9hl9

CRYO-EM STRUCTURE OF LEISHMANIA MAJOR 80S RIBOSOME WITH P/E-site tRNA AND mRNA : LM14Cs1H3 sKO STRAIN

spinqualitylabelsall models 9hl9, resolution 2.50Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 9hl9 is a 10 chain structure with sequence from Leishmania major strain Friedlin. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: Electron Microscopy, Resolution 2.5Å Ligands: 5MC, A2M, B8N, G7M, MA6, OMC, OMG, OMU, PSU Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function Q4FWX5_LEIMA Publication Abstract from PubMed Neglected tropical diseases caused by trypanosomatid parasites present a major public healthcare issue, partly due to emerging resistance. Attachment of omega-alkynyl chains characteristic of the lipid tails of antiparasitic peptides to the p-position of anisomycin gave ethers exhibiting potent activity, rivalling that of the parent ribosomal inhibitor, especially against resistant Leishmania strains. Single-particle cryoelectron microscopy analysis revealed that O-propargyl anisomycin binds to the highly conserved peptidyl transferase center of the ribosome similar to the parent inhibitor. Thermal proteomic profiling and gene ontology analysis demonstrated that O-propargyl anisomycin exhibited a broader mode of action, including activity against glycosome-associated proteins. Alkynyl substituents improved antiparasitic activity against resistant strains, likely by enlarging the mode of action, offering a novel path toward therapy against trypanosomatid infections. p-Alkoxy-Substituted Anisomycins with Potent Anti-Trypanosomiasis Activity and Expanded Modes of Action.,Bora Bhowal K, Nguyen AMT, Ibarra-Meneses AV, Brito Lira A, Rajan KS, Castano JD, Beaudry F, Bashan A, Fernandez-Prada C, Olivier M, Yonath A, Lubell WD J Med Chem. 2025 Oct 9;68(19):20264-20282. doi: 10.1021/acs.jmedchem.5c01291. , Epub 2025 Sep 22. PMID:40980996 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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