Samer S. Daher

Mycobacterium tuberculosis KasA as a drug target: Structure-based inhibitor design

Rudraraju Srilakshmi Reshma, Samer S. Daher, Ricardo Gallardo‐Macias, Xin Wang et autres

Recent studies have reported the β-ketoacyl-acyl carrier protein KasA as a druggable target for Mycobacterium tuberculosis. This review summarizes the current status of major classes of KasA inhibitors with an emphasis on significant contributions from structure-based design methods leveraging X-ray crystal structures …

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Development of amidase-dependent pyrazinoic acid prodrugs with activity against pyrazinamide resistant Mycobacterium tuberculosis

Carly Levine, Ravindra D. Jadhav, Yan Pan, Kholiswa Tsotetsi et autres

ABSTRACT Rapid emergence of drug resistance in Mycobacterium tuberculosis (Mtb) is one of the most significant healthcare challenges of our time. The cause of drug resistance is multifactorial, with the long course anti-tubercular therapy required to treat tuberculosis (TB) constituting a major …

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Rickettsia Aglow: A Fluorescence Assay and Machine Learning Model to Identify Inhibitors of Intracellular Infection

Alexander D. Lemenze, Nisha Mittal, Alexander L. Perryman, Samer S. Daher et autres

Rickettsia is a genus of Gram-negative bacteria that has for centuries caused large-scale morbidity and mortality. In recent years, the resurgence of rickettsial diseases as a major cause of pyrexias of unknown origin, bioterrorism concerns, vector movement, and concerns over drug resistance …

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Alternative approaches utilizing click chemistry to develop next-generation analogs of solithromycin

Samer S. Daher, Miseon Lee, Xiao Jin, Christiana N. Teijaro et autres

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Synthesis, Biological Evaluation, and Computational Analysis of Biaryl Side‐Chain Analogs of Solithromycin

Samer S. Daher, Miseon Lee, Xiao Jin, Christiana N. Teijaro et autres

Abstract There is an urgent need for new antibiotics to mitigate the existential threat posed by antibiotic resistance. Within the ketolide class, solithromycin has emerged as one of the most promising candidates for further development. Crystallographic studies of bacterial ribosomes and ribosomal …

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Bayesian Modeling and Intrabacterial Drug Metabolism Applied to Drug-Resistant Staphylococcus aureus

Jimmy S. Patel, Javiera Norambuena, Hassan Al‐Tameemi, Yong-Mo Ahn et autres

We present the application of Bayesian modeling to identify chemical tools and/or drug discovery entities pertinent to drug-resistant Staphylococcus aureus infections. The quinoline JSF-3151 was predicted by modeling and then empirically demonstrated to be active against in vitro cultured clinical methicillin- and …

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Assessment of carbapenems in a mouse model of Mycobacterium tuberculosis infection

Ravindra D. Jadhav, Ricardo Gallardo‐Macias, Gaurav Kumar, Samer S. Daher et autres

We present further study of a subset of carbapenems, arising from a previously reported machine learning approach, with regard to their mouse pharmacokinetic profiling and subsequent study in a mouse model of sub-acute Mycobacterium tuberculosis infection. Pharmacokinetic metrics for such small molecules …

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Staphylococcus aureus resistance to albocycline can be achieved by mutations that alter cellular NAD/PH pools

Tyler Scherzi, Elizabeth A. D’Ambrosio, Samer S. Daher, Catherine Leimkuhler Grimes et autres

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Synthesis and biological evaluation of semi-synthetic albocycline analogs

Samer S. Daher, Kevin P. Franklin, Tyler Scherzi, Paul M. Dunman et autres

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Machine Learning Platform to Discover Novel Growth Inhibitors of Neisseria gonorrhoeae

Janaína Cruz Pereira, Samer S. Daher, Kimberley M. Zorn, Matthew Sherwood et autres

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VIPはATF6α経路を通して小胞体ストレスを特権することによってヒト子宮内膜受容性を条件する【JST・京大機械翻訳】

Elizabeth Soczewski, Soledad Gori, Daniel Paparini, E. Grasso et autres

Synthesis and biological evaluation of solithromycin analogs against multidrug resistant pathogens

Samer S. Daher, Xiao Jin, Jimmy S. Patel, Joel S. Freundlich et autres

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