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Browsing by Author "Queener, Sherry"
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Item Development of substituted pyrido[3,2-d]pyrimidines as potent and selective dihydrofolate reductase inhibitors for pneumocystis pneumonia infection(Elsevier, 2019-08-01) Shah, Khushbu; Queener, Sherry; Cody, Vivian; Pace, Jim; Gangjee, Aleem; Pharmacology and Toxicology, School of MedicinePneumocystis pneumonia (PCP) caused by Pneumocystis jirovecii (pj) can lead to serious health consequences in patients with an immunocompromised system. Trimethoprim (TMP), used as first-line therapy in combination with sulfamethoxazole, is a selective but only moderately potent pj dihydrofolate reductase (pjDHFR) inhibitor, whereas non-clinical pjDHFR inhibitors, such as, piritrexim and trimetrexate are potent but non-selective pjDHFR inhibitors. To meet the clinical needs for a potent and selective pjDHFR inhibitor for PCP treatment, fourteen 6-substituted pyrido[3,2-d]pyrimidines were developed. Comparison of the amino acid residues in the active site of pjDHFR and human DHFR (hDHFR) revealed prominent amino acid differences which could be exploited to structurally design potent and selective pjDHFR inhibitors. Molecular modeling followed by enzyme assays of the compounds revealed 15 as the best compound of the series with an IC50 of 80 nM and 28-fold selectivity for inhibiting pjDHFR over hDHFR. Compound 15 serves as the lead analog for further structural variations to afford more potent and selective pjDHFR inhibitors.Item Diversifying biomedical training: A synergistic intervention(2010) Gibau, Gina Sanchez; Foertsch, Julie; Blum, Janice; Brutkiewicz, Randy; Queener, Sherry; Roman, Ann; Rhodes, Simon; Sturek, Michael; Wilkes, David; Broxmeyer, HalFor over three decades, the scientific community has expressed concern over the paucity of African American, Latino and Native American researchers in the biomedical training pipeline. Concern has been expressed regarding what is forecasted as a shortage of these underrepresented minority (URM) scientists given the demographic shifts occurring worldwide and particularly in the United States. Increased access to graduate education has made a positive contribution in addressing this disparity. This article describes the multiple pathway approaches that have been employed by a school of medicine at an urban Midwest research institution to increase the number of URM students enrolled in, and graduating from, doctoral programs within basic science departments, through the combination of R25 grants and other grant programs funded by the National Institutes of Health (NIH). This article outlines the process of implementing a strong synergistic approach to the training of URM students through linkages between the NIH-funded "Bridges to the Doctorate (BRIDGES)" and "Initiative for Maximizing Graduate Student Diversity (IMGSD)" programs. The article documents the specific gains witnessed by this particular institution and identifies key components of the interventions that may prove useful for institutions seeking to increment the biomedical pipeline with scientists from diverse backgrounds.