authors | , , , , |
Format | Journal Article |
Language | English |
Published |
WASHINGTON
American Chemical Society
13.01.2005
Amer Chemical Soc |
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Abstract | Several groups of proteasome inhibitors are widely used to study the role of the ubiquin proteasome pathway in various cellular processes or as anticancer drugs. Peptidomimetics have been developed to circumvent problems inherent in peptides such as poor bioavailability and protease-mediated degradation, while retaining biological activity. In this study, we introduce new pseudopeptides, the retro hydrazino-azapeptoids, designed as proteasome inhibitor peptidomimetics. Their proteasome inhibitory activity and antiproliferative properties are reported here. |
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AbstractList | Several groups of proteasome inhibitors are widely used to study the role of the ubiquin proteasome pathway in various cellular processes or as anticancer drugs. Peptidomimetics have been developed to circumvent problems inherent in peptides such as poor bioavailability and protease-mediated degradation, while retaining biological activity. In this study, we introduce new pseudopeptides, the retro hydrazino-azapeptoids, designed as proteasome inhibitor peptidomimetics. Their proteasome inhibitory activity and antiproliferative properties are reported here. |
Author | Delcros, Jean-Guy Baudy-Floc'h, Michèle Aubin, Sandrine Martin, Bénédicte Arlot-Bonnemains, Yannick |
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Keywords | 20S PROTEASOME ACID DERIVATIVES POTENT SOLID-PHASE SYNTHESIS PEPTOIDS AZA N-SUBSTITUTED GLYCINES AGENTS MULTICATALYTIC PROTEINASE COMPLEX AZAPEPTIDES Antineoplastic agent Organic hydrazide Multicatalytic endopeptidase complex Enzyme Peptidomimetic compound Rodentia Enzyme inhibitor Cytotoxicity In vitro Pseudopeptide Peptidases Vertebrata Mammalia Cell line Structure activity relation Mouse Animal B16-Melanoma Hydrolases Peptide synthesis Chemical synthesis Tumor cell |
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SubjectTerms | Animals Antineoplastic agents Antineoplastic Agents - pharmacology Biochemistry - methods Biological and medical sciences Cell Proliferation - drug effects Chemistry, Medicinal Drug Screening Assays, Antitumor General aspects Hydrazines - chemistry Inhibitory Concentration 50 Leukemia L1210 Life Sciences & Biomedicine Medical sciences Mice Molecular Mimicry Peptoids - chemistry Peptoids - pharmacology Pharmacology & Pharmacy Pharmacology. Drug treatments Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Proteasome Inhibitors Science & Technology Tumor Cells, Cultured |
Title | Retro Hydrazino-azapeptoids as Peptidomimetics of Proteasome Inhibitors |
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