Studies concerning the antibiotic actinonin. Part VII. Mass spectra of actinonin and related compounds

Anderson, Nicholas H.; Devlin, John P.; Jones, Stephen; Ollis, W. D.; Thorpe, J. E.

doi:10.1039/p19750000852

Cited by 5 publications

(2 citation statements)

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“…93 About 20 years later, actinonin was also obtained from another strain referenced MG848-hF6 and its inhibition against APN was found to be competitive with the substrate. 94 The structural study and the chemical synthesis of 13 and some analogues have aroused numerous works [95][96][97][98][99][100][101][102] completed by a structure-activity relationship investigation dealing with anti bacterial properties observed in this actinonin series. 103…”

Section: A Naturally Occurring Apn/cd13 Inhibitorsmentioning

confidence: 99%

Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: Chemistry, biological evaluations, and therapeutic prospects

Bauvois¹,

Dauzonne²

2005

Med. Res. Rev.

233

162

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Aminopeptidase N (APN)/CD13 (EC 3.4.11.2) is a transmembrane protease present in a wide variety of human tissues and cell types (endothelial, epithelial, fibroblast, leukocyte). APN/CD13 expression is dysregulated in inflammatory diseases and in cancers (solid and hematologic tumors). APN/CD13 serves as a receptor for coronaviruses. Natural and synthetic inhibitors of APN activity have been characterized. These inhibitors have revealed that APN is able to modulate bioactive peptide responses (pain management, vasopressin release) and to influence immune functions and major biological events (cell proliferation, secretion, invasion, angiogenesis). Therefore, inhibition of APN/CD13 may lead to the development of anti-cancer and anti-inflammatory drugs. This review provides an update on the biological and pharmacological profiles of known natural and synthetic APN inhibitors. Current status on their potential use as therapeutic agents is discussed with regard to toxicity and specificity.

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Section: A Naturally Occurring Apn/cd13 Inhibitorsmentioning

confidence: 99%

Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: Chemistry, biological evaluations, and therapeutic prospects

Bauvois¹,

Dauzonne²

2005

Med. Res. Rev.

233

162

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“…18 Microbiological assessment revealed that actinonin is a bacteriostatic agent with activity against Gram‐positive and Gram‐negative microorganisms 19. Actinonin has also been shown to be cytotoxic to tumor cell lines in vitro 20–22. This strong inhibitor of PDF provides an excellent reference for comparison with the other chosen ligands.…”

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confidence: 99%

Drug screening of pharmaceutical discovery compounds by micro‐size exclusion chromatography/mass spectrometry

Wabnitz

Loo

2001

Rapid Comm Mass Spectrometry

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Micro-size exclusion chromatography coupled with capillary liquid chromatography (capLC) and mass spectrometry (MS) provides a rapid and simple approach to the preliminary screening of active ligands toward a specific target macromolecule. In this study, the effectiveness of this technique is demonstrated by a number of small molecule ligands with known binding affinities towards the protein target. All ligands were incubated together with a target protein under native conditions. Separation was then achieved by microcentrifugation where the high molecular weight (MW) compounds were selectively passed through the size-exclusion material. The retained low MW compounds were then recovered and analyzed by capLC/MS. The absence of the ligand indicated strong affinity towards the target, while ligand detection indicated inactivity. This assay demonstrated the drugs that were acting as strong inhibitors of Co-PDF from those showing to be comparatively inactive. The relative binding rank order of the drugs towards Co-PDF was also determined. The results were validated by a corresponding set of control experiments in which the target molecules were excluded from the process. In principle, high-throughput micro-size exclusion chromatography, coupled with capLC/MS, offers a powerful technique as a preliminary screen in determining both the strong binding affinity and the relative affinity rank ordering of ligands towards a specific target macromolecule, and is complementary with other analytical drug screening techniques.

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ChemInform Abstract: STUDIES CONCERNING THE ANTIBIOTIC ACTINONIN PART 7, MASS SPECTRA OF ACTINONIN AND RELATED COMPOUNDS

Anderson¹,

Devlin²,

Jones³

et al. 1975

Chemischer Informationsdienst

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Studies concerning the antibiotic actinonin. Part VII. Mass spectra of actinonin and related compounds

Cited by 5 publications

References 0 publications

Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: Chemistry, biological evaluations, and therapeutic prospects

Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: Chemistry, biological evaluations, and therapeutic prospects

Drug screening of pharmaceutical discovery compounds by micro‐size exclusion chromatography/mass spectrometry

ChemInform Abstract: STUDIES CONCERNING THE ANTIBIOTIC ACTINONIN PART 7, MASS SPECTRA OF ACTINONIN AND RELATED COMPOUNDS

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