Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor

Authors: Zhuang, Linghang, Tice, Colin M., Xu, Zhenrong, Zhao, Wei, Cacatian, Salvacion, Ye, Yuan-Jie, Singh, Suresh B., Lindblom, Peter, McKeever, Brian M., Krosky, Paula M., Zhao, Yi, Lala, Deepak, Kruk, Barbara A., Meng, Shi, Howard, Lamont, Johnson, Judith A., Bukhtiyarov, Yuri, Panemangalore, Reshma, Guo, Joan, Guo, Rong, Himmelsbach, Frank, Hamilton, Bradford, Schuler-Metz, Annette, Schauerte, Heike, Gregg, Richard, McGeehan, Gerard M., Leftheris, Katerina, Claremon, David A.

Source: In Bioorganic & Medicinal Chemistry 15 July 2017 25(14):3649-3657

Brain penetrant liver X receptor (LXR) modulators based on a 2, 4, 5, 6-tetrahydropyrrolo[3, 4-c]pyrazole core

Authors: Tice, Colin M., Noto, Paul B., Fan, Kristi Yi, Zhao, Wei, Lotesta, Stephen D., Dong, Chengguo, Marcus, Andrew P., Zheng, Ya-Jun, Chen, Guozhou, Wu, Zhongren, Van Orden, Rebecca, Zhou, Jing, Bukhtiyarov, Yuri, Zhao, Yi, Lipinski, Kerri, Howard, Lamont, Guo, Joan, Kandpal, Geeta, Meng, Shi, Hardy, Andrew, Krosky, Paula, Gregg, Richard E., Leftheris, Katerina, McKeever, Brian M., Singh, Suresh B., Lala, Deepak, McGeehan, Gerard M., Zhuang, Linghang, Claremon, David A.

Source: Bioorganic & medicinal chemistry letters. 26(20):5044-5050

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100069966687.0x000001&indx=1&recIds=ETOCvdc_100069966687.0x000001

Regulation of Sphingomyelin Phosphodiesterase Acid-Like 3A Gene (SMPDL3A) by Liver X Receptors

Authors: Noto, Paul B. ^*, Bukhtiyarov, Yuri, Shi, Meng, McKeever, Brian M., McGeehan, Gerard M., Lala, Deepak S.

Source: In Molecular Pharmacology October 2012 82(4):719-727

Crystal Structure of Inhibitor-Bound Human 5-Lipoxygenase: Activating Protein

Authors: Ferguson, Andrew D., McKeever, Brian M., Xu, Shihua, Wisniewski, Douglas, Miller, Douglas K., Yamin, Ting-Ting, Spencer, Robert H., Chu, Lin, Ujjainwalla, Feroze, Cunningham, Barry R., Evans, Jilly F., Becker, Joseph W.

Source: Science, 2007 Jul . 317(5837), 510-512.

Access URL: https://www.jstor.org/stable/20037456

A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia

Authors: Krivtsov, Andrei V., Evans, Kathryn, Gadrey, Jayant Y., Eschle, Benjamin K., Hatton, Charlie, Uckelmann, Hannah J., Ross, Kenneth N., Perner, Florian, Olsen, Sarah N., Pritchard, Tara, McDermott, Lisa, Jones, Connor D., Jing, Duohui, Braytee, Ali, Chacon, Diego, Earley, Eric, McKeever, Brian M., Claremon, David, Gifford, Andrew J., Lee, Heather J., Teicher, Beverly A., Pimanda, John E., Beck, Dominik, Perry, Jennifer A., Smith, Malcolm A., McGeehan, Gerard M., Lock, Richard B., Armstrong, Scott A.

Source: Cancer cell. 36(6):660-673.e11

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100093950868.0x000001&indx=1&recIds=ETOCvdc_100093950868.0x000001

Protein Crystal Growth in Microgravity

Authors: DeLucas, Lawrence J., Smith, Craig D., Smith, H. Wilson, Vijay-Kumar, Senadhi, Senadhi, Shobha E., Ealick, Steven E., Carter, Daniel C., Snyder, Robert S., Weber, Patricia C., Salemme, F. Raymond, Ohlendorf, D. H., Einspahr, H. M., Clancy, L. L., Navia, Manuel A., McKeever, Brian M., Nagabhushan, T. L., Nelson, George, McPherson, A., Koszelak, S., Taylor, G., Stammers, D., Powell, K., Darby, G., Bugg, Charles E.

Source: Science, 1989 Nov 01. 246(4930), 651-654.

Access URL: https://www.jstor.org/stable/1704856

Structure of Human Neutrophil Elastase in Complex with a Peptide Chloromethyl Ketone Inhibitor at 1.84- angstrom Resolution

Authors: Navia, Manuel A., McKeever, Brian M., Springer, James P., Lin, Tsau-Yen, Williams, Hollis R., Fluder, Eugene M., Dorn, Conrad P., Hoogsteen, Karst

Source: Proceedings of the National Academy of Sciences of the United States of America, 1989 Jan 01. 86(1), 7-11.

Access URL: https://www.jstor.org/stable/33046

Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1.

Authors: Navia, Manuel A., Fitzgerald, Paula M. D., McKeever, Brian M.

Source: Nature; February 16 1989, Vol. 337, p615-620, 6p

Amino acid substitution of arginine 80 in 17β-hydroxysteroid dehydrogenase type 3 and its effect on NADPH cofactor binding and oxidation/reduction kinetics

Authors: McKeever, Brian M ^*, Hawkins, Barton K, Geissler, Wayne M, Wu, Ling, Sheridan, Robert P, Mosley, Ralph T, Andersson, Stefan

Source: In BBA - Proteins and Proteomics 2002 1601(1):29-37

The three-dimensional structure of human granzyme B compared to caspase-3, key mediators of cell death with cleavage specificity for aspartic acid in P1

Authors: Rotonda, Jennifer ^*, Garcia-Calvo, Margarita, Bull, Herb G, Geissler, Wayne M, McKeever, Brian M, Willoughby, Christopher A, Thornberry, Nancy A, Becker, Joseph W

Source: In Chemistry & Biology 2001 8(4):357-368

Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core

Authors: Tice, Colin M., Noto, Paul B., Fan, Kristi Yi, Zhao, Wei, Lotesta, Stephen D., Dong, Chengguo, Marcus, Andrew P., Zheng, Ya-Jun, Chen, Guozhou, Wu, Zhongren, Van Orden, Rebecca, Zhou, Jing, Bukhtiyarov, Yuri, Zhao, Yi, Lipinski, Kerri, Howard, Lamont, Guo, Joan, Kandpal, Geeta, Meng, Shi, Hardy, Andrew, Krosky, Paula, Gregg, Richard E., Leftheris, Katerina, McKeever, Brian M., Singh, Suresh B., Lala, Deepak, McGeehan, Gerard M., Zhuang, Linghang, Claremon, David A.

Source: In Bioorganic & Medicinal Chemistry Letters 15 October 2016 26(20):5044-5050

Biphenyl/diphenyl ether renin inhibitors: Filling the S1 pocket of renin via the S3 pocket

Authors: Yuan, Jing, Simpson, Robert D., Zhao, Wei, Tice, Colin M., Xu, Zhenrong, Cacatian, Salvacion, Jia, Lanqi, Flaherty, Patrick T., Guo, Joan, Ishchenko, Alexey, Wu, Zhongren, McKeever, Brian M., Scott, Boyd B., Bukhtiyarov, Yuri, Berbaum, Jennifer, Panemangalore, Reshma, Bentley, Ross, Doe, Christopher P., Harrison, Richard K., McGeehan, Gerard M., Singh, Suresh B., Dillard, Lawrence W., Baldwin, John J., Claremon, David A.

Source: In Bioorganic & Medicinal Chemistry Letters 15 August 2011 21(16):4836-4843

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Spirocyclic ureas: Orally bioavailable 11β-HSD1 inhibitors identified by computer-aided drug design

Authors: Tice, Colin M., Zhao, Wei, Xu, Zhenrong, Cacatian, Salvacion T., Simpson, Robert D., Ye, Yuan-Jie, Singh, Suresh B., McKeever, Brian M., Lindblom, Peter, Guo, Joan, Krosky, Paula M., Kruk, Barbara A., Berbaum, Jennifer, Harrison, Richard K., Johnson, Judith J., Bukhtiyarov, Yuri, Panemangalore, Reshma, Scott, Boyd B., Zhao, Yi, Bruno, Joseph G., Zhuang, Linghang, McGeehan, Gerard M., He, Wei, Claremon, David A.

Source: In Bioorganic & Medicinal Chemistry Letters 2010 20(3):881-886

Optimization of orally bioavailable alkyl amine renin inhibitors

Authors: Xu, Zhenrong, Cacatian, Salvacion, Yuan, Jing, Simpson, Robert D., Jia, Lanqi, Zhao, Wei, Tice, Colin M., Flaherty, Patrick T., Guo, Joan, Ishchenko, Alexey, Singh, Suresh B., Wu, Zhongren, McKeever, Brian M., Scott, Boyd B., Bukhtiyarov, Yuri, Berbaum, Jennifer, Mason, Jennifer, Panemangalore, Reshma, Cappiello, Maria Grazia, Bentley, Ross, Doe, Christopher P., Harrison, Richard K., McGeehan, Gerard M., Dillard, Lawrence W., Baldwin, John J., Claremon, David A.

Source: In Bioorganic & Medicinal Chemistry Letters 2010 20(2):694-699

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