Geschmack ist vorhersagbar: Mit FlavorMiner. FlavorMiner heißt das Tool, das IPB-Chemiker und Partner aus Kolumbien jüngst entwickelt haben. Das Programm kann, basierend auf maschinellem Lernen (KI), anhand der…
Seit Februar 2021 bietet Wolfgang Brandt, ehemaliger Leiter der Arbeitsgruppe Computerchemie am IPB, sein Citizen Science-Projekt zur Pilzbestimmung an. Dafür hat er in regelmäßigen Abständen öffentliche Vorträge zur Vielfalt…
Mpetga, J. D. S.; Nago, R. D. T.; Tamokou, J.-D.-D.; Fobofou, S. A. T.; Bitchagno, G. T. M.; Wessjohann, L. A.; Tene, M.; Ngouela, A. S.;A new ceramide from Cissus aralioides Baker (Vitaceae) and its antimicrobial activityChem. Biodivers.19e202200678(2022)DOI: 10.1002/cbdv.202200678
Purification through repeated column chromatography over silica gel and Sephadex LH-20 of the ethanol extract of the stems of Cissus aralioides (Baker) Planch. resulted in the isolation of a new ceramide, aralioidamide A (1) along with five known compounds (2-6). Their structures were determined by the extensive analysis of their spectroscopic (1D and 2D NMR) and spectrometric data, and comparison with those reported in the literature. Aralioidamide A (1) displayed weak antibacterial activity (MIC = 256 μg/mL) against Bacillus subtilis, Staphylococcus aureus and Shigella flexneri and was inactive (MIC > 256 μg/mL) against the tested fungi.
Publikation
Wasternack, C.;Termination in Jasmonate Signaling by MYC2 and MTBsTrends Plant Sci.24667-669(2019)DOI: 10.1016/j.tplants.2019.06.001
Jasmonic acid (JA) signaling can be switched off by metabolism of JA. The master regulator MYC2, interacting with MED25, has been shown to be deactivated by the bHLH transcription factors MTB1, MTB2, and MTB3. An autoregulatory negative feedback loop has been proposed for this termination in JA signaling.
Publikation
Méndez, Y.; De Armas, G.; Pérez, I.; Rojas, T.; Valdés-Tresanco, M. E.; Izquierdo, M.; Alonso del Rivero, M.; Álvarez-Ginarte, Y. M.; Valiente, P. A.; Soto, C.; de León, L.; Vasco, A. V.; Scott, W. L.; Westermann, B.; González-Bacerio, J.; Rivera, D. G.;Discovery of potent and selective inhibitors of the Escherichia coli M1-aminopeptidase via multicomponent solid-phase synthesis of tetrazole-peptidomimeticsEur. J. Med. Chem.163481-499(2019)DOI: 10.1016/j.ejmech.2018.11.074
The Escherichia coli neutral M1-aminopeptidase (ePepN) is a novel target identified for the development of antimicrobials. Here we describe a solid-phase multicomponent approach which enabled the discovery of potent ePepN inhibitors. The on-resin protocol, developed in the frame of the Distributed Drug Discovery (D3) program, comprises the implementation of parallel Ugi-azide four-component reactions with resin-bound amino acids, thus leading to the rapid preparation of a focused library of tetrazole-peptidomimetics (TPMs) suitable for biological screening. By dose-response studies, three compounds were identified as potent and selective ePepN inhibitors, as little inhibitory effect was exhibited for the porcine ortholog aminopeptidase. The study allowed for the identification of the key structural features required for a high ePepN inhibitory activity. The most potent and selective inhibitor (TPM 11) showed a non-competitive inhibition profile of ePepN. We predicted that both diastereomers of compound TPM 11 bind to a site distinct from that occupied by the substrate. Theoretical models suggested that TPM 11 has an alternative inhibition mechanism that doesn't involve Zn coordination. On the other hand, the activity landscape analysis provided a rationale for our findings. Of note, compound TMP 2 showed in vitro antibacterial activity against Escherichia coli. Furthermore, none of the three identified inhibitors is a potent haemolytic agent, and only two compounds showed moderate cytotoxic activity toward the murine myeloma P3X63Ag cells. These results point to promising compounds for the future development of rationally designed TPMs as antibacterial agents.
Publikation
Wasternack, C.;New Light on Local and Systemic Wound SignalingTrends Plant Sci.24102-105(2019)DOI: 10.1016/j.tplants.2018.11.009
Electric signaling and Ca2+ waves were discussed to occur in systemic wound responses. Two new overlapping scenarios were identified: (i) membrane depolarization in two special cell types followed by an increase in systemic cytoplasmic Ca2+ concentration ([Ca2+]cyt), and (ii) glutamate sensed by GLUTAMATE RECEPTOR LIKE proteins and followed by Ca2+-based defense in distal leaves.