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Development of a Photo-Cross-Linkable Diaminoquinazoline Inhibitor for Target Identification in Plasmodium falciparum

التفاصيل البيبلوغرافية
العنوان: Development of a Photo-Cross-Linkable Diaminoquinazoline Inhibitor for Target Identification in Plasmodium falciparum
المؤلفون: Holly Matthews, Julia Morales-Sanfrutos, Ainoa Rueda-Zubiaurre, Kate Hadavizadeh, Alexandra S. Lubin, Fabio R. Fisher, Edward W. Tate, Matthew J. Fuchter, Jake Baum, Artur Scherf, Flore Nardella, Hella Baumann
المساهمون: Imperial College London, Biologie des Interactions Hôte-Parasite - Biology of Host-Parasite Interactions, Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut Pasteur [Paris]-Centre National de la Recherche Scientifique (CNRS), Institut Pasteur [Paris] (IP)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), Wellcome Trust
المصدر: ACS Infect Dis
ACS Infectious Diseases
ACS Infectious Diseases, American Chemical Society, 2018, 4 (4), pp.523-530. ⟨10.1021/acsinfecdis.7b00228⟩
ACS Infectious Diseases, 2018, 4 (4), pp.523-530. ⟨10.1021/acsinfecdis.7b00228⟩
سنة النشر: 2018
مصطلحات موضوعية: 0301 basic medicine, QUINAZOLINES, [SDV]Life Sciences [q-bio], GLP, Plasmodium falciparum, malaria, Chemistry, Medicinal, GENE-FUNCTION, Computational biology, Plasma protein binding, Proteomics, 01 natural sciences, Article, BIX-01294, 03 medical and health sciences, Antimalarials, proteomics, Histone-lysine methyltransferase, STAGE, parasitic diseases, PANTHER, photoaffinity probe, Pharmacology & Pharmacy, HISTONE METHYLTRANSFERASE INHIBITORS, Enzyme Inhibitors, ComputingMilieux_MISCELLANEOUS, Science & Technology, pull-down, G9A, Photoaffinity labeling, biology, 010405 organic chemistry, Chemistry, CHEMICAL PROBE, Diaminoquinazoline, biology.organism_classification, 0104 chemical sciences, 3. Good health, 030104 developmental biology, Infectious Diseases, Cross-Linking Reagents, Molecular targets, ANTIMALARIAL ACTIVITY, Identification (biology), Life Sciences & Biomedicine, Protein Binding
الوصف: Diaminoquinazolines represent a privileged scaffold for antimalarial discovery, including use as putative Plasmodium histone lysine methyltransferase inhibitors. Despite this, robust evidence for their molecular targets is lacking. Here we report the design and development of a small-molecule photo-crosslinkable probe to investigate the targets of our diaminoquinazoline series. We demonstrate the effectiveness of our designed probe for photoaffinity labelling of Plasmodium lysates and identify similarities between the target profiles of the probe and the representative diaminoquinazoline BIX-01294. Initial pull-down proteomics experiments identified 104 proteins from different classes, many of which are essential, highlighting the suitability of the developed probe as a valuable tool for target identification in Plasmodium falciparum.
تدمد: 2373-8227
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aaadc3308f7dc14bf6b227dd61862f79
https://pubmed.ncbi.nlm.nih.gov/29377668
حقوق: OPEN
رقم الأكسشن: edsair.doi.dedup.....aaadc3308f7dc14bf6b227dd61862f79
قاعدة البيانات: OpenAIRE
الوصف
تدمد:23738227