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 inJournal of medicinal chemistry Vol. 48; no. 1; pp. 330 - 334
Main Authors Aubin, Sandrine, Martin, Bénédicte, Delcros, Jean-Guy, Arlot-Bonnemains, Yannick, Baudy-Floc'h, Michèle
Format Journal Article
LanguageEnglish
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.
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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Issue 1
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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PublicationTitle Journal of medicinal chemistry
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SSID ssj0003123
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Snippet Several groups of proteasome inhibitors are widely used to study the role of the ubiquin proteasome pathway in various cellular processes or as anticancer...
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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
URI http://dx.doi.org/10.1021/jm049455f
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