Results 191 to 200 of about 47,945 (287)

Differential Water Networks Guide Selectivity Optimization of a Cell Active BPTF Inhibitor in Neuroblastoma

open access: yesAngewandte Chemie, EarlyView.
BZ2 is a second‐generation Bromodomain PHD finger Transcription Factor (BPTF) inhibitor with improved selectivity over Class I and Class IV BRD off‐targets identified in our previously reported inhibitor, BZ1. Structural analyses reveal that water network engagement is key to this selectivity.
Kesavan Babu   +19 more
wiley   +2 more sources

A Conserved Isoleucine Gates the Diffusion of CO and O2 to the Active Site of NiFe CO‐Dehydrogenase

open access: yesAngewandte Chemie, EarlyView.
A combination of protein film electrochemistry and site‐directed mutagenesis shows that isoleucine 563 (numbering of Thermococcus sp. AM4) gates the arrival of both CO and O2 to the active site of the nickel‐iron CO dehydrogenases. Mutations at this position increase the resistance to O2 at the cost of a slower reaction with CO.
Laura Opdam   +7 more
wiley   +2 more sources

Characterization of a Fungal Modular Polyketide Synthase System Reveals an Unusual Strategy for Polyketide Chain Initiation

open access: yesAngewandte Chemie, EarlyView.
Fungal modular polyketide synthases (PKSs) remain largely unexplored. Functional characterization of the LasC/LasD assembly line established its role in strasseriolide C biosynthesis and suggested an unexpected strategy for chain initiation, in which a malonyl unit is transferred from the module 2 acyl carrier protein (ACP) domains to the loading ACP ...
Qiaolin Ji   +5 more
wiley   +2 more sources

Broad‐Spectrum, Cell Envelope‐Active Marinocyclin Antibiotics From a Coral‐Derived Bacterium Are Effective Against Colistin‐Resistant Bacteria

open access: yesAngewandte Chemie, EarlyView.
Marinocyclins, polycationic macrocyclic depsipeptides, were discovered by genome mining from the marine coral‐derived bacterium Aquimarina megaterium. The compounds have broad‐spectrum activity against gram‐positive and gram‐negative ESKAPE bacteria.
Clara Chepkirui   +9 more
wiley   +2 more sources

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