Publications by authors named "Benjamin Eyer"

After a high-throughput screening campaign identified thioether 1 as an antagonist of the nuclear androgen receptor, a zone model was developed for structure-activity relationship (SAR) purposes and analogues were synthesized and evaluated in a cell-based luciferase assay. A novel thioether isostere, cyclopropane (1S,2R)-27, showed the desired increased potency and structural properties (stereospecific SAR response, absence of a readily oxidized sulfur atom, low molecular weight, reduced number of flexible bonds and polar surface area, and drug-likeness score) in the prostate-specific antigen luciferase assay in C4-2-PSA-rl cells to qualify as a new lead structure for prostate cancer drug development.

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The low-molecular weight isopropyl 2-acetamido-α-glucoside (C34) inhibits toll-like receptor 4 (TLR4) in enterocytes and macrophages , and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis. We used a copper(II)-mediated solvolysis of anomeric oxazolines and an acid-mediated conversion of β-glucosamine and β-galactosamine pentaacetates to generate analogs of at the anomeric carbon and at C-4 of the pyranose ring. These compounds were evaluated for their influence on TLR4-mediated inflammatory signaling in cultured enterocytes and monocytes.

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Many inflammatory diseases may be linked to pathologically elevated signaling via the receptor for lipopolysaccharide (LPS), toll-like receptor 4 (TLR4). There has thus been great interest in the discovery of TLR4 inhibitors as potential anti-inflammatory agents. Recently, the structure of TLR4 bound to the inhibitor E5564 was solved, raising the possibility that novel TLR4 inhibitors that target the E5564-binding domain could be designed.

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Unique chemical methodology enables the synthesis of innovative and diverse scaffolds and chemotypes and allows access to previously unexplored "chemical space." Compound collections based on such new synthetic methods can provide small-molecule probes of proteins and/or pathways whose functions are not fully understood. We describe the identification, characterization, and evolution of two such probes.

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The knee is an intricate joint with numerous tendinous, ligamentous, and meniscal attachments, which make it particularly vulnerable to complex injuries after trauma. A variety of avulsion fractures of the knee can occur, including Segond and reverse Segond fractures; avulsions of the anterior and posterior cruciate ligaments; arcuate complex avulsion; iliotibial band avulsion; avulsions of the biceps femoris, semimembranosus, and quadriceps tendons; Sinding-Larsen-Johansson syndrome; and Osgood-Schlatter disease. These fractures often have a subtle appearance at conventional radiography, which is typically the first imaging modality performed in these cases.

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Objective: The purpose of our study was to investigate clinician response and patient outcome associated with the radiologist's report of isolated subsegmental pulmonary emboli (ISSPE) or indeterminate or inconclusive results on MDCT for venous thromboembolism.

Materials And Methods: All patients were examined using 8- or 16-MDCT. Reported findings on combined CT pulmonary angiography and CT venography of 1,435 consecutive patients were analyzed retrospectively.

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